Details of the Target

General Information of Target

Target ID LDTP09852
Target Name Ryanodine receptor 2 (RYR2)
Gene Name RYR2
Gene ID 6262
Synonyms
Ryanodine receptor 2; RYR-2; RyR2; hRYR-2; Cardiac muscle ryanodine receptor; Cardiac muscle ryanodine receptor-calcium release channel; Type 2 ryanodine receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNGQLDLSGKLIIKAQLGEDIRRIPIHNEDITYDELVLMMQRVFRGKLLSNDEVTIKYKD
EDGDLITIFDSSDLSFAIQCSRILKLTLFVNGQPRPLESSQVKYLRRELIELRNKVNRLL
DSLEPPGEPGPSTNIPENDTVDGREEKSASDSSGKQSTQVMAASMSAFDPLKNQDEINKN
VMSAFGLTDDQVSGPPSAPAEDRSGTPDSIASSSSAAHPPGVQPQQPPYTGAQTQAGQIE
GQMYQQYQQQAGYGAQQPQAPPQQPQQYGIQYSASYSQQTGPQQPQQFQGYGQQPTSQAP
APAFSGQPQQLPAQPPQQYQASNYPAQTYTAQTSQPTNYTVAPASQPGMAPSQPGAYQPR
PGFTSLPGSTMTPPPSGPNPYARNRPPFGQGYTQPGPGYR
Target Bioclass
Transporter and channel
Family
Ryanodine receptor (TC 1.A.3.1) family, RYR2 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 cardiac muscle contraction. Aberrant channel activation can lead to cardiac arrhythmia. In cardiac myocytes, calcium release is triggered by increased Ca(2+) cytosolic levels due to activation of the L-type calcium channel CACNA1C. The calcium channel activity is modulated by formation of heterotetramers with RYR3. Required for cellular calcium ion homeostasis. Required for embryonic heart development.
Uniprot ID
Q92736
Ensemble ID
ENST00000366574.7
HGNC ID
HGNC:10484
ChEMBL ID
CHEMBL4403

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.R1888Q; p.P3753S .
786O SNV: p.D1112V .
A172 SNV: p.G2337Ter .
AGS Deletion: p.C1509LfsTer19
SNV: p.F1768I		 .
CAL148 SNV: p.P2678S .
CAL78 SNV: p.S1767R .
CALU6 SNV: p.R2235S .
CCK81 SNV: p.K4092N; p.G4321C; p.H4468Q .
CHL1 SNV: p.G2949S .
COLO792 SNV: p.F4951Y .
COLO800 SNV: p.R3904Q .
CORL88 SNV: p.G369D .
DAOY SNV: p.P2286L .
DU145 SNV: p.A4357P; p.C4957Ter .
EFO27 SNV: p.A4091V .
ETK1 SNV: p.I898F .
HCC15 SNV: p.Q12H .
HCC827 SNV: p.L3519M .
HCT116 Deletion: p.E4011del
SNV: p.I952M		 .
HCT15 SNV: p.A2515D; p.A4682T; p.L4780I .
HEC1 SNV: p.G3735D; p.A4203V .
HEC1B SNV: p.K3329R; p.R3397H; p.G3735D .
HELA SNV: p.E2726Q .
HEPG2 SNV: p.W733C .
HGC27 SNV: p.G2008R .
HLF SNV: p.M1? .
HS936T SNV: p.P1600S .
HT115 SNV: p.R111Ter; p.G432S; p.A2213V; p.K4324T; p.D4745N .
HUH1 SNV: p.S4360F .
IGR1 SNV: p.S837N; p.G2310E .
IGROV1 Insertion: p.M964NfsTer42 .
Ishikawa (Heraklio) 02 ER SNV: p.A4142T .
JHH6 SNV: p.L900I; p.K1394N .
KATOIII SNV: p.Y706Ter .
KMCH1 SNV: p.K2140N; p.K2965E .
KMRC3 SNV: p.P2873R; p.S3006C .
KMS11 SNV: p.E1635K .
KMS12BM SNV: p.F1201L .
KO52 SNV: p.H1841Y .
KP4 SNV: p.E4872Q .
KPL1 SNV: p.P4534H .
KYSE410 SNV: p.A1075T; p.P2428H; p.D3176G; p.H4108N .
KYSE510 SNV: p.L4720F .
LNCaP clone FGC Deletion: .
SNV: p.C633Y		 .
LS123 SNV: p.G719V .
LS180 SNV: p.I1273L .
LS513 SNV: p.A2346E .
MCC13 SNV: p.R564K;p.P853S;p.S4285L
Substitution: .		 .
MCC26 SNV: p.G2900E; p.G3141E .
MDAMB453 SNV: p.D1808N; p.R2616K; p.A3165T .
MEWO SNV: p.L648F; p.Q1940Ter; p.F1979C; p.D2696N; p.A2799T; p.E4064K; p.F4305L; p.L4376I .
MFE280 SNV: p.G1163W .
MINO SNV: p.A4091V .
MOLT4 SNV: p.D4646N .
NALM6 SNV: p.W2732R .
NCIH1048 Insertion: p.K1887QfsTer17 .
NCIH1155 SNV: p.D1449N .
NCIH1650 SNV: p.E535Q .
NCIH1703 SNV: p.P1356S; p.E1526Ter; p.V1563G; p.Q3422R; p.V4125L .
NCIH1792 SNV: p.A1568E; p.L1893M .
NCIH1793 Deletion: p.C1914LfsTer9
SNV: p.A2243V		 .
NCIH196 SNV: p.L2610Q .
NCIH1993 SNV: p.C65R; p.R414L; p.E1646V; p.R3567L .
NCIH2170 SNV: p.C2308Y .
NCIH2172 SNV: p.G570V;p.A1365D;p.V2171L;p.R2886I
Substitution: p.R235G		 .
NCIH2286 SNV: p.P448T; p.P916T; p.H1674D; p.G2537V; p.P2915H; p.A4400D .
NCIH23 SNV: p.T3199N;p.D4079Y
Substitution: p.L1829P		 .
NCIH358 SNV: p.P2774T .
NCIH661 SNV: p.Q669K .
ONS76 SNV: p.I1632F .
OSRC2 SNV: p.P2428H .
OV90 SNV: p.R807Ter .
PC9 SNV: p.Q1123K .
PF382 SNV: p.N2318S .
REC1 SNV: p.H1710N .
REH SNV: p.G2110S .
RL952 SNV: p.E4443V .
RPMI7951 SNV: p.F4020Y; p.V4042A .
RT112 SNV: p.G1291R .
SG231 SNV: p.A224T .
SHP77 SNV: p.P816T .
SKMEL28 SNV: p.G605R .
SNGM SNV: p.P1759S .
SNU478 SNV: p.G717D .
SSP25 SNV: p.I898F
Substitution: p.L933P		 .
SUPT1 Deletion: p.D3347TfsTer10 .
SW1271 SNV: p.G2310V; p.S4141R .
SW756 SNV: p.E3630Q .
T24 SNV: p.R2401H .
TE11 SNV: p.T1716I .
TE4 SNV: p.G4820R .
TOV21G SNV: p.S1567Ter; p.F3835L .
UACC62 SNV: p.W4708Ter .
ZR751 SNV: p.D1298N; p.E2769K .

