SitesBLAST

D54 (≠ E41) mutation to A: Loss of transport activity.; mutation to E: Retains 50% of its transport activity.
D57 (= D44) mutation to A: Loss of transport activity.; mutation to E: Retains 50% of its transport activity.
R103 (≠ K97) mutation to A: Loss of transport activity.

Sites not aligning to the query:

309 W→V: Loss of transport activity.
312 D→A: Loss of transport activity.
313 R→A: Loss of transport activity.
317 mutation I->H,Y: Loss of transport activity.
386 R→A: Loss of transport activity.

O15244 Solute carrier family 22 member 2; Organic cation transporter 2; hOCT2 from Homo sapiens (Human) (see 8 papers)
23% identity, 73% coverage: 86:415/454 of query aligns to 162:492/555 of O15244

query
sites
O15244

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M165 (≠ I89) to I: lower Vmax for MPP(+) transport; no change in transport efficiency (Vmax/Km) and clearance of cyclo(his-pro) and salsolinol; dbSNP:rs8177507
Y169 (≠ H93) mutation to F: No change in TEA uptake.
T201 (≠ N125) to M: in dbSNP:rs145450955
Y241 (≠ V173) mutation to F: Slight decrease in TEA uptake. No change in tyrosine phosphorylation. Strong decrease in TEA uptake; when associated with F-362. Strong decrease in TEA and metformin uptake and YES1-mediated tyrosine phosphorylation; when associated with F-362 and F-377.
Y257 (≠ F188) mutation to F: No change in TEA uptake.
S270 (≠ M193) to A: decreased Ki value for TBA inhibition of MPP(+); no change in transport efficiency (Vmax/Km) and clearance of cyclo(his-pro) and salsolinol; dbSNP:rs316019
Y279 (≠ W202) mutation to F: No change in TEA uptake.
Y280 (≠ G203) mutation to F: No change in TEA uptake.
P284 (= P207) mutation to A: Decreased TEA and metformin uptake. Decreased tyrosine phosphorylation.
PESPR 284:288 (≠ P---- 207) Proline-rich sequence
S286 (vs. gap) mutation to A: No change in TEA and metformin uptake. No change in tyrosine phosphorylation.
P287 (vs. gap) mutation to A: Decreased TEA and metformin uptake. Decreased tyrosine phosphorylation.
Y362 (≠ M284) mutation to F: Decreased TEA uptake and YES1-mediated tyrosine phosphorylation. Strong decrease in TEA uptake; when associated with F-241. Strong decrease in TEA uptake; when associated with F-377. Strong decrease in TEA and metformin uptake and YES1-mediated tyrosine phosphorylation; when associated with F-241 and F-377.
Y377 (≠ L299) mutation to F: Slight decrease in TEA uptake. No change in tyrosine phosphorylation. Strong decrease in TEA uptake; when associated with F-362. Strong decrease in TEA and metformin uptake and YES1-mediated tyrosine phosphorylation; when associated with F-241 and F-362.
R400 (≠ K322) to C: lower Vmax and reduced Ki value for TBA inhibition of MPP(+); lower transport efficiency (Vmax/Km) and clearance of cyclo(his-pro); no change in transport efficiency (Vmax/Km) and clearance of salsolinol; dbSNP:rs8177516
K432 (≠ M356) to Q: lower Km value for MPP(+) and reduced Ki value for TBA inhibition of MPP; no change in transport efficiency (Vmax/Km) and clearance of cyclo(his-pro) and salsolinol; dbSNP:rs8177517
Y458 (≠ F382) mutation to F: No change in TEA uptake.

Sites not aligning to the query:

54 P → S: in dbSNP:rs8177504
73 Y→F: No change in TEA uptake.
92 Y→F: No change in TEA uptake.
128 Y→F: No change in TEA uptake.
544 Y→F: No change in TEA uptake.

Q9R0W2 Solute carrier family 22 member 2; Organic cation transporter 2; rOCT2 from Rattus norvegicus (Rat) (see paper)
23% identity, 71% coverage: 86:408/454 of query aligns to 162:484/555 of Q9R0W2

query
sites
Q9R0W2

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C451 (≠ P375) Involved in recognition of organic cations and participates in structural changes that occur during translocation of organic cations; mutation to M: Transport activity strongly reduced.

8bw7A Cryo-em structure of rat slc22a6 bound to alpha-ketoglutaric acid (see paper)
23% identity, 74% coverage: 75:408/454 of query aligns to 118:447/497 of 8bw7A

query
sites
8bw7A

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binding 2-oxoglutaric acid: G209 (≠ Q174), Y212 (≠ N177), K354 (vs. gap)

8et9A Cryo-em structure of the organic cation transporter 2 in complex with 1-methyl-4-phenylpyridinium (see paper)
26% identity, 71% coverage: 86:408/454 of query aligns to 160:467/517 of 8et9A

query
sites
8et9A

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V

S

L

V

G

G

L

L

F

L

I

V

A

L

T

A

G

G

V

V

-

A

-

Y

-

A

-

I

-

P

-

H

-

W

-

R

-

W

F

L

A

Q

L

L

V

A

V

V

M

T

L

L

P

P

E

N

E

F

D

F

L

F

M

L

S

L

W

Y

G

Y

W

W

R

C

V

I

P

P

-

E

-

S

-

P

-

R

F

W

L

L

L

I

S

S

I

Q

A

N

L

K

L

N

F

A

V

K

G

A

M

M

F

K

I

I

R

I

S

K

R

H

I

I

E

A

E

-

T

-

P

-

V

-

F

-

Q

-

E

-

N

-

Q

K

K

K

Q

N

Q

G

Q

K

N

K

A

L

P

P

K

K

A

S

A

E

E

K

Q

L

K

N

F

P

P

S

I

F

L

L

T

D

V

L

L

V

K

R

-

T

-

P

H

Q

H

I

R

R

K

K

A

H

V

T

F

L

L

I

A

L

M

M

G

Y

-

N

-

W

-

F

-

T

-

S

-

V

-

L

-

Y

-

Q

-

G

-

L

-

I

M

M

R

H

M

M

G

G

E

-

I

I

V

A

L

G

G

G

W

N

L

I

T

Y

V

L

A

D

F

F

M

Y

S

S

Y

A

V

L

T

V

R

E

E

-

L

-

N

-

F

-

T

-

R

-

E

-

T

-

A

-

L

-

N

-

G

-

L

-

L

F

L

P

A

A

S

A

F

F

V

I

G

I

I

I

F

L

T

T

F

I

P

-

F

-

G

-

W

-

L

-

S

-

D

D

K

R

I

I

G

G

R

R

P

Y

V

P

Y

W

-

A

-

N

L

M

A

V

G

A

A

G

A

A

I

A

T

C

L

L

I

I

F

T

A

A

F

F

P

-

L

L

F

F

W

W

M

L

I

K

D

-

S

-

G

-

S

-

V

-

K

-

M

-

F

-

M

-

F

-

A

T

T

T

T

V

F

A

C

C

Y

L

-

G

S

R

V

M

G

G

L

I

G

T

M

M

M

A

F
|
F

S

E

V

M

Q

V

P

C

A

F

F

V

F

N

S

T

E

E

L

L

F

Y

D

P

T

T

S

F

V

I

R

R

Y

N

T

L

G

G

V

V

S

L

L

V

G

C

F

S

Q

S

L

L

A

C

N

D

I

I

V

G

G

G

G

I

L

I

T

T

P

P

M

F

I

L

binding 1-methyl-4-phenylpyridin-1-ium: W216 (= W150), Q240 (= Q174), F243 (≠ N177), F430 (= F371)

