Details of the Target

General Information of Target

Target ID LDTP03136
Target Name Ryanodine receptor 1 (RYR1)
Gene Name RYR1
Gene ID 6261
Synonyms
RYDR; Ryanodine receptor 1; RYR-1; RyR1; Skeletal muscle calcium release channel; Skeletal muscle ryanodine receptor; Skeletal muscle-type ryanodine receptor; Type 1 ryanodine receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGDAEGEDEVQFLRTDDEVVLQCSATVLKEQLKLCLAAEGFGNRLCFLEPTSNAQNVPPD
LAICCFVLEQSLSVRALQEMLANTVEAGVESSQGGGHRTLLYGHAILLRHAHSRMYLSCL
TTSRSMTDKLAFDVGLQEDATGEACWWTMHPASKQRSEGEKVRVGDDIILVSVSSERYLH
LSTASGELQVDASFMQTLWNMNPICSRCEEGFVTGGHVLRLFHGHMDECLTISPADSDDQ
RRLVYYEGGAVCTHARSLWRLEPLRISWSGSHLRWGQPLRVRHVTTGQYLALTEDQGLVV
VDASKAHTKATSFCFRISKEKLDVAPKRDVEGMGPPEIKYGESLCFVQHVASGLWLTYAA
PDPKALRLGVLKKKAMLHQEGHMDDALSLTRCQQEESQAARMIHSTNGLYNQFIKSLDSF
SGKPRGSGPPAGTALPIEGVILSLQDLIIYFEPPSEDLQHEEKQSKLRSLRNRQSLFQEE
GMLSMVLNCIDRLNVYTTAAHFAEFAGEEAAESWKEIVNLLYELLASLIRGNRSNCALFS
TNLDWLVSKLDRLEASSGILEVLYCVLIESPEVLNIIQENHIKSIISLLDKHGRNHKVLD
VLCSLCVCNGVAVRSNQDLITENLLPGRELLLQTNLINYVTSIRPNIFVGRAEGTTQYSK
WYFEVMVDEVTPFLTAQATHLRVGWALTEGYTPYPGAGEGWGGNGVGDDLYSYGFDGLHL
WTGHVARPVTSPGQHLLAPEDVISCCLDLSVPSISFRINGCPVQGVFESFNLDGLFFPVV
SFSAGVKVRFLLGGRHGEFKFLPPPGYAPCHEAVLPRERLHLEPIKEYRREGPRGPHLVG
PSRCLSHTDFVPCPVDTVQIVLPPHLERIREKLAENIHELWALTRIEQGWTYGPVRDDNK
RLHPCLVDFHSLPEPERNYNLQMSGETLKTLLALGCHVGMADEKAEDNLKKTKLPKTYMM
SNGYKPAPLDLSHVRLTPAQTTLVDRLAENGHNVWARDRVGQGWSYSAVQDIPARRNPRL
VPYRLLDEATKRSNRDSLCQAVRTLLGYGYNIEPPDQEPSQVENQSRCDRVRIFRAEKSY
TVQSGRWYFEFEAVTTGEMRVGWARPELRPDVELGADELAYVFNGHRGQRWHLGSEPFGR
PWQPGDVVGCMIDLTENTIIFTLNGEVLMSDSGSETAFREIEIGDGFLPVCSLGPGQVGH
LNLGQDVSSLRFFAICGLQEGFEPFAINMQRPVTTWFSKGLPQFEPVPLEHPHYEVSRVD
GTVDTPPCLRLTHRTWGSQNSLVEMLFLRLSLPVQFHQHFRCTAGATPLAPPGLQPPAED
EARAAEPDPDYENLRRSAGGWSEAENGKEGTAKEGAPGGTPQAGGEAQPARAENEKDATT
EKNKKRGFLFKAKKVAMMTQPPATPTLPRLPHDVVPADNRDDPEIILNTTTYYYSVRVFA
GQEPSCVWAGWVTPDYHQHDMSFDLSKVRVVTVTMGDEQGNVHSSLKCSNCYMVWGGDFV
SPGQQGRISHTDLVIGCLVDLATGLMTFTANGKESNTFFQVEPNTKLFPAVFVLPTHQNV
IQFELGKQKNIMPLSAAMFQSERKNPAPQCPPRLEMQMLMPVSWSRMPNHFLQVETRRAG
ERLGWAVQCQEPLTMMALHIPEENRCMDILELSERLDLQRFHSHTLRLYRAVCALGNNRV
AHALCSHVDQAQLLHALEDAHLPGPLRAGYYDLLISIHLESACRSRRSMLSEYIVPLTPE
TRAITLFPPGRSTENGHPRHGLPGVGVTTSLRPPHHFSPPCFVAALPAAGAAEAPARLSP
AIPLEALRDKALRMLGEAVRDGGQHARDPVGGSVEFQFVPVLKLVSTLLVMGIFGDEDVK
QILKMIEPEVFTEEEEEEDEEEEGEEEDEEEKEEDEEETAQEKEDEEKEEEEAAEGEKEE