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  		C1078(1.56)  LDD3423  [1]
IA-alkyne
 Probe Info  		N.A.  LDD2242  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C1078(1.08)  LDD1507  [3]
 LDCM0276  AC17 HEK-293T C1078(1.14)  LDD1515  [3]
 LDCM0285  AC25 HEK-293T C1078(0.97)  LDD1524  [3]
 LDCM0294  AC33 HEK-293T C1078(1.13)  LDD1533  [3]
 LDCM0303  AC41 HEK-293T C1078(1.08)  LDD1542  [3]
 LDCM0311  AC49 HEK-293T C1078(1.24)  LDD1550  [3]
 LDCM0320  AC57 HEK-293T C1078(1.24)  LDD1559  [3]
 LDCM0356  AKOS034007680 HEK-293T C1078(1.07)  LDD1570  [3]
 LDCM0367  CL1 HEK-293T C1078(1.21)  LDD1571  [3]
 LDCM0370  CL101 HEK-293T C1078(1.24)  LDD1574  [3]
 LDCM0374  CL105 HEK-293T C1078(1.11)  LDD1578  [3]
 LDCM0378  CL109 HEK-293T C1078(1.28)  LDD1582  [3]
 LDCM0383  CL113 HEK-293T C1078(1.44)  LDD1587  [3]
 LDCM0387  CL117 HEK-293T C1078(1.25)  LDD1591  [3]
 LDCM0392  CL121 HEK-293T C1078(1.37)  LDD1596  [3]
 LDCM0396  CL125 HEK-293T C1078(1.10)  LDD1600  [3]
 LDCM0400  CL13 HEK-293T C1078(1.25)  LDD1604  [3]
 LDCM0404  CL17 HEK-293T C1078(1.26)  LDD1608  [3]
 LDCM0413  CL25 HEK-293T C1078(1.21)  LDD1617  [3]
 LDCM0417  CL29 HEK-293T C1078(1.29)  LDD1621  [3]
 LDCM0426  CL37 HEK-293T C1078(1.13)  LDD1630  [3]
 LDCM0431  CL41 HEK-293T C1078(1.17)  LDD1635  [3]
 LDCM0439  CL49 HEK-293T C1078(1.18)  LDD1643  [3]
 LDCM0440  CL5 HEK-293T C1078(1.26)  LDD1644  [3]
 LDCM0444  CL53 HEK-293T C1078(1.22)  LDD1647  [3]
 LDCM0453  CL61 HEK-293T C1078(1.11)  LDD1656  [3]
 LDCM0457  CL65 HEK-293T C1078(1.25)  LDD1660  [3]
 LDCM0466  CL73 HEK-293T C1078(1.24)  LDD1669  [3]
 LDCM0470  CL77 HEK-293T C1078(1.26)  LDD1673  [3]
 LDCM0479  CL85 HEK-293T C1078(1.21)  LDD1682  [3]
 LDCM0483  CL89 HEK-293T C1078(1.16)  LDD1686  [3]
 LDCM0492  CL97 HEK-293T C1078(1.07)  LDD1695  [3]
 LDCM0022  KB02 A673 C1078(1.68)  LDD2261  [1]
 LDCM0023  KB03 SK-ES1 C1078(1.18)  LDD3006  [1]
 LDCM0024  KB05 SK-ES1 C1078(1.56)  LDD3423  [1]

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 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
3 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402