8bvsA Cryo-em structure of rat slc22a6 bound to tenofovir (see paper)
24% identity, 74% coverage: 75:408/454 of query aligns to 118:451/502 of 8bvsA

query
sites
8bvsA

L

L

T

A

L

Q

S

S

I

L

T

Y

F

M

V

V

S

G

R

V

P

L

I

L

G

G

A

A

I

M

V

V

F

F

G

G

H

Y

Y

L

G

A

D

D

K

R

I

L

G

G

R

R

K

R

K

K

S

V

L

L

V

I

L

L

S

N

L

Y

M

L

I

Q

M

T

G

A

I

V

S

S

T

G

F

T

F

C

I

A

G

A

L

Y

I

A

P

P

S

N

Y

Y

N

T

T

-

I

-

G

-

N

-

A

-

P

-

L

-

I

V

L

Y

I

C

F

V

L

F

R

R

L

L

C

L

Q

S

G

G

F

M

A

S

I

L

G

A

G

S

E

I

W

A

G

I

G

N

A

C

T

M

T

T

L

L

I

N

T

V

E

E

Y

W

A

M

P

P

R

I

H

H

R

T

R

R

G

A

F

Y

F

V

G

G

T

T

F

L

V

I

Q

G

L

Y

G

V

N
x
Y

V

S

L

L

G

G

L

Q

F

F

I

L

A

L

T

A

G

G

V

I

F

A

A

Y

L

A

V

V

V

-

M

-

L

-

P

P

E

H

E

W

D

R

L

H

M

L

S

Q

W

L

G

V

W

V

R

S

V

V

P

P

F

F

L

F

L

-

S

-

I

I

A

A

L

F

L

I

F

Y

V

S

G

W

M

F

F

F

I

I

R

E

S

S

-

A

-

R

-

W

-

Y

-

S

-

G

R

R

I

L

E

D

E

L

T

T

-

L

-

R

-

A

-

L

-

Q

P

R

V

V

F

A

Q

R

E

I

N

N

Q

G

K

K

Q

Q

Q

E

N

G

A

A

P

K

K

L

A

S

A

I

E

E

-

V

-

L

-

R

-

T

-

S

-

L

Q

Q

K

K

F

-

P

E

I

L

L

T

T

S

V

A

L

M

K

E

H

L

R

R

-

C

-

P

-

T

-

L

K

R

A

H

V

L

F

F

L

L

A

C

M

L

G

S

M

M

R

L

M

-

G

-

E

-

I

-

V

-

L

-

G

-

W

W

L

F

T

A

V

T

A

S

F

F

F

A

M

Y

S
x
Y

Y

G

V

L

T

V

R

M

E

D

L

L

N

-

F

-

T

-

R

Q

E

G

T

F

A

G

L

V

N

S

G

M

L

Y

L

L

L

I

A

Q

S

V

F

I

V

F

G

G

I

A

F

V

T

D

F

L

P

P

-

A

-

K

F

F

F

V

G

C

W

F

L

L

S

V

-

I

D

N

K

S

I

M

G

G

R

R

P

P

V

A

Y

Q

L

M

A

A

G

-

A

-

I

-

T

S

L

L

I

L

F

L

A

A

F

-

P

G

L

I

F

C

W

I

M

L

I

V

D

N

S

G

G

I

S

I

V

P

K

K

M

S

F

H

M

T

F

I

A

I

T

R

T

T

F

S

C

L

Y

A

S

V

V

L

G

G

L

K

G

G

M

C

M

L

F

A

S

S

V

S

Q

F

P

N

A

C

F

I

F

F

-

L

-

Y

-

T

S

G

E

E

L

L

F

Y

D

P

T

T

S

V

V

I

R

R

Y

Q

T

T

G

G

V

L

S

G

L

M

G

G

F

S

Q

T

L

M

A

A

N

R

I

V

V

G

G

S

G

I

L

V

T

S

P

P

M

L

I

V

binding [2-(6-amino-9h-purin-9-yl)-1-methylethoxy]methylphosphonic acid: Y212 (≠ N177), Y330 (≠ S285)

8bvtA Cryo-em structure of rat slc22a6 bound to probenecid (see paper)
23% identity, 74% coverage: 75:408/454 of query aligns to 127:460/508 of 8bvtA

query
sites
8bvtA

L

L

T

A

L

Q

S

S

I

L

T

Y

F

M

V

V

S

G

R

V

P

L

I

L

G

G

A

A

I

M

V

V

F

F

G

G

H

Y

Y

L

G

A

D

D

K

R

I

L

G

G

R

R

K

R

K

K

S

V

L

L

V

I

L

L

S

N

L

Y

M

L

I

Q

M

T

G

A

I

V

S

S

T

G

F

T

F

C

I

A

G

A

L

Y

I

A

P

P

S

N

Y

Y

N

T

T

-

I

-

G

-

N

-

A

-

P

-

L

-

I

V

L

Y

I

C

F

V

L

F

R

R

L

L

C

L

Q

S

G

G

F

M

A

S

I

L

G

A

G

S

E

I

W

A

G

I

G

N

A

C

T
x
M

T

T

L

L

I

N

T

V

E

E

Y

W

A

M

P

P

R

I

H

H

R

T

R

R

G

A

F

Y

F

V

G

G

T

T

F

L

V
x
I

Q

G

L

Y

G

V

N
x
Y

V

S

L

L

G

G

L

Q

F

F

I

L

A

L

T

A

G

G

V

I

F

A

A

Y

L

A

V

V

V

-

M

-

L

-

P

P

E

H

E

W

D

R

L

H

M

L

S

Q

W

L

G

V

W

V

R

S

V

V

P

P

F

F

L

F

L

-

S

-

I

I

A

A

L

F

L

I

F

Y

V

S

G

W

M

F

F

F

I

I

R

E

S

S

-

A

-

R

-

W

-

Y

-

S

-

G

R

R

I

L

E

D

E

L

T

T

-

L

-

R

-

A

-

L

-

Q

P

R

V

V

F

A

Q

R

E

I

N

N

Q

G

K

K

Q

Q

Q

E

N

G

A

A

P

K

K

L

A

S

A

I

E

E

-

V

-

L

-

R

-

T

-

S

-

L

Q

Q

K

K

F

-

P

E

I

L

L

T

T

S

V

A

L

M

K

E

H

L

R

R

-

C

-

P

-

T

-

L

K

R

A

H

V

L

F

F

L

L

A

C

M

L

G

S

M

M

R

L

M

-

G

-

E

-

I

-

V

-

L

-

G

-

W

W

L

F

T

A

V

T

A

S

F

F

F

A

M

Y

S
x
Y

Y

G

V

L

T

V

R

M

E

D

L

L

N

-

F

-

T

-

R

Q

E

G

T

F

A

G

L

V

N

S

G

M

L

Y

L

L

L

I

A

Q

S

V

F

I

V

F

G

G

I

A

F

V

T

D

F

L

P

P

-

A

-

K

F

F

F

V

G

C

W

F

L

L

S

V

-

I

D

N

K

S

I

M

G

G

R

R

P

P

V

A

Y

Q

L

M

A

A

G

S

A

L

I

L

T

A

L

G

I

I

F

C

A

I

F

-

P

-

L

-

F

-

W

-

M

L

I

V

D

N

S

G

G

I

S

I

V

P

K

K

M

S

F

H

M

T

F

I

A

I

T

R

T

T

F

S

C

L

Y

A

S

V

V

L

G

G

L

K

G

G

M

C

M

L

F

A

S

S

V

S

Q

F

P

N

A

C

F

I

F

F

-

L

-

Y

-

T

S

G

E

E

L

L

F

Y

D

P

T

T

S

V

V

I

R

R

Y

Q

T

T

G

G

V

L

S

G

L

M

G

G

F

S

Q

T

L

M

A

A

N

R

I

V

V

G

G

S

G

I

L

V

T

S

P

P

M

L

I

V

binding 4-(dipropylsulfamoyl)benzoic acid: M198 (≠ T154), I217 (≠ V173), Y221 (≠ N177), Y339 (≠ S285)