GLEEGLLQMKLPESVKLQMCHLLEYFCDQELQHRVESLAAFAERYVDKLQANQRSRYGLL
IKAFSMTAAETARRTREFRSPPQEQINMLLQFKDGTDEEDCPLPEEIRQDLLDFHQDLLA
HCGIQLDGEEEEPEEETTLGSRLMSLLEKVRLVKKKEEKPEEERSAEESKPRSLQELVSH
MVVRWAQEDFVQSPELVRAMFSLLHRQYDGLGELLRALPRAYTISPSSVEDTMSLLECLG
QIRSLLIVQMGPQEENLMIQSIGNIMNNKVFYQHPNLMRALGMHETVMEVMVNVLGGGES
KEIRFPKMVTSCCRFLCYFCRISRQNQRSMFDHLSYLLENSGIGLGMQGSTPLDVAAASV
IDNNELALALQEQDLEKVVSYLAGCGLQSCPMLVAKGYPDIGWNPCGGERYLDFLRFAVF
VNGESVEENANVVVRLLIRKPECFGPALRGEGGSGLLAAIEEAIRISEDPARDGPGIRRD
RRREHFGEEPPEENRVHLGHAIMSFYAALIDLLGRCAPEMHLIQAGKGEALRIRAILRSL
VPLEDLVGIISLPLQIPTLGKDGALVQPKMSASFVPDHKASMVLFLDRVYGIENQDFLLH
VLDVGFLPDMRAAASLDTATFSTTEMALALNRYLCLAVLPLITKCAPLFAGTEHRAIMVD
SMLHTVYRLSRGRSLTKAQRDVIEDCLMSLCRYIRPSMLQHLLRRLVFDVPILNEFAKMP
LKLLTNHYERCWKYYCLPTGWANFGVTSEEELHLTRKLFWGIFDSLAHKKYDPELYRMAM
PCLCAIAGALPPDYVDASYSSKAEKKATVDAEGNFDPRPVETLNVIIPEKLDSFINKFAE
YTHEKWAFDKIQNNWSYGENIDEELKTHPMLRPYKTFSEKDKEIYRWPIKESLKAMIAWE
WTIEKAREGEEEKTEKKKTRKISQSAQTYDPREGYNPQPPDLSAVTLSRELQAMAEQLAE
NYHNTWGRKKKQELEAKGGGTHPLLVPYDTLTAKEKARDREKAQELLKFLQMNGYAVTRG
LKDMELDSSSIEKRFAFGFLQQLLRWMDISQEFIAHLEAVVSSGRVEKSPHEQEIKFFAK
ILLPLINQYFTNHCLYFLSTPAKVLGSGGHASNKEKEMITSLFCKLAALVRHRVSLFGTD
APAVVNCLHILARSLDARTVMKSGPEIVKAGLRSFFESASEDIEKMVENLRLGKVSQART
QVKGVGQNLTYTTVALLPVLTTLFQHIAQHQFGDDVILDDVQVSCYRTLCSIYSLGTTKN
TYVEKLRPALGECLARLAAAMPVAFLEPQLNEYNACSVYTTKSPRERAILGLPNSVEEMC
PDIPVLERLMADIGGLAESGARYTEMPHVIEITLPMLCSYLPRWWERGPEAPPSALPAGA
PPPCTAVTSDHLNSLLGNILRIIVNNLGIDEASWMKRLAVFAQPIVSRARPELLQSHFIP
TIGRLRKRAGKVVSEEEQLRLEAKAEAQEGELLVRDEFSVLCRDLYALYPLLIRYVDNNR
AQWLTEPNPSAEELFRMVGEIFIYWSKSHNFKREEQNFVVQNEINNMSFLTADNKSKMAK
AGDIQSGGSDQERTKKKRRGDRYSVQTSLIVATLKKMLPIGLNMCAPTDQDLITLAKTRY
ALKDTDEEVREFLHNNLHLQGKVEGSPSLRWQMALYRGVPGREEDADDPEKIVRRVQEVS
AVLYYLDQTEHPYKSKKAVWHKLLSKQRRRAVVACFRMTPLYNLPTHRACNMFLESYKAA
WILTEDHSFEDRMIDDLSKAGEQEEEEEEVEEKKPDPLHQLVLHFSRTALTEKSKLDEDY
LYMAYADIMAKSCHLEEGGENGEAEEEVEVSFEEKQMEKQRLLYQQARLHTRGAAEMVLQ
MISACKGETGAMVSSTLKLGISILNGGNAEVQQKMLDYLKDKKEVGFFQSIQALMQTCSV
LDLNAFERQNKAEGLGMVNEDGTVINRQNGEKVMADDEFTQDLFRFLQLLCEGHNNDFQN
YLRTQTGNTTTINIIICTVDYLLRLQESISDFYWYYSGKDVIEEQGKRNFSKAMSVAKQV
FNSLTEYIQGPCTGNQQSLAHSRLWDAVVGFLHVFAHMMMKLAQDSSQIELLKELLDLQK
DMVVMLLSLLEGNVVNGMIARQMVDMLVESSSNVEMILKFFDMFLKLKDIVGSEAFQDYV
TDPRGLISKKDFQKAMDSQKQFSGPEIQFLLSCSEADENEMINCEEFANRFQEPARDIGF
NVAVLLTNLSEHVPHDPRLHNFLELAESILEYFRPYLGRIEIMGASRRIERIYFEISETN
RAQWEMPQVKESKRQFIFDVVNEGGEAEKMELFVSFCEDTIFEMQIAAQISEPEGEPETD
