4YAY,4ZUD


Conserved Protein Domain Family
7tmA_AT1R

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cd15192: 7tmA_AT1R 
Click on image for an interactive view with Cn3D
type 1 angiotensin II receptor, member of the class A family of seven-transmembrane G protein-coupled receptors
Angiotensin II (Ang II), the main effector in the renin-angiotensin system, plays a crucial role in the regulation of cardiovascular homeostasis through its type 1 (AT1) and type 2 (AT2) receptors. Ang II contributes to cardiovascular diseases such as hypertension and atherosclerosis via AT1R activation. Ang II increases blood pressure through Gq-mediated activation of phospholipase C, resulting in phosphoinositide (PI) hydrolysis and increased intracellular calcium levels. Through the AT2R, Ang II counteracts the vasoconstrictor action of AT1R and thereby induces vasodilation, sodium excretion, and reduction of blood pressure. Moreover, AT1R promotes cell proliferation, whereas AT2R inhibits proliferation and stimulates cell differentiation. The AT2R is highly expressed during fetal development, however it is scarcely present in adult tissues and is induced in pathological conditions. Generally, the AT1R mediates many actions of Ang II, while the AT2R is involved in the regulation of blood pressure and renal function.
Statistics
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PSSM-Id: 320320
View PSSM: cd15192
Aligned: 9 rows
Threshold Bit Score: 445.723
Threshold Setting Gi: 40241258
Created: 11-Dec-2008
Updated: 26-Jul-2017
Structure
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Program:
Drawing:
Aligned Rows:
  next features
Conserved site includes 17 residues -Click on image for an interactive view with Cn3D
Feature 1:putative peptide ligand binding pocket [polypeptide binding site]
Evidence:
  • Comment:based on the structures of some angiotensin receptor family (class A) members with bound ligands (agonist peptides or chemical compound agonists/antagonists)
  • Comment:Small-molecule chemical ligands tend to bind deeper within the receptor core, compared to a peptide ligands, which binds towards the extracelllular surface of its receptor.
  • Structure:4YAY: Human Type 1 Angiotensin Receptor binds selective antagonist ZD7155; contacts at 4A
    View structure with Cn3D
  • Structure:4ZUD: Human angiotensin II type1 receptor (AT1R) binds an inverse agonist (Olmesartan), an highly potent anti-hypertensive drug; contacts at 4A
    View structure with Cn3D