Sites not aligning to the query:

binding 4-(dipropylsulfamoyl)benzoic acid: 31, 35

Q8VC69 Solute carrier family 22 member 6; Kidney-specific transport protein; Novel kidney transcript; mNKT; Organic anion transporter 1; mOAT1; Renal organic anion transporter 1; mROAT1 from Mus musculus (Mouse) (see 2 papers)
24% identity, 71% coverage: 86:408/454 of query aligns to 141:469/545 of Q8VC69

query
sites
Q8VC69

I

L

G

G

A

A

I

M

V

M

F

F

G

G

H

Y

Y

L

G

A

D

D

K

R

I

L

G

G

R

R

K

R

K

K

S

V

L

L

V

I

L

L

S

N

L

Y

M

L

I

Q

M

T

G

A

I

V

S

S

T

G

F

T

F

C

I

A

G

A

L

Y

I

A

P

P

S

N

Y

Y

N

T

T

-

I

-

G

-

N

-

A

-

P

-

L

-

I

V

L

Y

I
x
C

F

I

L

F

R

R

L

L

C

L

Q

S

G

G

F

M

A

S

I

L

G

A

G

S

E

I

W

A

G

I

G

N

A

C

T

M

T

T

L

L

I

N

T

M

E

E

Y

W

A

M

P

P

R

I

H

H

R

T

R

R

G

A

F

Y

F

V

G

G

T

T

F

L

V

I

Q

G

L

Y

G

V

N

Y

V

S

L

L

G

G

L

Q

F

F

I

L

A

L

T

A

G

G

V

I

F

A

A

Y

L

A

V

V

V

-

M

-

L

-

P

P

E

H

E

W

D

R

L

H

M

L

S

Q

W

L

G

A

W

V

R

S

V

V

P

P

F

F

L

F

L

-

S

-

I

V

A

A

L

F

L

I

F

Y

V

S

G

W

M

F

F

F

I

I

R

E

S

S

-

A

-

R

-

W

-

Y

-

S

-

G

R

R

I

L

E

D

E

L

T

T

-

L

-

R

-

A

-

L

-

Q

P

R

V

V

F

A

Q

R

E

I

N

N

Q

G

K

K

Q

Q

Q

E

N

G

A

A

P

K

K

L

A

S

A

I

E

E

-

V

-

L

-

Q

-

T

-

S

-

L

Q

Q

K

K

F

E

P

-

I

-

L

L

T

T

V

L

L

N

K

K

H

G

H

Q

R

A

K

S

A

A

V

M

F

E

L

L

A

L

M

R

G

C

M

P

R

T

M

L

G

R

E

R

I

L

V

F

L

L

G

C

W

L

L

S

T

M

V

L

A

W

F

F

F

A

M

T

S

S

Y

F

V

A

T

Y

R

Y

E

G

L

L

N

V

F

M

T

D

R

L

E

Q

T

G

-

F

A

G

L

V

N

S

G

M

L

Y

L

L

L

I

A

Q

S

V

F

I

V

F

G

G

I

A

F

V

T

D

F

L

P

P

-

A

-

K

F

F

F

V

G

C

W

F

L

L

S

V

-

I

D

N

K

S

I

M

G

G

R

R

P

P

-

A

-

Q

-

L

-

A

-

S

V

L

Y

L

L

L

A

A

G

G

A

I

A

C

I

I

T

L

L

V

I

N

F

G

A

I

F

I

P

P

L

R

F

G

W

H

M

T

I

I

D

I

S

R

G

T

S

S

V

L

K

A

M

V

F

L

M

-

F

-

A

-

T

G

T

K

F

G

C

C

Y

L

S

A

V

S

G

S

L

F

G

N

M
x
C

M

I

F

F

S

-

V

-

Q

-

P

-

A

L

F

Y

F

T

S

G

E

E

L

L

F

Y

D

P

T

T

S

M

V

I

R

R

Y

Q

T

T

G

G

V

L

S

G

L

M

G

G

F

S

Q

T

L

M

A

A

N

R

I

V

V

G

G

S

G

I

L

V

T

S

P

P

M

L

I

I

C183 (≠ I136) mutation to A: Decreased cell surface expression level and PAH transport activity. Complete loss of PAH transport activity; when associated with A-49; A-78; A-99; A-122; A-172; A-200; A-362; A-335; A-379; A-402; A-427 and A-434.
C434 (≠ M369) mutation to A: Decreased cell surface expression level and PAH transport activity. 80% decrease of PAH transport activity; when associated with A-49; A-122 and A-183. Complete loss of PAH transport activity; when associated with A-49; A-78; A-99; A-122; A-172; A-183; A-200; A-362; A-335; A-379; A-402 and A-427.

Sites not aligning to the query:

39 N→Q: Complete loss of PAH transport activity.
49 C→A: Decreased cell surface expression level and PAH transport activity. Complete loss of PAH transport activity; when associated with A-78; A-99; A-122; A-172; A-183; A-200; A-362; A-335; A-379; A-402; A-427 and A-434.
56 modified: carbohydrate, N-linked (GlcNAc...) asparagine
86 modified: carbohydrate, N-linked (GlcNAc...) asparagine
91 modified: carbohydrate, N-linked (GlcNAc...) asparagine
107 modified: carbohydrate, N-linked (GlcNAc...) asparagine
122 C→A: Decreased cell surface expression level and PAH transport activity. Complete loss of PAH transport activity; when associated with A-49; A-78; A-99; A-172; A-183; A-200; A-362; A-335; A-379; A-402; A-427 and A-434.

8et8A Cryo-em structure of the organic cation transporter 1 in complex with verapamil (see paper)
22% identity, 73% coverage: 86:417/454 of query aligns to 160:492/532 of 8et8A

