General Information of Target

Target ID LDTP05733
Target Name Serine/threonine-protein kinase 4 (STK4)
Gene Name STK4
Gene ID 6789
Synonyms
KRS2; MST1; Serine/threonine-protein kinase 4; EC 2.7.11.1; Mammalian STE20-like protein kinase 1; MST-1; STE20-like kinase MST1; Serine/threonine-protein kinase Krs-2) [Cleaved into: Serine/threonine-protein kinase 4 37kDa subunit; MST1/N; Serine/threonine-protein kinase 4 18kDa subunit; MST1/C)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
METVQLRNPPRRQLKKLDEDSLTKQPEEVFDVLEKLGEGSYGSVYKAIHKETGQIVAIKQ
VPVESDLQEIIKEISIMQQCDSPHVVKYYGSYFKNTDLWIVMEYCGAGSVSDIIRLRNKT
LTEDEIATILQSTLKGLEYLHFMRKIHRDIKAGNILLNTEGHAKLADFGVAGQLTDTMAK
RNTVIGTPFWMAPEVIQEIGYNCVADIWSLGITAIEMAEGKPPYADIHPMRAIFMIPTNP
PPTFRKPELWSDNFTDFVKQCLVKSPEQRATATQLLQHPFVRSAKGVSILRDLINEAMDV
KLKRQESQQREVDQDDEENSEEDEMDSGTMVRAVGDEMGTVRVASTMTDGANTMIEHDDT
LPSQLGTMVINAEDEEEEGTMKRRDETMQPAKPSFLEYFEQKEKENQINSFGKSVPGPLK
NSSDWKIPQDGDYEFLKSWTVEDLQKRLLALDPMMEQEIEEIRQKYQSKRQPILDAIEAK
KRRQQNF
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, STE20 subfamily
Subcellular location
Cytoplasm
Function
Stress-activated, pro-apoptotic kinase which, following caspase-cleavage, enters the nucleus and induces chromatin condensation followed by internucleosomal DNA fragmentation. Key component of the Hippo signaling pathway which plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. STK3/MST2 and STK4/MST1 are required to repress proliferation of mature hepatocytes, to prevent activation of facultative adult liver stem cells (oval cells), and to inhibit tumor formation. Phosphorylates 'Ser-14' of histone H2B (H2BS14ph) during apoptosis. Phosphorylates FOXO3 upon oxidative stress, which results in its nuclear translocation and cell death initiation. Phosphorylates MOBKL1A, MOBKL1B and RASSF2. Phosphorylates TNNI3 (cardiac Tn-I) and alters its binding affinity to TNNC1 (cardiac Tn-C) and TNNT2 (cardiac Tn-T). Phosphorylates FOXO1 on 'Ser-212' and regulates its activation and stimulates transcription of PMAIP1 in a FOXO1-dependent manner. Phosphorylates SIRT1 and inhibits SIRT1-mediated p53/TP53 deacetylation, thereby promoting p53/TP53 dependent transcription and apoptosis upon DNA damage. Acts as an inhibitor of PKB/AKT1. Phosphorylates AR on 'Ser-650' and suppresses its activity by intersecting with PKB/AKT1 signaling and antagonizing formation of AR-chromatin complexes.
TTD ID
T47164
Uniprot ID
Q13043
DrugMap ID
TTCPLVN
Ensemble ID
ENST00000372801.5
HGNC ID
HGNC:11408
ChEMBL ID
CHEMBL4598

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.S111Y .
HT SNV: p.V44I .
MDAMB453 SNV: p.V204L .
NCIH2172 SNV: p.R115L .
