3RZE


Conserved Protein Domain Family
7tmA_Histamine_H1R
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cd15050: 7tmA_Histamine_H1R 
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histamine subtype H1 receptor, member of the class A family of seven-transmembrane G protein-coupled receptors
This group includes histamine receptor subtype H1R, a member of histamine receptor family, which belongs to the class A of GPCRs. Histamine plays a key role as chemical mediator and neurotransmitter in various physiological and pathophysiological processes in the central and peripheral nervous system. Histamine exerts its functions by binding to four different G protein-coupled receptors (H1-H4). H1R selectively interacts with the G(q)-type G protein that activates phospholipase C and the phosphatidylinositol pathway. Antihistamines, a widely used anti-allergy medication, act on the H1 subtype and produce drowsiness as a side effect. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes.
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Statistics
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PSSM-Id: 320178
Aligned: 7 rows
Threshold Bit Score: 328.619
Created: 13-Nov-2008
Updated: 17-Oct-2022
Structure
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Program:
Drawing:
Aligned Rows:
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Conserved site includes 13 residues -Click on image for an interactive view with Cn3D
Feature 1:ligand binding site [chemical binding site]
Evidence:
  • Structure:3RZE: Human histamine H1 receptor bound doxepin (a first-generation H1R antagonist), contacts at 4A.
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Sequence Alignment
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Format: Row Display: Color Bits: Type Selection: 
Feature 1                                                                                        
3RZE_A         9 MPLVVVLSTICLVTVGLNLLVLYAVRSERKLHtvGNLYIVSLSVADLIVGAVVMPMNILYLLms-kWSLGrplCLFWLSM 87 
NP_001012721  61 IPIVTAMSFVSLITCIGNALVIVAVRTDRRLRtvSNYFILSLAVADLLIGTLVMPLSIIYFVeg-kWILGlivCETWLTV 139 purple urchin
NP_001036196  52 AVLGIFLGMLSLLTVIMNLLVLFAVRKERTLHtvGNLYIVSLSIADLIVGATVMPLNLVYLLed-qWKLGhvvCQFWLVM 130 zebrafish
XP_005013834  15 ALLGLFLGSISLITVVMNILVLCAVKTEKKLQtvGNLYIVSLSVADLIVGAAVMPLNIVYLLnsyvWTLGvtaCSFWLSM 94  mallard
XP_002734542  59 VPIGIILSIISLITFLGNALVIHAVRTEKRLQtvSNYFILSLAVADMLIGMVIMPLSTMYYLah-rWPLGlgiCQMWLSL 137 Saccoglossus ko...
XP_002944395  18 ASLGLALGTISALTVVLNILVLYAVRTERKLHtvGNLYIVSLSIADLIVGAAVMPLNIVYLLnr-eWILGrpaCLFWLSM 96  western clawed ...
P35367        28 MPLVVVLSTICLVTVGLNLLVLYAVRSERKLHtvGNLYIVSLSVADLIVGAVVMPMNILYLLms-kWSLGrplCLFWLSM 106 human

Feature 1        ##  ##  #                                          #                            
3RZE_A        88 DYVASTASIFSVFILCIDRYRSVQQPlrYLKYRtKTRASATILGAWFLSFLWVIPILGWnhfmqq--tsvrreDKCETDF 165
NP_001012721 140 DYVSCTASIFNLFILSLDRYWSISSPlkYMKKRtPRRAMLMISLAWCLSFSWIVPVWGWhyferdgeprgvpsDECDTEF 219 purple urchin
NP_001036196 131 DYVASTASIFSLFILCLDRYRSVRHPlqYLKYRtRGRATLLICSAWLLSMTWTIPILGWrmfasvd-kkteleNQCDTDF 209 zebrafish
XP_005013834  95 DYVASTASIFNLFILCIDRYRSVQQPlkYLKYRtKMRALLMILGAWLLSFLWVIPILGWhifaga--ekkkeiVKCETDF 172 mallard
XP_002734542 138 DYVCCTASILNLFILSLDRYWSITSPlkYLRRRtGKRASILISMVWAVSLLWVIPVTGWhafsrgg-ervilhGHCDAEF 216 Saccoglossus ko...
XP_002944395  97 DYVASTASIFSLFILCIDRYRSIQQPlrYLKYRtKTRASLMISGAWLLSFTWVVPILGWhvfangg-vrsvpeSTCETEF 175 western clawed ...
P35367       107 DYVASTASIFSVFILCIDRYRSVQQPlrYLKYRtKTRASATILGAWFLSFLWVIPILGWnhfmqq--tsvrreDKCETDF 184 human

Feature 1                 #   #                                                                  
3RZE_A       166 yDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVrqhcnifemlrideglrlkiykdtegyytigighlltkspslnaaks 245
NP_001012721 220 gSNIIFKVLTAILNFYIPLVSMLFVYGKIFYEIktrskmcvgqrssgnkkysirhsahmiplpvavdvcpntpsneepee 299 purple urchin
NP_001036196 210 rFVTWFKVLTAILNFYIPSFLMLVFYSQIFIAVrdhyrewenfagpalktdatdtltnglqlqitkasekeslalnaysq 289 zebrafish
XP_005013834 173 sTVTWFKVFTAFVNFYLPSILMLCFYCKIFIAVrkhcqhrelinrsylsfsesksvqpgktkdkqsiclqkqildentpp 252 mallard
XP_002734542 217 hRDTIFKVVTGAVNFYIPMIIMVCLYGRIFHEIrkrsnlnigrctyghgvsvttdttyayakdfrktsvndhdfhteyef 296 Saccoglossus ko...
XP_002944395 176 hKVTWFKVLTATLNFYIPSLLMLWFYAKIYKAVrehyqhrevvngsfqlfydsklvqsvrvlkgqqsctktqckdgnltv 255 western clawed ...
P35367       185 yDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVrqhcqhrelinrslpsfseiklrpenpkgdakkpgkespwevlkrkp 264 human