EDEGAGAAEAGAEGAEEGAAGLEGTAATAAAGATARVVAAAGRALRGLSYRSLRRRVRRL
RRLTAREAATAVAALLWAAVTRAGAAGAGAAAGALGLLWGSLFGGGLVEGAKKVTVTELL
AGMPDPTSDEVHGEQPAGPGGDADGEGASEGAGDAAEGAGDEEEAVHEAGPGGADGAVAV
TDGGPFRPEGAGGLGDMGDTTPAEPPTPEGSPILKRKLGVDGVEEELPPEPEPEPEPELE
PEKADAENGEKEEVPEPTPEPPKKQAPPSPPPKKEEAGGEFWGELEVQRVKFLNYLSRNF
YTLRFLALFLAFAINFILLFYKVSDSPPGEDDMEGSAAGDVSGAGSGGSSGWGLGAGEEA
EGDEDENMVYYFLEESTGYMEPALRCLSLLHTLVAFLCIIGYNCLKVPLVIFKREKELAR
KLEFDGLYITEQPEDDDVKGQWDRLVLNTPSFPSNYWDKFVKRKVLDKHGDIYGRERIAE
LLGMDLATLEITAHNERKPNPPPGLLTWLMSIDVKYQIWKFGVIFTDNSFLYLGWYMVMS
LLGHYNNFFFAAHLLDIAMGVKTLRTILSSVTHNGKQLVMTVGLLAVVVYLYTVVAFNFF
RKFYNKSEDEDEPDMKCDDMMTCYLFHMYVGVRAGGGIGDEIEDPAGDEYELYRVVFDIT
FFFFVIVILLAIIQGLIIDAFGELRDQQEQVKEDMETKCFICGIGSDYFDTTPHGFETHT
LEEHNLANYMFFLMYLINKDETEHTGQESYVWKMYQERCWDFFPAGDCFRKQYEDQLS
Target Type
Discontinued
Target Bioclass
Transporter and channel
Family
Ryanodine receptor (TC 1.A.3.1) family, RYR1 subfamily
Subcellular location
Sarcoplasmic reticulum membrane
Function
Cytosolic calcium-activated calcium channel that mediates the release of Ca(2+) from the sarcoplasmic reticulum into the cytosol and thereby plays a key role in triggering muscle contraction following depolarization of T-tubules. Repeated very high-level exercise increases the open probability of the channel and leads to Ca(2+) leaking into the cytoplasm. Can also mediate the release of Ca(2+) from intracellular stores in neurons, and may thereby promote prolonged Ca(2+) signaling in the brain. Required for normal embryonic development of muscle fibers and skeletal muscle. Required for normal heart morphogenesis, skin development and ossification during embryogenesis.
TTD ID
T92328
Uniprot ID
P21817
DrugMap ID
TTU5CIX
Ensemble ID
ENST00000355481.8
HGNC ID
HGNC:10483
ChEMBL ID
CHEMBL1846

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.A2391V; p.L3964I .
A172 SNV: p.L4793M .
AN3CA SNV: p.Q379R .
CAL78 SNV: p.V1122L .
CAMA1 SNV: p.D133N; p.E210K .
CASKI SNV: p.V895L .
COLO792 SNV: p.G1049D .
COLO800 SNV: p.T1275I .
DU145 SNV: p.E337K; p.P978T; p.M2198T .
FTC133 SNV: p.P3697H .
G415 SNV: p.R1964C .
GB1 SNV: p.N771I .
HCC15 SNV: p.D1856Y .
HCT15 Insertion: p.G2407WfsTer2
SNV: p.V2073L;p.A2566V;p.E3687D		 .
HDQP1 SNV: p.A4597P .
HEC1 SNV: p.S1462N; p.R2369W; p.E2371D .
HEC1B SNV: p.S1462N; p.R2369W; p.E2371D .
