4PHU


Conserved Protein Domain Family
7tmA_FFAR1

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cd15169: 7tmA_FFAR1 
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free fatty acid receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors
This subgroup includes the mammalian free fatty acid receptor 1 (FFAR1), also called GPR40. FFAR1 is a cell-surface receptor for medium- and long-chain free fatty acids (FFAs). The receptor is most potently activated by eicosatrienoic acid (C20:3), but can also be activated at micromolar concentrations of various fatty acids. FFAR1 directly mediates FFA stimulation of glucose-stimulated insulin secretion and indirectly increases insulin secretion by enhancing the release of incretin. Free fatty acid receptors (FFARs) belong to the class A G-protein coupled receptors and are comprised of three members, each encoded by a separate gene (FFAR1, FFAR2, and FFAR3). These genes and a fourth pseudogene, GPR42, are localized together on chromosome 19. FFARs are considered important components of the body's nutrient sensing mechanism, and therefore, these receptors are potential therapeutic targets for the treatment of metabolic disorders, such as type 2 diabetes and obesity.
Statistics
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PSSM-Id: 320297
Aligned: 3 rows
Threshold Bit Score: 473.727
Created: 15-Dec-2013
Updated: 25-Oct-2021
Structure
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Program:
Drawing:
Aligned Rows:
  next features
Conserved site includes 41 residues -Click on image for an interactive view with Cn3D
Feature 1:putative ligand binding pocket [chemical binding site]
Evidence:
  • Structure:4PHU: Human GPR40 (FFAR1) binds allosteric agonist TAK-875, contacts at 4A.
  • Comment:based on the structures of some class A family members with bound ligands (peptides or chemicals), agonists, or antagonists
  • Comment:Small-molecule chemical ligands tend to bind deeper within the receptor core, compared to a peptide ligand neurotensin, which binds towards the extracellular surface of its receptor.

Sequence Alignment
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Format: Row Display: Color Bits: Type Selection:
Feature 1                                                             #  ##            ###### 
4PHU_A     19 QLSFGLYVAAFALGFPLNVLAIRGATAHARlrLTPSAVYALNLGCSDLLLTVSLPLKAVEALasgAWPLPasLCPVFAVA 98 
O14842      6 QLSFGLYVAAFALGFPLNVLAIRGATAHARlrLTPSLVYALNLGCSDLLLTVSLPLKAVEALasgAWPLPasLCPVFAVA 85  human
Q76JU8      6 QLFFALYVSAFALGFPLNLLAIRGAVARARlrLTPNLVYTLHLACSDLLLAITLPVKAVEALasgAWPLPlpLCPVFVLV 85  golden hamster
Feature 1     ##  #                                            # #####                        
4PHU_A     99 HFAPLYAGGGFLAALSAARYLGAAFPLgYQAFRRPCYSWGVCAAIWALVLCHLGLVFGLEApggwldhsntslgintpvn 178
O14842     86 HFFPLYAGGGFLAALSAGRYLGAAFPLgYQAFRRPCYSWGVCAAIWALVLCHLGLVFGLEApggwldhsntslgintpvn 165 human
Q76JU8     86 HFAPLYAGGGFLAALSAGRYLGAAFPFgYQAVRRPRYSWGVCVAIWALVLCHMGLVLGLEApggwlnttssslgintpvn 165 golden hamster
Feature 1                  #  ### ### ##                                                      
4PHU_A    179 gSPVCLEAWDPasAGPARFSLSLLLFFLPLAITAFCFVGCLRALargsnifemlrideglrlkiykdtegyytigighll 258
O14842    166 gSPVCLEAWDPasAGPARFSLSLLLFFLPLAITAFCYVGCLRALar---------------------------------- 211 human
Q76JU8    166 gSPVCLEAWDPnsARPARLSFSILLFFVPLVITAFCYVGCLRALah---------------------------------- 211 golden hamster
Feature 1                                                                                     
4PHU_A    259 tkspslnaakseldkaigrntngvitkdeaeklfnqdvdaavrgilrnaklkpvydsldavrraalinmvfqmgetgvag 338
O14842        --------------------------------------------------------------------------------     human
Q76JU8        --------------------------------------------------------------------------------     golden hamster
Feature 1                                                                              #  ## #
4PHU_A    339 ftnslrmlqqkrwdeaavnlaksrwynqtpnrakrvittfrtgtwdaygsLTHRRKLRAAWVAGGALLTLLLCVGPYNAS 418
O14842    212 ------------------------------------------------sgLTHRRKLRAAWVAGGALLTLLLCVGPYNAS 243 human
Q76JU8    212 ------------------------------------------------sgLSHKRKLRAAWAAGGAFLTLLLCLGPYNAS 243 golden hamster
Feature 1     #  #      ## ###  #  ##                       
4PHU_A    419 NVASFLypnlGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVC 464
O14842    244 NVASFLypnlGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVC 289 human
Q76JU8    244 NVASFVnpdlGGSWRKLGLITGSWSVVLNPLVTGYLGASPGRGTVC 289 golden hamster

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