Feature 1                                                                                        
3RZE_A       246 eldkaigrntngvitkdeaeklfnqdvdaavrgilrn------------------------------------------- 282
NP_001012721 300 aeeqnaswipdydslstskdtsqeyadqsescppniaakrikkgevdhqlknishltlatmglagivgpsmmgvpsgqri 379 purple urchin
NP_001036196 290 neglldqysleqpynsrenteemtsepkrkmcykkkaifnlskrmrksvpdseisfqsd--------------------- 348 zebrafish
XP_005013834 253 rdkqrspqpknteaklhfsdpdssskvivsrrnsevlkwscfplttaq-------------------------------- 300 mallard
XP_002734542 297 dssqsnerdsevknleqearfnftnvallrrlkniirtdrnanptvarnldsdqpsstsnedkllhsesyadddtlrfng 376 Saccoglossus ko...
XP_002944395 256 pemnfpaqytpiskefrqsrstqekdpvedygkqkgfshcdnnvfklhcfp----------------------------- 306 western clawed ...
P35367       265 kdagggsvlkspsqtpkemkspvvfsqeddrevdklycfpldivhmqa-------------------------------- 312 human

Feature 1                                                                                        
3RZE_A           --------------------------------------------------------------------------------    
NP_001012721 380 lkrkraekealaikqvkrilpeennrprietihvpmikepsnstssgtvdpqldgeiiqmkeingdvshnksilrqeeaf 459 purple urchin
NP_001036196     --------------------------------------------------------------------------------     zebrafish
XP_005013834     --------------------------------------------------------------------------------     mallard
XP_002734542 377 ttsn---------------------------------------------------------------tdspngqicilrp 393 Saccoglossus ko...
XP_002944395     --------------------------------------------------------------------------------     western clawed ...
P35367           --------------------------------------------------------------------------------     human

Feature 1                                                                                        
3RZE_A       283 ----------------------------------aklkpvydsldavrraalinmvfqmgetgvagftnslrmlqqkrwd 328
NP_001012721 460 lcpdrapngtakrrisftvdsvaskeeleplrrnsyderkttspkyrgvrynkessspthllptdnispdnlspsraipk 539 purple urchin
NP_001036196 349 -----------dgetvaegrpslslaflqsentaqpqtfinvsdcnvlvpnsvgnicesaptvdihnytavlctppspps 417 zebrafish
XP_005013834 301 -----------------------sepgldktgeksvtkdnkneedlfsqdsdlsdasdsqtfteevpcgeesspnperac 357 mallard
XP_002734542 394 pptphlnvnnrritktpepeviwrrrsedelkpppmhfgknvknhspstpmqrsnarrspyhvsathltvtspgmktrkl 473 Saccoglossus ko...
XP_002944395 307 --------------------laiiqgspqecrnyvtvtrgaleehnclrprqreeiseehtfaeaascmvdlsqvgksnm 366 western clawed ...
P35367       313 ----------------------aaegssrdyvavnrshgqlktdeqglnthgaseisedqmlgdsqsfsrtdsdttteta 370 human

Feature 1                                                                 #  ##  #               
3RZE_A       329 eaavnlaksrwynqtpnrakrvittfrtgtwdaylhmNRERKAAKQLGFIMAAFILCWIPYFIFFMVIafcknccNEHLH 408
NP_001012721 540 aqvknggvagrfsfarfsirhgktseflrdrikrfslNKERKAAKQLGIIVSCFITCWLPYFISFMVIaycptcvNPNVH 619 purple urchin
NP_001036196 418 pwaensppldasialpakqswqklceqskqsihsmriRKERKAARQLGFIIGVFMVCWIPYFITFMVMalcetcvHHDLH 497 zebrafish
XP_005013834 358 spqektenrdskgltylrktwqrlhtrsknhlrrlhvNRERKAAKQLGVIMAAFMLCWIPYFVLYMVIafhhderYSTLQ 437 mallard
XP_002734542 474 evtsgiapknskkntfklgklehflkaprkkrfsatlNRERKAAKQLGVIMGCFILCWLPYFILFLIValckdciPENIY 553 Saccoglossus ko...
XP_002944395 367 eapgrtearlsgnfrylkhtwerfrthskqhiqglhmNRERKAAKQLGFIMAAFMLCWIPYFVLFMVIafchnccNHNFH 446 western clawed ...
P35367       371 pgkgklrsgsntgldyikftwkrlrshsrqyvsglhmNRERKAAKQLGFIMAAFILCWIPYFIFFMVIafcknccNEHLH 450 human

Feature 1               #                     
3RZE_A       409 MFTIWLGYINSTLNPLIYPLCNenFKKTF 437
NP_001012721 620 YALIWLGYLNSTMNPFIYPLCNsnFRKAF 648 purple urchin
NP_001036196 498 MFTIWLGYINSTLNPFIYPLCNenFKRVF 526 zebrafish
XP_005013834 438 MVTIWLGYLNSTLNPFLYPLCNhnFKKTF 466 mallard
XP_002734542 554 YATIWLGYVNSTLNPFLYPLCNhnFRRAF 582 Saccoglossus kowalevskii
XP_002944395 447 MFTIWLGYINSTLNPLIYPLCNenFKKTF 475 western clawed frog
P35367       451 MFTIWLGYINSTLNPLIYPLCNenFKKTF 479 human

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