RL952 SNV: p.C203Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 19 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info 
50.00  LDD0214  [1]
m-APA
 Probe Info 
15.00  LDD0402  [2]
TG42
 Probe Info 
4.01  LDD0043  [3]
STPyne
 Probe Info 
K135(1.38)  LDD2217  [4]
DBIA
 Probe Info 
C80(1.49)  LDD3331  [5]
Sulforaphane-probe2
 Probe Info 
3.71  LDD0160  [6]
IPM
 Probe Info 
C80(1.75)  LDD1702  [7]
5E-2FA
 Probe Info 
N.A.  LDD2235  [8]
AMP probe
 Probe Info 
N.A.  LDD0200  [9]
ATP probe
 Probe Info 
K59(0.00); K151(0.00); K180(0.00)  LDD0199  [9]
4-Iodoacetamidophenylacetylene
 Probe Info 
N.A.  LDD0038  [10]
IA-alkyne
 Probe Info 
N.A.  LDD0036  [10]
Lodoacetamide azide
 Probe Info 
N.A.  LDD0037  [10]
ATP probe
 Probe Info 
K59(0.00); K151(0.00)  LDD0035  [11]
KY-26
 Probe Info 
N.A.  LDD0301  [12]
SF
 Probe Info 
N.A.  LDD0028  [13]
1c-yne
 Probe Info 
N.A.  LDD0228  [14]
Methacrolein
 Probe Info 
N.A.  LDD0218  [15]
AOyne
 Probe Info 
15.00  LDD0443  [16]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C220
 Probe Info 
13.36  LDD1894  [17]
C350
 Probe Info 
22.47  LDD2011  [17]
FFF probe11
 Probe Info 
20.00  LDD0471  [18]
FFF probe3
 Probe Info 
20.00  LDD0465  [18]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C80(0.93)  LDD1507  [19]
 LDCM0215  AC10 PaTu 8988t C80(0.97)  LDD1094  [20]
 LDCM0226  AC11 PaTu 8988t C80(1.12)  LDD1105  [20]
 LDCM0230  AC113 PaTu 8988t C80(1.04)  LDD1109  [20]
 LDCM0231  AC114 PaTu 8988t C80(0.90)  LDD1110  [20]
 LDCM0232  AC115 PaTu 8988t C80(0.86)  LDD1111  [20]
 LDCM0233  AC116 PaTu 8988t C80(1.02)  LDD1112  [20]
 LDCM0234  AC117 PaTu 8988t C80(1.03)  LDD1113  [20]
 LDCM0235  AC118 PaTu 8988t C80(0.93)  LDD1114  [20]
 LDCM0236  AC119 PaTu 8988t C80(1.08)  LDD1115  [20]
 LDCM0237  AC12 PaTu 8988t C80(1.08)  LDD1116  [20]
 LDCM0238  AC120 PaTu 8988t C80(1.06)  LDD1117  [20]
 LDCM0239  AC121 PaTu 8988t C80(1.06)  LDD1118  [20]
 LDCM0240  AC122 PaTu 8988t C80(0.98)  LDD1119  [20]
 LDCM0241  AC123 PaTu 8988t C80(0.85)  LDD1120  [20]
 LDCM0242  AC124 PaTu 8988t C80(0.98)  LDD1121  [20]
 LDCM0243  AC125 PaTu 8988t C80(0.75)  LDD1122  [20]
 LDCM0244  AC126 PaTu 8988t C80(0.91)  LDD1123  [20]
 LDCM0245  AC127 PaTu 8988t C80(0.96)  LDD1124  [20]
 LDCM0259  AC14 PaTu 8988t C80(1.15)  LDD1138  [20]
 LDCM0270  AC15 PaTu 8988t C80(1.01)  LDD1149  [20]
 LDCM0276  AC17 HEK-293T C80(0.95)  LDD1515  [19]
 LDCM0277  AC18 HEK-293T C80(0.98)  LDD1516  [19]