query
sites
8et8A

I

L

G

G

A

S

I

L

V

G

F

V

G

G

H

Y

Y

I

G

A

D

D

K

R

I

F

G

G

R

R

K

K

K

L

S

C

L

L

V

L

L

A

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T

L

T

M

L

I

I

M

S

G

A

I

V

S

S

T

G

F

V

F

L

I

M

G

A

L

V

I

A

P

P

S

D

Y

Y

N

T

T

S

I

-

G

-

N

-

A

-

P

-

L

-

I

-

L

M

I

L

F

L

L

F

R

R

L

L

C

L

Q

Q

G

G

F

L

A

V

I

S

G
x
K

G

G

E

S

W
|
W

G

M

G

S

A

G

T

Y

T

T

L

L

I

I

T

T

E

E

Y

F

A

V

P

G

R

S

H

G

R

Y

R

R

G

R

F

T

F

V

G

A

T

I

F

L

V

Y

Q
|
Q

L

M

G

A

N

F

V

T

L

V

G

G

L

L

F

V

I

L

A

L

T

S

G

G

V

V

-

A

-

Y

-

A

-

I

-

P

-

H

-

W

-

R

-

W

F

L

A

Q

L

L

V

A

V

V

M

S

L

L

P

P

E

T

E

F

D

L

L

F

M

L

S

L

W

Y

G

Y

W

W

R

C

V

V

P

P

-

E

-

S

-

P

-

R

F

W

L

L

S

S

I

Q

A

K

L

R

L

N

F

T

V

Q

G

A

M

I

F

K

I

I

R

M

S

D

R

H

I

I

E

A

E

Q

T

K

-

N

-

G

-

K

-

L

-

P

P

P

V

A

F

D

Q

L

E

K

N

M

Q

L

K

S

Q

L

Q

K

Q

E

N

D

A

S

P

T

K

E

A

K

A

L

E

S

Q

P

K

S

F

F

P

A

I

D

L

L

T

F

V

R

L

T

K

P

H

Q

H

L

R

R

K

K

A

H

V

T

F

F

L

I

A

L

M

M

G

Y

M

L

R
x
W

M

F

G

T

E

S

I

S

V

V

L

L

-
x
Y

-

Q

-

G

-

L

-

I

-

M

-

H

-

M

-

G

-

A

-

T

-

G

G

G

W

N

L

L

T

Y

V

L

A

D

F
|
F

F

F

M

Y

S
|
S

Y

A

V

L

T

V

R
x
E

E

-

L

-

N

-

F

-

T

-

R

-

E

-

T

-

A

-

L

-

N

-

G

-

L

-

L

F

L

P

A

A

S

A

F

F

V

I

G

I

I

L

F

V

T

T

F

I

P

-

F

-

G

-

W

-

L

-

S

-

D

D

K

R

I

V

G

G

R

R

R

-

P

-

V

I

Y

Y

L

P

A

L

G

A

A

V

A

S

I

N

T

L

L

V

I

A

F

G

A

A

F

A

P

C

L

L

F

I

W

M

M

I

I

F

D

I

S

S

G

Q

S

D

V

L

K

H

M

W

F

L

M

N

F

I

A

T

T

V

T

A

F

C

C

V

Y

G

S

R

V

M

G

G

L

I

G

T

M

I

M

V

F

F

S

Q

V

M

Q

V

P
x
C

A

L

F

V

F

N

S

A

E

E

L

L

F

Y

D

P

T

T

S

F

V

I

R

R

Y

N

T

L

G

G

V

V

S

M

L

V

G

C

F
x
S

Q

S

L

L

A

C

N

D

I

L

V

G

G

G

G

I

L

I

T

T

P

P

-

F

M

L

I

V

G

F

T

R

L

L

L

M

L

E

V

V

W

W

S

Q

G

G

binding (2S)-2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile: K213 (≠ G147), W216 (= W150), Q240 (= Q174), W353 (≠ R269), Y360 (vs. gap), F378 (= F282), S381 (= S285), E385 (≠ R289), C449 (≠ P375), S469 (≠ F395)

Sites not aligning to the query:

binding (2S)-2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile: 31, 35

8et7A Cryo-em structure of the organic cation transporter 1 in complex with diphenhydramine (see paper)
22% identity, 73% coverage: 86:417/454 of query aligns to 160:492/532 of 8et7A

query
sites
8et7A

I

L

G

G

A

S

I

L

V

G

F

V

G

G

H

Y

Y

I

G

A

D

D

K

R

I

F

G

G

R

R

K

K

K

L

S

C

L

L

V

L

L

A

S

T

L

T

M

L

I

I

M

S

G

A

I

V

S

S

T

G

F

V

F

L

I

M

G

A

L

V

I

A

P

P

S

D

Y

Y

N

T

T

S

I

-

G

-

N

-

A

-

P

-

L

-

I

-

L

M

I

L

F

L

L

F

R

R

L

L

C

L

Q

Q

G

G

F

L

A

V

I

S

G

K

G

G

E

S

W

W

G

M

G

S

A

G

T

Y

T

T

L

L

I

I

T

T

E

E

Y

F

A

V

P

G

R

S

H

G

R

Y

R

R

G

R

F

T

F

V

G

A

T

I

F

L

V

Y

Q

Q

L

M

G

A

N

F

V

T

L

V

G

G

L

L

F

V

I

L

A

L

T

S

G

G

V

V

-

A

-

Y

-

A

-

I

-

P

-

H

-

W

-

R

-

W

F

L

A

Q

L

L

V

A

V

V

M

S

L

L

P

P

E

T

E

F

D

L

L

F

M

L

S

L

W

Y

G

Y

W

W

R

C

V

V

P

P

-

E

-

S

-

P

-

R

F

W

L

L

S

S

I

Q

A

K

L

R

L

N

F

T

V

Q

G

A

M

I

F

K

I

I

R

M

S

D

R

H

I

I

E

A

E

Q

T

K

-

N

-

G

-

K

-

L

-

P

P

P

V

A

F

D

Q

L

E

K

N

M

Q

L

K

S

Q

L

Q

K

Q

E

N

D

A

S

P

T

K

E

A

K

A

L

E

S

Q

P

K

S

F

F

P

A

I

D

L

L

T

F

V

R

L

T

K

P

H

Q

H

L

R

R

K

K

A

H

V

T

F

F

L

I

A

L

M

M

G

Y

M

L

R

W

M

F

G

T

E

S

I

S

V

V

L

L

-

Y

-

Q

-

G

-

L

-

I

-

M

-

H

-

M

-

G

-

A

-

T

-

G

G

G

W

N

L

L

T

Y

V

L

A

D

F

F

M

Y

S

S

Y

A

V

L

T

V

R
x
E

E

-

L

-

N

-

F

-

T

-

R

-

E

-

T

-

A

-

L

-

N

-

G

-

L

-

L

F

L

P

A

A

S

A

F

F

V

I

G

I

I

L

F

V

T

T

F

I

P

-

F

-

G

-

W

-

L

-

S

-

D

D

K

R

I

V

G

G

R

R

R

-

P

-

V

I

Y

Y

L

P

A

L

G

A

A

V

A

S

I

N

T

L

L

V

I

A

F

G

A

A

F

A

P

C

L

L

F

I

W

M

M

I

I

F

D

I

S

S

G

Q

S

D

V

L

K

H

M

W

F

L

M

N

F

I

A

T

T

V

T

A

F

C

C

V

Y

G

S

R

V

M

G

G

L

I

G

T

M

I

M

V

F
|
F

S

Q

V

M

Q

V

P

C

A

L

F

V

F

N

S

A

E

E

L

L

F

Y

D

P

T

T

S

F

V

I

R

R

Y

N

T

L

G

G

V

V

S

M

L

V

G

C

F

S

Q

S

L

L

A

C

N

D

I

L

V

G

G

G

G

I

L

I

T

T

P

P

-

F

M

L

I

V

G

F

T

R

L

L

L

M

L

E

V

V

W

W

S

Q

G

G

binding n-[2-(benzhydryloxy)ethyl]-n,n-dimethylamine: E385 (≠ R289), F445 (= F371)

Sites not aligning to the query:

binding n-[2-(benzhydryloxy)ethyl]-n,n-dimethylamine: 35

O08966 Solute carrier family 22 member 1; Organic cation transporter 1; mOCT1 from Mus musculus (Mouse) (see paper)
24% identity, 73% coverage: 86:417/454 of query aligns to 162:494/556 of O08966

