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Table 3 Comparison of functionally important motifs/residues conserved in GPR17 and related receptors

From: GPR17: Molecular modeling and dynamics studies of the 3-D structure and purinergic ligand binding features in comparison with P2Y receptors

GPR17

GPCR (type/family)

SHARED FEATURES (1)

(residue number and structural domain)

  

N49-D77-G290

TM1-TM2-TM7

b Rh

1.50–2.50–7.46

Y38-S287

TM1-TM7

P2Y

1.39–7.43

N114-D293

TM3-TM7

P2Y

3.35–7.49

H72-TRP156

TM2-TM4

b Rh

2.45–4.50

D128-R129

conserved

interaction TM3-TM6

not conserved (3.50–6.30)

b Rh R of the DRY motif interacts with acidic residue in 6.30 (maintains the ground state) GPR17, P2Y, CysLT receptors have a basic residue in 6.30

D/E-R-Y/W motif

3.49–3.50–3.51

A233-M236

b Rh

Hydrophobic pocket accommodating DRY motif

2.33–2.36

H252-X-X-R255

TM6

P2Y, CysLT receptors in P2Y agonists mediate receptor activation/coordination of the phosphate moiety

H-X-X-R motif

6.52-X-X-6.55

N77-N289-D293

D2.50-N7.45-D7.49

TM2-TM7

b Rh

D2.50-N7.45-D7.49 TM7 residues belong to N/D-P-X-X-Y motif

G10-L17

V173-L182

b Rh

Plug β-hairpin in Nt and EL2

S118-water

b Rh

3.39-water

C104-C181

All GPCR

disulphide bridge TM3-EL2

C23-C269

P2Y, CysLT receptors

disulphide bridge Nt-EL3

  1. (1)See Ballestero and Weinstein's numbering system for residue index [36].