 LDCM0278  AC19 HEK-293T C80(0.96)  LDD1517  [19]
 LDCM0279  AC2 HEK-293T C80(0.93)  LDD1518  [19]
 LDCM0280  AC20 HEK-293T C80(0.95)  LDD1519  [19]
 LDCM0281  AC21 HEK-293T C80(0.96)  LDD1520  [19]
 LDCM0282  AC22 HEK-293T C80(1.08)  LDD1521  [19]
 LDCM0283  AC23 HEK-293T C80(0.95)  LDD1522  [19]
 LDCM0284  AC24 HEK-293T C80(0.93)  LDD1523  [19]
 LDCM0285  AC25 PaTu 8988t C80(1.05)  LDD1164  [20]
 LDCM0286  AC26 PaTu 8988t C80(0.98)  LDD1165  [20]
 LDCM0287  AC27 PaTu 8988t C80(1.01)  LDD1166  [20]
 LDCM0288  AC28 PaTu 8988t C80(1.08)  LDD1167  [20]
 LDCM0289  AC29 PaTu 8988t C80(1.07)  LDD1168  [20]
 LDCM0290  AC3 HEK-293T C80(0.98)  LDD1529  [19]
 LDCM0291  AC30 PaTu 8988t C80(1.10)  LDD1170  [20]
 LDCM0292  AC31 PaTu 8988t C80(1.12)  LDD1171  [20]
 LDCM0293  AC32 PaTu 8988t C80(0.96)  LDD1172  [20]
 LDCM0294  AC33 PaTu 8988t C80(0.95)  LDD1173  [20]
 LDCM0295  AC34 PaTu 8988t C80(1.04)  LDD1174  [20]
 LDCM0296  AC35 PaTu 8988t C80(0.86)  LDD1175  [20]
 LDCM0297  AC36 PaTu 8988t C80(0.79)  LDD1176  [20]
 LDCM0298  AC37 PaTu 8988t C80(0.90)  LDD1177  [20]
 LDCM0299  AC38 PaTu 8988t C80(0.88)  LDD1178  [20]
 LDCM0300  AC39 PaTu 8988t C80(0.82)  LDD1179  [20]
 LDCM0301  AC4 HEK-293T C80(1.02)  LDD1540  [19]
 LDCM0302  AC40 PaTu 8988t C80(0.86)  LDD1181  [20]
 LDCM0303  AC41 PaTu 8988t C80(0.91)  LDD1182  [20]
 LDCM0304  AC42 PaTu 8988t C80(0.88)  LDD1183  [20]
 LDCM0305  AC43 PaTu 8988t C80(0.94)  LDD1184  [20]
 LDCM0306  AC44 PaTu 8988t C80(0.88)  LDD1185  [20]
 LDCM0307  AC45 PaTu 8988t C80(0.84)  LDD1186  [20]
 LDCM0308  AC46 PaTu 8988t C80(0.91)  LDD1187  [20]
 LDCM0309  AC47 PaTu 8988t C80(0.93)  LDD1188  [20]
 LDCM0310  AC48 PaTu 8988t C80(0.82)  LDD1189  [20]
 LDCM0311  AC49 PaTu 8988t C80(0.92)  LDD1190  [20]
 LDCM0312  AC5 HEK-293T C80(0.98)  LDD1551  [19]
 LDCM0313  AC50 PaTu 8988t C80(0.92)  LDD1192  [20]
 LDCM0314  AC51 PaTu 8988t C80(0.93)  LDD1193  [20]
 LDCM0315  AC52 PaTu 8988t C80(1.02)  LDD1194  [20]
 LDCM0316  AC53 PaTu 8988t C80(1.04)  LDD1195  [20]
 LDCM0317  AC54 PaTu 8988t C80(1.11)  LDD1196  [20]
 LDCM0318  AC55 PaTu 8988t C80(0.82)  LDD1197  [20]
 LDCM0319  AC56 PaTu 8988t C80(0.97)  LDD1198  [20]
 LDCM0320  AC57 HEK-293T C80(0.87)  LDD1559  [19]
 LDCM0321  AC58 HEK-293T C80(0.90)  LDD1560  [19]
 LDCM0322  AC59 HEK-293T C80(1.00)  LDD1561  [19]
 LDCM0323  AC6 PaTu 8988t C80(1.02)  LDD1202  [20]
 LDCM0324  AC60 HEK-293T C80(0.97)  LDD1563  [19]