query
sites
O08966

I

L

G

G

A

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I

L

V

V

F

V

G

G

H

Y

Y

I

G

A

D

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K

R

I

F

G

G

R

R

K

K

K

L

S

C

L

L

V

L

L

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T

L

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M

L

I

V

M

T

G

S

I

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S

T

G

F

V

F

L

I

T

G

A

L

V

I

A

P

P

S

D

Y

Y

N

T

T

S

I

-

G

-

N

-

A

-

P

-

L

-

I

-

L

M

I

L

F

L

L

F

R

R

L

L

C

L

Q

Q

G

G

F

M

A

V

I

S

G

K

G

G

E

S

W

W

G

V

G

S

A

G

T

Y

T

T

L

L

I

I

T

T

E

E

Y

F

A

V

P

G

R

S

H

G

R

Y

R

R

G

R

F

T

G

A

T

I

F

L

V

Y

Q

Q

L

V

G

A

N

F

V

T

L

V

G

G

L

L

F

V

I

G

A

L

T

A

G

G

V

V

-

A

-

Y

-

A

-

I

-

P

-

D

-

W

-

R

-

W

F

L

A

Q

L

L

V

A

V

V

M

S

L

L

P

P

E

T

E

F

D

L

L

F

M

L

S

L

W

Y

G

Y

W

W

R

F

V

V

P

P

-

E

-

S

-

P

-

R

F

W

L

L

S

S

I

-

A

-

L

-

F

-

V

-

G

-

M

-

F

-

I

-

R

Q

S

K

R

R

I

T

E

T

E

Q

T

A

P

V

V

R

F

I

Q

M

E

E

N

Q

Q

I

K

A

Q

Q

Q

K

Q

N

N

R

A

K

P

V

K

P

A

P

A

A

E

D

Q

L

K

K

F

M

P

M

I

C

L

L

T

E

V

E

L

D

K

A

H

S

H

E

R

R

K

R

A

S

-

P

-

S

-

F

-

A

-

D

V

L

F

F

L

R

A

T

M

P

G

S

M

L

R

R

M

K

G

H

E

T

I

L

V

I

L

L

G

M

-

Y

-

L

W

W

L

F

T

S

V

C

A

A

F

V

F

L

M

Y

S

Q

Y

G

V

L

T

I

R

M

E

H

L

V

N

G

F

A

T

T

R

G

E

A

T

N

A

L

L

Y

N

L

G

D

L

F

L

Y

A

S

S

S

F

L

V

V

G

E

I

-

F

F

T

P

F

A

P

A

F

F

F

I

G

I

W

L

L

V

S

T

-

I

D

D

K

R

I

I

G

G

R

R

-

I

R

Y

P

P

V

I

-

A

-

S

-

N

Y

L

L

V

A

A

G

G

A

A

I

C

T

L

L

L

I

M

F

I

A

F

F

I

P

P

-

H

-

E

L

L

F

H

W

W

M

L

I

N

D

V

S

T

G

L

S

A

V

C

K

L

M

G

F

R

M

M

F

G

A

A

T

T

T

-

F

-

C

-

Y

-

S

-

V

I

G

V

L

L

G

Q

M

M

M

V

F

C

S

L

V

V

Q

N

P

-

A

-

F

-

S

A

E

E

L

L

F

Y

D

P

T

T

S

F

V

I

R

R

Y

N

T

L

G

G

V

M

S

M

L

V

G

C

F

S

Q

A

L

L

A

C

N

D

I

L

V

G

G

G

G

I

L

F

T

T

P

P

-

F

M

M

I

V

G

F

T

R

L

L

L

M

L

E

V

V

W

W

S

Q

G

A

Sites not aligning to the query:

32 L→F: Increased trospium uptake. Increased trospium affinity. No change in fenoterol uptake.
36 Y→C: Decreased fenoterol uptake. Decreased fenoterol affinity. No change in trospium uptake. No change in terbutaline affinity.

Q4U2R8 Solute carrier family 22 member 6; Organic anion transporter 1; hOAT1; PAH transporter; hPAHT; Renal organic anion transporter 1; hROAT1 from Homo sapiens (Human) (see 6 papers)
32% identity, 25% coverage: 75:187/454 of query aligns to 136:240/563 of Q4U2R8

query
sites
Q4U2R8

L

L

T

A

L

Q

S

S

I

L

T

Y

F

M

V

V

S

G

R

V

P

L

I

L

G

G

A

A

I

M

V

V

F

F

G

G

H

Y

Y

L

G

A

D

D

K

R

I

L

G

G

R

R

K

R

K

K

S

V

L

L

V

I

L

L

S

N

L

Y

M

L

I

Q

M

T

G

A

I

V

S

S

T

G

F

T

F

C

I

A

G

A

L

F

I

A

P

P

S

N

Y

F

N

-

T

-

I

-

G

-

N

-

A

-

P

P

L

I

I

Y

L

C

I

A

F

F

L

-

R

R

L

L

C

L

Q

S

G

G

F

M

A

A

I

L

G

A

G

G

E

I

W

S

G

L

G

N

A

C

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M

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E

E

Y

W

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H

H

R

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R

R

G

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F

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G

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x
Y

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L

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A

L

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A

G

G

V

V

Y230 (≠ N177) mutation to A: Loss of membrane protein expression and little uptake of cidofovir.

Sites not aligning to the query:

7 L → P: in dbSNP:rs1415632329
30 L→A: Complete loss of PAH transport activity.
36 T→A: Complete loss of PAH transport activity.
39 modified: carbohydrate, N-linked (GlcNAc...) asparagine; N→Q: Complete loss of PAH transport activity.
50 R → H: lower Vmax; increase in substrate affinity and increase in the affinity for the nucleoside phosphonate analogs cidofovir, adefovir and tenofovir; dbSNP:rs11568626
56 modified: carbohydrate, N-linked (GlcNAc...) asparagine
92 modified: carbohydrate, N-linked (GlcNAc...) asparagine
97 modified: carbohydrate, N-linked (GlcNAc...) asparagine
104 P → L: in dbSNP:rs11568627
113 modified: carbohydrate, N-linked (GlcNAc...) asparagine
431 K→A: Decrease in the level of membrane protein expression and 70 % loss of PAH uptake.
438 F→A: Decrease in the level of membrane protein expression, 70 % loss of PAH uptake, increased affinity for cidofovir, lower Vmax for PAH, and lower Km and Vmax for cidofovir.

Q63089 Solute carrier family 22 member 1; Organic cation transporter 1; rOCT1 from Rattus norvegicus (Rat) (see 4 papers)
25% identity, 36% coverage: 86:247/454 of query aligns to 162:305/556 of Q63089

query
sites
Q63089

I

L

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C179 (≠ S103) mutation to A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; S-322; A-358; A-418; S-437; A-470 and A-474.
M212 (≠ F144) mutation to L: No change in TEA and MPP(+) uptake.
V213 (≠ A145) mutation to G: Decreased TEA uptake. No change in MPP(+) uptake.
S214 (≠ I146) mutation to G: Decreased TEA and MPP(+) uptake.
K215 (≠ G147) mutation to Q: Loss of TEA and MPP(+) uptake activity.; mutation to R: Loss of TEA and MPP(+) uptake activity.
G216 (= G148) mutation to A: Decreased TEA and MPP(+) uptake.
S217 (≠ E149) mutation to G: No change in TEA and MPP(+) uptake.
W218 (= W150) mutation to F: Decreased guanidine, histamine, serotonin and TEA uptake. No change in MPP(+) uptake. No change in TEA and MPP(+) affinity. Decreased TEA Vmax. No change in MPP(+) Vmax.; mutation to L: Decreased guanidine, histamine, serotonin, TEA and MPP(+) uptake. Decreased TEA affinity. No change in MPP(+) affinity. Decreased TEA and MPP(+) Vmax.; mutation to Y: Decreased guanidine, histamine, serotonin and TEA uptake. No change in MPP(+) uptake. Increased TEA and MPP(+) affinity. Decreased TEA and MPP(+) Vmax.
V219 (≠ G151) mutation to L: No change in TEA and MPP(+) uptake.
S220 (≠ G152) mutation to I: Decreased TEA and MPP(+) uptake.
G221 (≠ A153) mutation to A: Decreased TEA and MPP(+) uptake.
Y222 (≠ T154) mutation to F: No change in guanidine, histamine, serotonin, TEA and MPP(+) uptake. Increased TEA affinity. No change in MPP(+) affinity. Decreased TEA Vmax. No change in MPP(+) Vmax.; mutation to L: Decreased guanidine, serotonin, TEA and MPP(+) uptake. No change in histamine uptake. Increased TEA and MPP(+) affinity. Decreased TEA and MPP(+) Vmax.
T223 (= T155) mutation to I: Decreased TEA uptake. No change in MPP(+) uptake.
L224 (= L156) mutation to V: Decreased TEA and MPP(+) uptake.
I225 (= I157) mutation to G: No change in TEA and MPP(+) uptake.
T226 (= T158) mutation to A: Decreased TEA uptake. No change in MPP(+) uptake.
E227 (= E159) mutation to D: Loss of TEA and MPP(+) uptake activity.; mutation to Q: Loss of TEA and MPP(+) uptake activity.
F228 (≠ Y160) mutation to I: No change in TEA and MPP(+) uptake.
V229 (≠ A161) mutation to A: Decreased TEA and MPP(+) uptake.; mutation to L: Loss of TEA and MPP(+) uptake activity.
S286 (≠ T228) mutation to A: No effect of PKC-induced stimulation on ASP uptake. No effect of PKC-induced stimulation on ASP uptake; when associated with A-292; A-296; A-328 and A-550. No effect of PKA activation on ASP uptake. No effect of PKA activation on ASP uptake; when associated with A-292; A-296; A-328 and A-550. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition; when associated with A-292; A-296; A-328 and A-550. No significant effect on trafficking from intracellular pools to the cell membrane; when associated with A-292; A-296; A-328 and A-550. suppresses phosphorylation by PKC; when associated with A-292; A-296; A-328 and A-550.
S292 (≠ N234) mutation to A: No effect of PKC-induced stimulation on ASP uptake. No effect of PKC-induced stimulation on ASP uptake; when associated with A-286; A-296; A-328 and A-550. No effect of PKA activation on ASP uptake. No effect of PKA activation on ASP uptake; when associated with A-286; A-296; A-328 and A-550. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition; when associated with A-286; A-296; A-328 and A-550. No significant effect on trafficking from intracellular pools to the cell membrane; when associated with A-286; A-296; A-328 and A-550. suppresses phosphorylation by PKC; when associated with A-286; A-296; A-328 and A-550.
T296 (≠ Q238) mutation to A: No effect of PKC-induced stimulation on ASP uptake. No effect of PKC-induced stimulation on ASP uptake; when associated with A-286; A-292; A-328; A-550. Significant increase of the ASP uptake by PKA activation. No effect of PKA activation on ASP uptake; when associated with A-286; A-292; A-328; A-550. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition; when associated with A-286; A-292; A-328; A-550. No significant effect on trafficking from intracellular pools to the cell membrane; when associated with A-286; A-292; A-328 and A-550. suppresses phosphorylation by PKC; when associated with A-286; A-292; A-328 and A-550.

