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Summary Structural details Experimental details Functional details Sequence Neighbor History Downloads

5TZR

GPR40 in complex with partial agonist MK-8666

Functional Information from GO Data

Chain	GOid	namespace	contents
A	0003796	molecular_function	lysozyme activity
A	0003824	molecular_function	catalytic activity
A	0004930	molecular_function	G protein-coupled receptor activity
A	0007186	biological_process	G protein-coupled receptor signaling pathway
A	0009253	biological_process	peptidoglycan catabolic process
A	0016020	cellular_component	membrane
A	0016787	molecular_function	hydrolase activity
A	0016798	molecular_function	hydrolase activity, acting on glycosyl bonds
A	0016998	biological_process	cell wall macromolecule catabolic process
A	0030430	cellular_component	host cell cytoplasm
A	0031640	biological_process	killing of cells of another organism
A	0042742	biological_process	defense response to bacterium
A	0044659	biological_process	viral release from host cell by cytolysis

Functional Information from PDB Data

site_id	AC1
Number of Residues	4
Details	binding site for residue NA A 2401

Chain	Residue
A	SER1036
A	PHE1114
A	SER1117
A	HOH2549

site_id	AC2
Number of Residues	13
Details	binding site for residue MK6 A 2402

Chain	Residue
A	GLY139
A	PHE142
A	LEU158
A	TRP174
A	ARG183
A	TYR2240
A	ARG2258
A	HOH2551
A	PRO80
A	ALA83
A	PHE87
A	TYR91
A	LEU138

site_id	AC3
Number of Residues	3
Details	binding site for residue MLI A 2403

Chain	Residue
A	GLU1011
A	GLY1030
A	GLN1105

site_id	AC4
Number of Residues	3
Details	binding site for residue OLC A 2404

Chain	Residue
A	LEU188
A	PHE2248
A	OLC2408

site_id	AC5
Number of Residues	7
Details	binding site for residue OLC A 2405

Chain	Residue
A	PHE9
A	PRO40
A	TYR44
A	ALA102
A	ALA103
A	LEU189
A	LEU190

site_id	AC6
Number of Residues	1
Details	binding site for residue OLC A 2407

Chain	Residue
A	OLC2408

site_id	AC7
Number of Residues	3
Details	binding site for residue OLC A 2408

Chain	Residue
A	THR31
A	OLC2404
A	OLC2407

site_id	AC8
Number of Residues	2
Details	binding site for residue OLC A 2409

Chain	Residue
A	TRP2224
A	GLY2227

site_id	AC9
Number of Residues	1
Details	binding site for residue OLC A 2410

Chain	Residue
A	GLN6

site_id	AD1
Number of Residues	4
Details	binding site for residue OLC A 2411

Chain	Residue
A	VAL64
A	PRO73
A	LEU78
A	LEU106

site_id	AD2
Number of Residues	1
Details	binding site for residue 1PE A 2412

Chain	Residue
A	TYR2250

site_id	AD3
Number of Residues	8
Details	binding site for residue 1PE A 2413

Chain	Residue
A	GLY1023
A	TYR1024
A	TYR1025
A	LYS1035
A	PRO1037
A	LYS1135
A	ARG1137
A	ASN1140

Functional Information from SwissProt/UniProt

site_id	SWS_FT_FI1
Number of Residues	63
Details	TOPO_DOM: Extracellular => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	MET1-SER8
A	GLU65-CYS79
A	GLY143-SER178
A	LEU2249-SER2256

site_id	SWS_FT_FI2
Number of Residues	22
Details	TRANSMEM: Helical; Name=1 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	PHE9-THR31

site_id	SWS_FT_FI3
Number of Residues	48
Details	TOPO_DOM: Cytoplasmic => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	ALA32-SER41
A	ALA102-CYS121
A	GLY2280-LYS2300

site_id	SWS_FT_FI4
Number of Residues	22
Details	TRANSMEM: Helical; Name=2 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	ALA42-VAL64

site_id	SWS_FT_FI5
Number of Residues	21
Details	TRANSMEM: Helical; Name=3 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	PRO80-SER101

site_id	SWS_FT_FI6
Number of Residues	20
Details	TRANSMEM: Helical; Name=4 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	TYR122-PHE142

site_id	SWS_FT_FI7
Number of Residues	21
Details	TRANSMEM: Helical; Name=5 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	ALA179-PHE200

site_id	SWS_FT_FI8
Number of Residues	24
Details	TRANSMEM: Helical; Name=6 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	TRP2224-PHE2248

site_id	SWS_FT_FI9
Number of Residues	22
Details	TRANSMEM: Helical; Name=7 => ECO:0000255, ECO:0000269\|PubMed:25043059

Chain	Residue	Details
A	TRP2257-LEU2279

site_id	SWS_FT_FI10
Number of Residues	2
Details	SITE: Important for receptor activation => ECO:0000269\|PubMed:19068482

Chain	Residue	Details
A	GLU145
A	GLU172

site_id	SWS_FT_FI11
Number of Residues	1
Details	CARBOHYD: N-linked (GlcNAc...) asparagine => ECO:0000255

Chain	Residue	Details
A	ASN155

site_id	SWS_FT_FI12
Number of Residues	1
Details	ACT_SITE: Proton donor/acceptor => ECO:0000255\|HAMAP-Rule:MF_04110, ECO:0000269\|PubMed:3382407, ECO:0000269\|PubMed:7831309, ECO:0000269\|PubMed:8266098

Chain	Residue	Details
A	GLU1011

site_id	SWS_FT_FI13
Number of Residues	1
Details	ACT_SITE: Proton donor/acceptor => ECO:0000255\|HAMAP-Rule:MF_04110, ECO:0000269\|PubMed:1892846, ECO:0000269\|PubMed:3382407, ECO:0000269\|PubMed:7831309, ECO:0000269\|PubMed:8266098

Chain	Residue	Details
A	ASP1020

site_id	SWS_FT_FI14
Number of Residues	2
Details	BINDING: BINDING => ECO:0000269\|PubMed:8266098

Chain	Residue	Details
A	LEU1032
A	PHE1104

site_id	SWS_FT_FI15
Number of Residues	2
Details	BINDING: BINDING => ECO:0000303\|PubMed:7831309

Chain	Residue	Details
A	SER1117
A	ASN1132

Catalytic Information from CSA

site_id	MCSA1
Number of Residues	2
Details	M-CSA 921

Chain	Residue	Details
A	GLU1011	proton shuttle (general acid/base)
A	ASP1020	covalent catalysis

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PDB entries from 2025-06-11

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