 LDCM0325  AC61 HEK-293T C80(0.92)  LDD1564  [19]
 LDCM0326  AC62 HEK-293T C80(0.98)  LDD1565  [19]
 LDCM0327  AC63 HEK-293T C80(0.94)  LDD1566  [19]
 LDCM0328  AC64 HEK-293T C80(0.96)  LDD1567  [19]
 LDCM0334  AC7 PaTu 8988t C80(0.95)  LDD1213  [20]
 LDCM0345  AC8 PaTu 8988t C80(1.02)  LDD1224  [20]
 LDCM0248  AKOS034007472 PaTu 8988t C80(1.18)  LDD1127  [20]
 LDCM0356  AKOS034007680 PaTu 8988t C80(0.94)  LDD1235  [20]
 LDCM0275  AKOS034007705 PaTu 8988t C80(1.04)  LDD1154  [20]
 LDCM0156  Aniline NCI-H1299 11.60  LDD0403  [2]
 LDCM0367  CL1 PaTu 8988t C80(1.42)  LDD1246  [20]
 LDCM0368  CL10 PaTu 8988t C80(1.19)  LDD1247  [20]
 LDCM0369  CL100 HEK-293T C80(1.06)  LDD1573  [19]
 LDCM0370  CL101 PaTu 8988t C80(0.97)  LDD1249  [20]
 LDCM0371  CL102 PaTu 8988t C80(1.07)  LDD1250  [20]
 LDCM0372  CL103 PaTu 8988t C80(1.18)  LDD1251  [20]
 LDCM0373  CL104 PaTu 8988t C80(1.02)  LDD1252  [20]
 LDCM0374  CL105 HEK-293T C80(1.02)  LDD1578  [19]
 LDCM0376  CL107 HEK-293T C80(1.09)  LDD1580  [19]
 LDCM0377  CL108 HEK-293T C80(1.03)  LDD1581  [19]
 LDCM0378  CL109 HEK-293T C80(1.01)  LDD1582  [19]
 LDCM0379  CL11 PaTu 8988t C80(0.95)  LDD1258  [20]
 LDCM0381  CL111 HEK-293T C80(1.16)  LDD1585  [19]
 LDCM0382  CL112 PaTu 8988t C80(0.99)  LDD1261  [20]
 LDCM0383  CL113 PaTu 8988t C80(1.17)  LDD1262  [20]
 LDCM0384  CL114 PaTu 8988t C80(1.01)  LDD1263  [20]
 LDCM0385  CL115 PaTu 8988t C80(1.08)  LDD1264  [20]
 LDCM0386  CL116 PaTu 8988t C80(0.84)  LDD1265  [20]
 LDCM0387  CL117 PaTu 8988t C80(0.94)  LDD1266  [20]
 LDCM0388  CL118 PaTu 8988t C80(0.86)  LDD1267  [20]
 LDCM0389  CL119 PaTu 8988t C80(0.81)  LDD1268  [20]
 LDCM0390  CL12 PaTu 8988t C80(1.25)  LDD1269  [20]
 LDCM0391  CL120 PaTu 8988t C80(0.81)  LDD1270  [20]
 LDCM0392  CL121 PaTu 8988t C80(0.93)  LDD1271  [20]
 LDCM0393  CL122 PaTu 8988t C80(1.00)  LDD1272  [20]
 LDCM0394  CL123 PaTu 8988t C80(0.94)  LDD1273  [20]
 LDCM0395  CL124 PaTu 8988t C80(1.04)  LDD1274  [20]
 LDCM0396  CL125 HEK-293T C80(1.12)  LDD1600  [19]
 LDCM0398  CL127 HEK-293T C80(1.15)  LDD1602  [19]
 LDCM0399  CL128 HEK-293T C80(1.05)  LDD1603  [19]
 LDCM0400  CL13 PaTu 8988t C80(2.05)  LDD1279  [20]
 LDCM0401  CL14 PaTu 8988t C80(1.47)  LDD1280  [20]
 LDCM0402  CL15 PaTu 8988t C80(1.21)  LDD1281  [20]
 LDCM0403  CL16 PaTu 8988t C80(0.99)  LDD1282  [20]
 LDCM0404  CL17 PaTu 8988t C80(0.91)  LDD1283  [20]
 LDCM0405  CL18 PaTu 8988t C80(1.05)  LDD1284  [20]
 LDCM0406  CL19 PaTu 8988t C80(1.05)  LDD1285  [20]