Sites not aligning to the query:

26 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-155; A-179; S-322; A-358; A-418; S-437; A-470 and A-474.
155 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-179; S-322; A-358; A-418; S-437; A-470 and A-474.
322 C→S: Reduces the activation by MMTS. Abolishes the activation by MMTs; when associated with M-451. Choline affinity is increased fivefold by MMTS. Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; A-358; A-418; S-437; A-470 and A-474. Choline affinity is increased four- to fivefold; when associated with M-451.
328 S→A: No effect of PKC-induced stimulation on ASP uptake. No effect of PKC-induced stimulation on ASP uptake; when associated with A-286; A-292; A-296 and A-550. No effect of PKA activation on ASP uptake. No effect of PKA activation on ASP uptake; when associated with A-286; A-292; A-296 and A-550. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition; when associated with A-286; A-292; A-296; A-550. No significant effect on trafficking from intracellular pools to the cell membrane; when associated with A-286; A-292; A-296 and A-550. suppresses phosphorylation by PKC; when associated with A-286; A-292; A-296 and A-550.
358 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; S-322; A-418; S-437; A-470 and A-474.
418 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; S-322; A-358; S-437; A-470 and A-474.
437 C→S: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; S-322; A-358; A-418; A-470 and A-474.
451 C→M: Reduces the activation by MMTS. Abolishes the activation by MMTs; when associated with S-322. Abolishes the effect of MMTs on choline-induced currents. Choline affinity is not influenced by MMTS. Choline affinity is increased four- to fivefold; when associated with S-322.
470 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; S-322; A-358; A-418; A-437 and A-474.
474 C→A: Choline affinity is increased fourfold by MMTS; when associated with A-26; A-155; A-179; S-322; A-358; A-418; A-437 and A-470.
475 D→E: Decreased MPP(+) uptake, no change in MPP(+) affinity. Decreased NMN uptake, increased NMN affinity. Decreased choline uptake, increased choline affinity.; D→N: Decreased MPP(+) uptake.; D→R: Decreased MPP(+) uptake.
550 T→A: No effect of PKC-induced stimulation on ASP uptake. No effect of PKC-induced stimulation on ASP uptake; when associated with A-286; A-292; A-296; A-328. Significant increase of the ASP uptake by PKA activation. No effect of PKA activation on ASP uptake; when associated with A-286; A-292; A-296 and A-328. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition. Significant reduction of ASP uptake by p56(lck) tyrosine kinase-induced inhibition; when associated with A-286; A-292; A-296; A-328. No significant effect on trafficking from intracellular pools to the cell membrane; when associated with A-286; A-292; A-296 and A-328. suppresses phosphorylation by PKC; when associated with A-286; A-292; A-296 and A-328.

O15245 Solute carrier family 22 member 1; Organic cation transporter 1; hOCT1 from Homo sapiens (Human) (see 10 papers)
24% identity, 71% coverage: 87:408/454 of query aligns to 162:483/554 of O15245

query
sites
O15245

G

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S189 (= S114) to L: no changes in MPP(+) uptake; dbSNP:rs34104736
G220 (≠ A153) to V: affects transporter activity; reduction of MPP(+) uptake when associated with V-408; dbSNP:rs36103319
Y240 (≠ V173) mutation to F: Decreased TEA uptake.
P283 (= P207) to L: in dbSNP:rs4646277; mutation to A: Decreased TEA uptake.
R287 (vs. gap) to G: in dbSNP:rs4646278
P341 (≠ K256) to L: affects transporter activity; reduction of TEA uptake; reduction o MPP(+) uptake when associated with V-408; largely localized to the plasma membrane; dbSNP:rs2282143
R342 (≠ H257) to H: no changes in MPP(+) uptake when associated with V-408; dbSNP:rs34205214
Y361 (≠ M284) mutation to F: Decreased TEA uptake.
Y376 (≠ L299) mutation to F: Decreased TEA uptake.
G401 (= G324) to S: affects transporter activity; reduction of MPP(+), serotonin and TEA uptake; no MPP(+) uptake when associated with L-160; dbSNP:rs34130495
M408 (vs. gap) to V: does not affect transporter activity; no changes in MPP(+) uptake when associated with F-14; no changes in MPP(+) uptake when associated with F-85; no changes in MPP(+) uptake when associated with L-189; no changes in MPP(+) uptake when associated with H-342; no changes in MPP(+) uptake when associated with M-420 del; no changes in MPP(+) uptake when associated with I-440; no changes in MPP(+) uptake when associated with I-461; no changes in MPP(+) uptake when associated with M-488; reduction of MPP uptake when associated with C-61; no MPP(+) uptake when associated with V-220; reduction of MPP(+) uptake when associated with L-341; no MPP(+) uptake when associated with S-401; no MPP(+) uptake when associated with R-465; dbSNP:rs628031
M420 (≠ L337) natural variant: Missing (reduction of serum O-isobutanoyl-(R)-carnitine levels; no change in MPP(+) uptake; no changes in MPP(+) uptake when associated with V-408; dbSNP:rs72552763)
M440 (≠ F361) to I: in dbSNP:rs35956182
V461 (= V386) to I: no changes in MPP(+) uptake when associated with V-408; dbSNP:rs34295611
G465 (= G390) to R: reduction of the localization to the basolateral membrane; no MPP(+) uptake when associated with V-408; dbSNP:rs34059508; mutation to A: No changes in MPP(+) uptake.

Sites not aligning to the query:

14 S → F: exclusively found in the African American population; increased MPP(+) uptake when associated with V-408; dbSNP:rs34447885
24 I→L: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake.
28 L→I: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake.
31 A→S: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake.
32 F→L: No change in fenoterol uptake. Decreased trospium uptake. Decreased trospium affinity.
36 C→Y: Increased fenoterol uptake. Increased fenoterol affinity. No change in trospium uptake. No change in terbutaline uptake. No change in terbutaline affinity.
41 F → L: in dbSNP:rs2297373
61 R → C: affects transporter activity; reduction of MPP(+) uptake; reduction of serum O-isobutanoyl-(R)-carnitine levels; reduction of MPP(+) uptake when associated with V-408; dbSNP:rs12208357
85 L → F: no changes in MPP(+) uptake; when associated with V-408; dbSNP:rs35546288
88 C → R: affects transporter activity; reduction of MPP(+), serotonin and TEA uptake; dbSNP:rs55918055
160 L → F: no changes in both MPP(+) and TEA uptake; abolishes MPP(+) uptake when associated with S-401; largely localized to the plasma membrane; dbSNP:rs683369
488 R → M: no changes in MPP(+) uptake when associated with V-408; dbSNP:rs35270274