HLF SNV: p.A1116T .
HS936T SNV: p.R1067C .
HT115 SNV: p.D329G; p.A2315T; p.F3017L .
HUH7 SNV: p.E4211Ter .
ICC4 SNV: p.L4379F .
IGR1 SNV: p.P2114L; p.V2168L; p.R2676Q .
IGROV1 Deletion: p.A1318PfsTer80 .
IPC298 SNV: p.L736F .
Ishikawa (Heraklio) 02 ER Deletion: p.C1268AfsTer4
SNV: p.Y919C;p.R1274G;p.T1527S		 .
J82 SNV: p.R1067L .
JHH4 SNV: p.L932M .
JURKAT Deletion: p.P3062QfsTer19
SNV: p.D4005V		 .
KELLY SNV: p.G2480S .
KMS27 SNV: p.S3279R .
KU1919 SNV: p.K1348E .
KYSE410 SNV: p.D2020Y .
LN18 SNV: p.A2106S .
LNCaP clone FGC SNV: p.C2021Y; p.I4009V .
MCC13 SNV: p.R552W; p.G705E; p.N1051S .
MCC26 SNV: p.G840D .
MELHO SNV: p.E2348K .
MELJUSO Substitution: p.R3768Q .
MEWO SNV: p.H2100Y; p.S3314F; p.E3754K .
MOLT4 SNV: p.S405N; p.S1291N .
MONOMAC6 SNV: p.S1489N .
NALM6 SNV: p.R1593W; p.N3325K .
NB4 SNV: p.H719N .
NCIH1155 SNV: p.A2277G; p.I2603V .
NCIH1993 SNV: p.P2146L .
NCIH2172 Deletion: p.Q1040RfsTer69
SNV: p.E294Ter;p.W1495C		 .
NCIH23 SNV: p.P752Q; p.R2738L .
NCIH446 SNV: p.P1795Q .
NCIH716 SNV: p.C145F .
NCIH82 SNV: p.L3553P .
PC3 SNV: p.N2213H .
PC9 SNV: p.E1878V .
PF382 SNV: p.R2954W .
REC1 SNV: p.A4739V .
REH SNV: p.E1876D .
RKN SNV: p.A555G; p.V1009A .
RL952 SNV: p.R2588C .
SHP77 SNV: p.V3748G .
SKMEL2 SNV: p.A2979V .
SKMEL28 SNV: p.N1333I .
SKMEL30 SNV: p.P1573S .
SKMEL5 SNV: p.W1604Ter .
SKNAS SNV: p.P2091T .
SNGM SNV: p.Q1143Ter; p.E4677G .
SNU1 SNV: p.V1765A .
SNU1196 Substitution: p.D1328T .
SSP25 SNV: p.F3828L .
SUPT1 SNV: p.D60H; p.P4154Q .
SW1116 SNV: p.Y964Ter .
SW1271 SNV: p.Y2882N .
SW403 SNV: p.E3564K .
TCCSUP SNV: p.L845F .
TOV21G SNV: p.W4779L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C2158(1.16)  LDD3401  [1]
Acrolein
 Probe Info  		N.A.  LDD0231  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 Rh41 C2158(1.07)  LDD2571  [1]
 LDCM0023  KB03 RD C2158(1.47)  LDD2984  [1]
 LDCM0024  KB05 RD C2158(1.16)  LDD3401  [1]
 LDCM0109  NEM HeLa N.A.  LDD0231  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Caffeine Small molecular drug DB00201
Calcium Phosphate Small molecular drug DB11348
Calcium Phosphate Dihydrate Small molecular drug DB14481
Dantrolene Small molecular drug DB01219
Tetracaine Small molecular drug DB09085
Calcium Citrate . DB11093
Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(O10eq)-benzyloxycarbonyl-beta-alanylryanodine Small molecular drug D0WT2Z
(O10eq)-beta-alanyl-anhydro-ryanodine Small molecular drug D04QNI
(O10eq)-beta-alanylryanodine Small molecular drug D0S6KD
(O10eq)-beta-guanidinopropionylryanodine Small molecular drug D0GM8V
(O10eq)-guanidino Acetylryanodine Small molecular drug D0J6WG
Anhydroryanidine Small molecular drug D0U3DW
Benzyloxycarbonyl-glycylryanodine Small molecular drug D01MHP
Di-benzyloxycarbonyl-guanidino Acetylryanodine Small molecular drug D0G2RB
Glycylryanodine Small molecular drug D05QKM
N-methyl Ryanodine-succinamidate Small molecular drug D05VJH
Ruthenium Red Small molecular drug D02DZN
Ryanodine Small molecular drug D08LUJ
Suramin Small molecular drug DB04786
Discontinued
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Arm036 Small molecular drug D0T2LP
Cdp-1050 . D0C3HS

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.