 LDCM0407  CL2 PaTu 8988t C80(1.51)  LDD1286  [20]
 LDCM0408  CL20 PaTu 8988t C80(0.98)  LDD1287  [20]
 LDCM0409  CL21 PaTu 8988t C80(0.96)  LDD1288  [20]
 LDCM0410  CL22 PaTu 8988t C80(1.05)  LDD1289  [20]
 LDCM0411  CL23 PaTu 8988t C80(1.01)  LDD1290  [20]
 LDCM0412  CL24 PaTu 8988t C80(1.12)  LDD1291  [20]
 LDCM0413  CL25 PaTu 8988t C80(0.89)  LDD1292  [20]
 LDCM0414  CL26 PaTu 8988t C80(0.88)  LDD1293  [20]
 LDCM0415  CL27 PaTu 8988t C80(1.01)  LDD1294  [20]
 LDCM0416  CL28 PaTu 8988t C80(1.19)  LDD1295  [20]
 LDCM0417  CL29 PaTu 8988t C80(1.01)  LDD1296  [20]
 LDCM0418  CL3 PaTu 8988t C80(1.55)  LDD1297  [20]
 LDCM0419  CL30 PaTu 8988t C80(0.99)  LDD1298  [20]
 LDCM0420  CL31 PaTu 8988t C80(1.17)  LDD1299  [20]
 LDCM0421  CL32 PaTu 8988t C80(1.24)  LDD1300  [20]
 LDCM0422  CL33 PaTu 8988t C80(1.08)  LDD1301  [20]
 LDCM0423  CL34 PaTu 8988t C80(1.08)  LDD1302  [20]
 LDCM0424  CL35 PaTu 8988t C80(1.18)  LDD1303  [20]
 LDCM0425  CL36 PaTu 8988t C80(0.72)  LDD1304  [20]
 LDCM0426  CL37 PaTu 8988t C80(1.18)  LDD1305  [20]
 LDCM0428  CL39 PaTu 8988t C80(1.02)  LDD1307  [20]
 LDCM0429  CL4 PaTu 8988t C80(1.31)  LDD1308  [20]
 LDCM0430  CL40 PaTu 8988t C80(1.09)  LDD1309  [20]
 LDCM0431  CL41 PaTu 8988t C80(1.15)  LDD1310  [20]
 LDCM0432  CL42 PaTu 8988t C80(1.20)  LDD1311  [20]
 LDCM0433  CL43 PaTu 8988t C80(1.32)  LDD1312  [20]
 LDCM0434  CL44 PaTu 8988t C80(1.18)  LDD1313  [20]
 LDCM0435  CL45 PaTu 8988t C80(1.03)  LDD1314  [20]
 LDCM0436  CL46 PaTu 8988t C80(0.95)  LDD1315  [20]
 LDCM0437  CL47 PaTu 8988t C80(1.04)  LDD1316  [20]
 LDCM0438  CL48 PaTu 8988t C80(0.92)  LDD1317  [20]
 LDCM0439  CL49 PaTu 8988t C80(1.07)  LDD1318  [20]
 LDCM0440  CL5 PaTu 8988t C80(1.69)  LDD1319  [20]
 LDCM0441  CL50 PaTu 8988t C80(0.97)  LDD1320  [20]
 LDCM0442  CL51 PaTu 8988t C80(0.97)  LDD1321  [20]
 LDCM0443  CL52 PaTu 8988t C80(1.06)  LDD1322  [20]
 LDCM0444  CL53 PaTu 8988t C80(1.13)  LDD1323  [20]
 LDCM0445  CL54 PaTu 8988t C80(1.00)  LDD1324  [20]
 LDCM0446  CL55 PaTu 8988t C80(1.01)  LDD1325  [20]
 LDCM0447  CL56 PaTu 8988t C80(0.81)  LDD1326  [20]
 LDCM0448  CL57 PaTu 8988t C80(1.16)  LDD1327  [20]
 LDCM0449  CL58 PaTu 8988t C80(0.88)  LDD1328  [20]
 LDCM0450  CL59 PaTu 8988t C80(1.08)  LDD1329  [20]
 LDCM0451  CL6 PaTu 8988t C80(1.54)  LDD1330  [20]
 LDCM0452  CL60 PaTu 8988t C80(1.03)  LDD1331  [20]
 LDCM0453  CL61 PaTu 8988t C80(1.07)  LDD1332  [20]