8sc2A Human oct1 bound to diltiazem in inward-open conformation (see paper)
24% identity, 71% coverage: 87:408/454 of query aligns to 144:422/453 of 8sc2A

query
sites
8sc2A

G

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L

S

P

I

T

A

F

L

L

L

F

F

L

V

L

G

Y

M

Y

F

W

I

C

R

V

S

P

R

E

I

S

E

P

E

R

T

S

P

P

V

S

F

F

Q

A

E

D

N

L

Q

F

K

R

Q

-

N

-

A

T

P

P

K

R

A

L

A

R

E

K

Q

R

K

T

F

F

P

-

I

I

L

L

T

M

V

Y

L

L

K
x
W

H

F

H

T

R

D

K
x
S

A

V

V

L

F

Y

L

Q

A

G

M

L

G

I

M

L

R

H

M

M

G

G

E

A

I

T

V

S

L

-

G

G

W

N

L

L

T

Y

V

L

A

D

F

F

F

L

M

Y

S

S

Y

A

V

L

T

V

R

E

E

-

L

-

N

-

F

-

T

-

R

-

E

-

T

-

A

-

L

-

N

-

G

-

L

-

L

I

L

P

A

G

S

A

F

F

V

I

G

A

I

L

F

I

T

T

F

I

P

-

F

-

G

-

W

-

L

-

S

-

D

D

K

R

I

V

G

G

R

R

R

-

P

-

V

I

Y

Y

-

P

-

M

-

A

-

M

-

S

-

N

-

L

L

L

A

A

G

G

A

A

-

C

I

L

T

V

L

M

I

I

F

F

A

I

F

S

P

P

-

D

L

L

F

H

W

W

M

L

I

-

D

-

S

-

G

-

S

-

V

N

K

I

M

I

F

I

M

M

F

C

A

V

T

G

T

R

F

M

C

G

Y

I

S

T

V

I

G

A

L
x
I

G

Q

M

M

M

I

F

C

S

L

V

V

Q

N

P

-

A

-

F

-

S

A

E

E

L

L

F

Y

D

P

T

T

S

F

V

V

R

R

Y

N

T

L

G

G

V

V

S

M

L

V

G

C

F

S

Q

S

L

L

A

C

N

D

I

I

V

G

G

G

G

I

L

I

T

T

P

P

M

F

I

I

binding Diltiazem: W199 (= W150), Q223 (= Q174), F226 (≠ N177), W293 (≠ K256), S297 (≠ K260), I385 (≠ L367)

Sites not aligning to the query:

binding Diltiazem: 18

5c65A Structure of the human glucose transporter glut3 / slc2a3
29% identity, 41% coverage: 63:247/454 of query aligns to 47:224/457 of 5c65A

query
sites
5c65A

N

N

L

A

S

P

P

P

L

S

M

E

A

V

L

L

V

T

S

S

F
x
L

L

W

T

S

L

L

S

S

I

V

T

A

F

I

-

F

-

S

V

V

S

G

R

G

P

M

I

I

G

G

A

S

I
x
F

V
x
S

F

V

G

G

H
x
L

Y

F

G

V

D

N

K

R

I

F

G

G

R

R

K
x
R

K

N

S

S

L

M

V

L

L

I

S

V

L

N

M
x
L

I
x
L

M

A

G

V

I

T

S

G

T

G

F

C

F

F

I

M

G

G

L

L

I

C

P

K

S

V

Y

A

N

K

T

S

I

V

G

E

N

-

A

-

P

-

L

-

I

M

L

L

I

I

F

L

L

G

R

R

L
|
L

C

V

Q

I

G

G

F

L

A

F

I

C

G

G

G

L

E

C

W

T

G

G

G

F

A

V

T

P

T

M

L

Y

I

I

T

G

E

E

Y

I

A

S

P

P

R

T

H

A

R

L

R

R

G

G

F

A

F

F

G

G

T

T

F

L

V

N

Q

Q

L

L

G

G

N

I

V

V

L

V

G

G

L

I

F

L

I

V

A

A

T

Q

G

-

V

I

F

F

A

G

L

L

V

E

V

F

M

I

L

L

P

G

E

S

E

E

D

E

L

L

M

-

S

-

W

W

G

-

W

-

R

-

V

-

P

P

F

L

L

L

S

G

I

F

A

T

L

I

L

L

F

-

V

-

G

P

M

A

F

I

I

L

R

Q

S

S

R

A

-

A

-

L

-
x
P

-

F

I

C

E

P

E

E

T

S

P

P

V

R

F

F

Q

L

E

L

-

I

N

N

Q

R

K

K

Q

E

N

N

A

A

P

K

K

Q

A

I

A

L

E

Q

Q

R

binding Octyl Glucose Neopentyl Glycol : L58 (≠ F74), F75 (≠ I89), S76 (≠ V90), L79 (≠ H93), R87 (≠ K101), L95 (≠ M109), L96 (≠ I110), L121 (= L140), P199 (vs. gap)

Sites not aligning to the query:

4zw9A Crystal structure of human glut3 bound to d-glucose in the outward- occluded conformation at 1.5 angstrom (see paper)
29% identity, 41% coverage: 63:247/454 of query aligns to 51:228/470 of 4zw9A

query
sites
4zw9A

N

N

L

A

S

P

P

P

L

S

M

E

A

V

L

L

V

T

S

S

F

L

L

W

T

S

L

L

S

S

I

V

T

A

F

I

-

F

-

S

V

V

S

G

R

G

P

M

I

I

G

G

A

S

I

F

V

S

F

V

G

G

H

L

Y

F

G

V

D

N

K

R

I

F

G

G

R

R

K

R

K

N

S

S

L

M

V

L

L

I

S

V

L

N

M

L

I

L

M

A

G

V

I

T

S

G

T

G

F

C

F

F

I

M

G

G

L

L

I

C

P

K

S

V

Y

A

N

K

T

S

I

V

G

E

N

-

A

-

P

-

L

-

I

M

L

L

I

I

F

L

L

G

R

R

L

L

C

V

Q

I

G

G

F

L

A

F

I

C

G

G

G

L

E

C

W

T

G

G

G

F

A

V

T

P

T

M

L

Y

I

I

T

G

E

E

Y

I

A

S

P

P

R

T

H

A

R

L

R

R

G

G

F

A

F

F

G

G

T

T

F

L

V

N

Q
|
Q

L

L

G

G

N
x
I

V

V

L

V

G

G

L
x
I

F

L

I

V

A

A

T

Q

G

-

V

I

F

F

A

G

L

L

V

E

V

F

M

I

L

L

P

G

E

S

E

E

D

E

L

L

M

-

S

-

W

W

G

-

W

-

R

-

V

-

P

P

F

L

L

L

S

G

I

F

A

T

L

I

L

L

F

-

V

-

G

P

M

A

F

I

I

L

R

Q

S

S

R

A

-

A

-

L

-

P

-

F

I

C

E

P

E

E

T

S

P

P

V

R

F

F

Q

L

E

L

-

I

N

N

Q

R

K

K

Q

E

N

N

A

A

P

K

K

Q

A

I

A

L

E

Q

Q

R

binding beta-D-glucopyranose: Q159 (= Q174), I166 (≠ L181)
binding alpha-D-glucopyranose: Q159 (= Q174), I162 (≠ N177), I166 (≠ L181)

Sites not aligning to the query:

binding beta-D-glucopyranose: 280, 281, 286, 377, 386
binding alpha-D-glucopyranose: 280, 281, 286, 386