Sequence Alignment
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Format: Row Display: Color Bits: Type Selection:
                         10        20        30        40        50        60        70        80
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1              #                                         #      #  ##   #            #  #
4YAY_A       124 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 203
4ZUD_A       124 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 203
gi 40241258   32 LMIPVVYSIIFVIGVLGNSMVIIVIYYYLKLKtvANIFLLNLALADLTFVITLPLWAASTameYHWPFGvfLCKMSATVL 111
gi 47223409   18 ILVPMVYGSIFVIGIVGNSMVVAVIYCYMKLKtvANIFVLNLAVSDLTFLITLPMWATSTakgYHWPFGefLCKASAGLV 97
gi 3023269    29 IMVPTVYSIIFIIGIFGNSLVVIVIYCYMKLKtvASIFLLNLALADLCFLITLPLWAAYTameYQWPFGncLCKLASAGI 108
gi 231519     29 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 108
gi 557014839  28 TMIPTIYGIIFVTGILGNSIVVAVIFCYMKLKtvANIFLFNLALADMIFLITLPLWAAYTamgYHWPFGncLCKISTALV 107
gi 632968653  23 LLIPITYSVIFVVGVIGNGLVVIVIYCYLKVItvANIFLLNLALADLIFIITLPVWAAYTamgYHWPFGgfLCKMCSTFV 102
gi 543781     31 ITIPIIYSTIFVVGVFGNSLVVIVIYSYMKMKtmASVFLMNLALSDLCFVITLPLWAVYTamhYHWPFGdlLCKIASTAI 110
                         90       100       110       120       130       140       150       160
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1        #  #                                                  #   #              #      
4YAY_A       204 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 282
4ZUD_A       204 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 282
gi 40241258  112 LLNMNASIFLVTCLSVDRYLAIVHPikSRTKRtlVHAWMACIMVWILAGLASLPAMFFRdavhysdwNKTICAFhypkq- 190
gi 47223409   98 IFNLYTSVFFLMALSIDRYLAIVHPvqSRRFRtvVYARVTCVVIWLFAFVLSLPTALTRdvhnisnvNMTVCGIlhnnie 177
gi 3023269   109 SFNLYASVFLLTCLSIDRYLAIVHPvkSRIRRtmFVARVTCIVIWLLAGVASLPVIIHRniffaenlNMTVCGFrydnn- 187
gi 231519    109 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 187
gi 557014839 108 SYNLYATMFLLTCLSIDRYLAIVHPmkSRPRRtlIFARITCILAWLLAGVASIPVLIFRqviflknqNITVCSFfyke-- 185
gi 632968653 103 LINMNASIFLVTCLSIDRYLAIVHPmrSRSKRtlIQARVVCTVVWLLAAVTSLPNTFLRdtvsyeswNKTICAFqyper- 181
gi 543781    111 TLNLYTTVFLLTCLSIDRYSAIVHPmkSRIRRtvMVARLTCVGIWLVAFLASLPSVIYRqififpdtNQTVCALvyhsg- 189
                        170       180       190       200       210       220       230       240
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1                                                                           #  #         
4YAY_A       283 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 360
4ZUD_A       283 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 360
gi 40241258  191 nrnqwVFGLALLKNLLGFLIPLLIILICYSLILKSLvqayq-ierskPVGNEAFKLIKAVVVSFILCWLPFQIFAFMDVL 269
gi 47223409  178 slkelLLAISLMKSLLGFLIPFIVIITCYCLIGRALlsartiqkssrSRDDEVLRMLAAAVLAFFLCWAPHQVFHLMQFF 257
gi 3023269   188 -nttlRVGLGLSKNLLGFLIPFLIILTSYTLIWKTLkkayq-iqrnkTRNDDIFKMIVAIVFFFFFSWIPHQVFTFLDVL 265
gi 231519    188 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 265
gi 557014839 186 -qdphLVVMGLMKNILGFFIPFAIILTCYTLIGKTLmetyk-vqknkSRCDEVLKVIMTVVVVFFICWFPHQVFNFLEVL 263
gi 632968653 182 hkeqwIFGMALLKILLGFLIPSFIILTCYFLILRSLmqayh-itrskQTNNEAFKVILAVVIMFLFCWLPYQIITFFDVL 260
gi 543781    190 -hiyfMVGMSLVKNIVGFFIPFVIILTSYTLIGKTLkevy---raqrARNDDIFKMIVAVVLLFFFCWIPHQVFTFLDVL 265
                        250       260       270       280
                 ....*....|....*....|....*....|....*....|....*...
Feature 1                              #   #                     
4YAY_A       361 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 408
4ZUD_A       361 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 408
gi 40241258  270 SQlkiiksCHIPEVIDTSIPFTICVAYFNSCLNPILYGLVGrnFREKF 317
gi 47223409  258 TQlkdadnCPLLEIIDTAMPFTICIAYFNSCVNPIVYGFVGhnFRKNL 305
gi 3023269   266 IQlhvitdCKITDIVDTAMPFTICIAYFNNCLNPFFYVFFGknFKKYF 313
gi 231519    266 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 313
gi 557014839 264 VRlevitdCHIVNIVDTAMPFTICIAYFNSCLNPILYGFVGdnFRKKF 311
gi 632968653 261 FRlnviqnCYFSEMIDSSIPFTICLAYSNSCLNPILYGFVGhnFREKL 308
gi 543781    266 IQmdviqnCKMYDIVDTGMPITICIAYFNSCLNPFLYGFFGkkFRKHF 313

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