7spsA Crystal structure of human glucose transporter glut3 bound with exofacial inhibitor sa47 (see paper)
29% identity, 41% coverage: 63:247/454 of query aligns to 48:225/468 of 7spsA

query
sites
7spsA

N

N

L

A

S

P

P

P

L

S

M

E

A

V

L

L

V

T

S

S

F

L

L

W

T

S

L

L

S

S

I

V

T

A

F

I

-

F

-

S

V

V

S

G

R

G

P

M

I

I

G

G

A

S

I

F

V

S

F

V

G

G

H

L

Y

F

G

V

D

N

K

R

I

F

G

G

R

R

K

R

K

N

S

S

L

M

V

L

L

I

S

V

L

N

M

L

I

L

M

A

G

V

I

T

S

G

T

G

F

C

F

F

I

M

G

G

L

L

I

C

P

K

S

V

Y

A

N

K

T

S

I

V

G

E

N

-

A

-

P

-

L

-

I

M

L

L

I

I

F

L

L

G

R

R

L

L

C

V

Q

I

G

G

F

L

A

F

I

C

G

G

G

L

E

C

W

T

G

G

G

F

A

V

T

P

T

M

L

Y

I

I

T

G

E

E

Y

I

A

S

P

P

R

T

H

A

R

L

R

R

G

G

F

A

F

F

G

G

T

T

F

L

V

N

Q
|
Q

L

L

G

G

N

I

V

V

L

V

G

G

L
x
I

F

L

I

V

A

A

T

Q

G

-

V

I

F

F

A

G

L

L

V

E

V

F

M

I

L

L

P

G

E

S

E

E

D

E

L

L

M

-

S

-

W

W

G

-

W

-

R

-

V

-

P

P

F

L

L

L

S

G

I

F

A

T

L

I

L

L

F

-

V

-

G

P

M

A

F

I

I

L

R

Q

S

S

R

A

-

A

-

L

-

P

-

F

I

C

E

P

E

E

T

S

P

P

V

R

F

F

Q

L

E

L

-

I

N

N

Q

R

K

K

Q

E

N

N

A

A

P

K

K

Q

A

I

A

L

E

Q

Q

R

binding methyl N-[(2-{4-[4-(5-fluoro-2-methoxyphenyl)piperazin-1-yl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}phenyl)methyl]-beta-alaninate: Q156 (= Q174), I163 (≠ L181)

Sites not aligning to the query:

binding methyl N-[(2-{4-[4-(5-fluoro-2-methoxyphenyl)piperazin-1-yl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}phenyl)methyl]-beta-alaninate: 21, 25, 29, 278, 286, 308, 312, 374, 375, 406, 407, 410

7crzA Crystal structure of human glucose transporter glut3 bound with c3361 (see paper)
29% identity, 41% coverage: 63:247/454 of query aligns to 49:226/469 of 7crzA

query
sites
7crzA

N

N

L

A

S

P

P

P

L

S

M

E

A

V

L

L

V

T

S

S

F

L

L

W

T

S

L

L

S

S

I

V

T
x
A

F

I

-

F

-
x
S

V

V

S

G

R

G

P

M

I

I

G

G

A

S

I

F

V

S

F

V

G

G

H

L

Y

F

G

V

D

N

K

R

I

F

G

G

R

R

K

R

K

N

S

S

L

M

V

L

L

I

S

V

L

N

M

L

I

L

M

A

G

V

I

T

S

G

T

G

F

C

F

F

I

M

G

G

L

L

I

C

P

K

S

V

Y

A

N

K

T

S

I

V

G

E

N

-

A

-

P

-

L

-

I

M

L

L

I

I

F

L

L

G

R

R

L

L

C

V

Q

I

G

G

F

L

A

F

I

C

G

G

G

L

E

C

W

T

G

G

G

F

A

V

T

P

T

M

L

Y

I

I

T

G

E

E

Y

I

A

S

P

P

R

T

H

A

R

L

R

R

G

G

F

A

F

F

G

G

T

T

F

L

V

N

Q
|
Q

L

L

G

G

N

I

V

V

L

V

G

G

L
x
I

F

L

I

V

A

A

T

Q

G

-

V

I

F

F

A

G

L

L

V

E

V

F

M

I

L

L

P

G

E

S

E

E

D

E

L

L

M

-

S

-

W

W

G

-

W

-

R

-

V

-

P

P

F

L

L

L

S

G

I

F

A

T

L

I

L

L

F

-

V

-

G

P

M

A

F

I

I

L

R

Q

S

S

R

A

-

A

-

L

-

P

-

F

I

C

E

P

E

E

T

S

P

P

V

R

F

F

Q

L

E

L

-

I

N

N

Q

R

K

K

Q

E

N

N

A

A

P

K

K

Q

A

I

A

L

E

Q

Q

R

binding (2S,3R,4S,5R,6R)-6-(hydroxymethyl)-4-undec-10-enoxy-oxane-2,3,5-triol: A66 (≠ T80), S69 (vs. gap), Q157 (= Q174), I164 (≠ L181)

Sites not aligning to the query:

binding (2S,3R,4S,5R,6R)-6-(hydroxymethyl)-4-undec-10-enoxy-oxane-2,3,5-triol: 26, 278, 279, 284, 313, 375, 384, 411, 412, 415

P11169 Solute carrier family 2, facilitated glucose transporter member 3; Glucose transporter type 3, brain; GLUT-3 from Homo sapiens (Human) (see paper)
29% identity, 41% coverage: 63:247/454 of query aligns to 51:228/496 of P11169

query
sites
P11169

N

N

L

A

S

P

P

P

L

S

M

E

A

V

L

L

V

T

S

S

F

L

L

W

T

S

L

L

S

S

I

V

T

A

F

I

-

F

-

S

V

V

S

G

R

G

P

M

I

I

G

G

A

S

I

F

V

S

F

V

G

G

H

L

Y

F

G

V

D

N

K

R

I

F

G

G

R

R

K

R

K

N

S

S

L

M

V

L

L

I

S

V

L

N

M

L

I

L

M

A

G

V

I

T

S

G

T

G

F

C

F

F

I

M

G

G

L

L

I

C

P

K

S

V

Y

A

N

K

T

S

I

V

G

E

N

-

A

-

P

-

L

-

I

M

L

L

I

I

F

L

L

G

R

R

L

L

C

V

Q

I

G

G

F

L

A

F

I

C

G

G

G

L

E

C

W

T

G

G

G

F

A

V

T

P

T

M

L

Y

I

I

T

G

E

E

Y

I

A

S

P

P

R

T

H

A

R

L

R

R

G

G

F

A

F

F

G

G

T

T

F

L

V

N

Q
|
Q

L

L

G

G

N

I

V

V

L

V

G

G

L

I

F

L

I

V

A

A

T

Q

G

-

V

I

F

F

A

G

L

L

V

E

V

F

M

I

L

L

P

G

E

S

E

E

D

E

L

L

M

-

S

-

W

W

G

-

W

-

R

-

V

-

P

P

F

L

L

L

S

G

I

F

A

T

L

I

L

L

F

-

V

-

G

P

M

A

F

I

I

L

R

Q

S

S

R

A

-

A

-

L

-

P

-

F

I

C

E

P

E

E

T

S

P

P

V

R

F

F

Q

L

E

L

-

I

N

N

Q

R

K

K

Q

E

N

N

A

A

P

K

K

Q

A

I

A

L

E

Q

Q

R

Q159 (= Q174) binding

Sites not aligning to the query:

277:279 Important for selectivity against fructose; QLS→HVA: Confers moderate fructose transport activity.
280:281 binding
286 binding
315 binding
378 binding
386 binding

Query Sequence

>BWI76_RS03450 FitnessBrowser__Koxy:BWI76_RS03450
MTMLTSPAMTPAKNEQTSQQTHERRKLLTVLGSGLSGTTIEFYDFFIYGTAAALVFPSLF
FPNLSPLMALLVSFLTLSITFVSRPIGAIVFGHYGDKIGRKKSLVLSLMIMGISTFFIGL
IPSYNTIGNAAPLILIFLRLCQGFAIGGEWGGATTLITEYAPRHRRGFFGTFVQLGNVLG
LFIATGVFALVVMLPEEDLMSWGWRVPFLLSIALLFVGMFIRSRIEETPVFQENQKQQQN
APKAAEQKFPILTVLKHHRKAVFLAMGMRMGEIVLGWLTVAFFMSYVTRELNFTRETALN
GLLLASFVGIFTFPFFGWLSDKIGRRPVYLAGAAITLIFAFPLFWMIDSGSVKMFMFATT
FCYSVGLGMMFSVQPAFFSELFDTSVRYTGVSLGFQLANIVGGLTPMIGTLLLVWSGGAS
WPISLFLACMALITILCVCVTRESYNDELNEVKK

Or try a new SitesBLAST search

SitesBLAST's Database

SitesBLAST's database includes (1) SwissProt entries with experimentally-supported functional features; and (2) protein structures with bound ligands, from the BioLip database.

by Morgan Price, Arkin group
Lawrence Berkeley National Laboratory