 LDCM0454  CL62 PaTu 8988t C80(0.82)  LDD1333  [20]
 LDCM0455  CL63 PaTu 8988t C80(0.97)  LDD1334  [20]
 LDCM0456  CL64 PaTu 8988t C80(0.90)  LDD1335  [20]
 LDCM0457  CL65 PaTu 8988t C80(1.09)  LDD1336  [20]
 LDCM0458  CL66 PaTu 8988t C80(1.21)  LDD1337  [20]
 LDCM0459  CL67 PaTu 8988t C80(1.17)  LDD1338  [20]
 LDCM0460  CL68 PaTu 8988t C80(0.88)  LDD1339  [20]
 LDCM0461  CL69 PaTu 8988t C80(1.07)  LDD1340  [20]
 LDCM0462  CL7 PaTu 8988t C80(1.64)  LDD1341  [20]
 LDCM0463  CL70 PaTu 8988t C80(1.03)  LDD1342  [20]
 LDCM0464  CL71 PaTu 8988t C80(1.10)  LDD1343  [20]
 LDCM0465  CL72 PaTu 8988t C80(1.05)  LDD1344  [20]
 LDCM0466  CL73 PaTu 8988t C80(0.93)  LDD1345  [20]
 LDCM0467  CL74 PaTu 8988t C80(0.99)  LDD1346  [20]
 LDCM0469  CL76 HEK-293T C80(1.04)  LDD1672  [19]
 LDCM0470  CL77 HEK-293T C80(0.90)  LDD1673  [19]
 LDCM0471  CL78 HEK-293T C80(1.02)  LDD1674  [19]
 LDCM0472  CL79 HEK-293T C80(1.08)  LDD1675  [19]
 LDCM0473  CL8 PaTu 8988t C80(1.34)  LDD1352  [20]
 LDCM0474  CL80 HEK-293T C80(1.17)  LDD1677  [19]
 LDCM0475  CL81 HEK-293T C80(1.00)  LDD1678  [19]
 LDCM0476  CL82 HEK-293T C80(1.12)  LDD1679  [19]
 LDCM0477  CL83 HEK-293T C80(1.07)  LDD1680  [19]
 LDCM0478  CL84 HEK-293T C80(1.11)  LDD1681  [19]
 LDCM0479  CL85 HEK-293T C80(1.07)  LDD1682  [19]
 LDCM0481  CL87 HEK-293T C80(1.05)  LDD1684  [19]
 LDCM0482  CL88 HEK-293T C80(0.95)  LDD1685  [19]
 LDCM0483  CL89 HEK-293T C80(0.85)  LDD1686  [19]
 LDCM0484  CL9 PaTu 8988t C80(1.46)  LDD1363  [20]
 LDCM0485  CL90 HEK-293T C80(0.89)  LDD1688  [19]
 LDCM0486  CL91 HEK-293T C80(1.02)  LDD1689  [19]
 LDCM0487  CL92 HEK-293T C80(0.99)  LDD1690  [19]
 LDCM0488  CL93 HEK-293T C80(0.96)  LDD1691  [19]
 LDCM0489  CL94 HEK-293T C80(1.11)  LDD1692  [19]
 LDCM0490  CL95 HEK-293T C80(1.04)  LDD1693  [19]
 LDCM0491  CL96 HEK-293T C80(0.95)  LDD1694  [19]
 LDCM0492  CL97 HEK-293T C80(1.04)  LDD1695  [19]
 LDCM0494  CL99 HEK-293T C80(0.97)  LDD1697  [19]
 LDCM0495  E2913 HEK-293T C80(1.03)  LDD1698  [19]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C80(1.75)  LDD1702  [7]
 LDCM0625  F8 Ramos C80(1.94)  LDD2187  [21]
 LDCM0572  Fragment10 Ramos C80(0.74)  LDD2189  [21]
 LDCM0573  Fragment11 Ramos C80(5.08)  LDD2190  [21]
 LDCM0574  Fragment12 Ramos C80(1.04)  LDD2191  [21]
 LDCM0575  Fragment13 Ramos C80(1.59)  LDD2192  [21]
 LDCM0576  Fragment14 Ramos C80(0.80)  LDD2193  [21]
 LDCM0579  Fragment20 Ramos C80(0.73)  LDD2194  [21]
 LDCM0580  Fragment21 Ramos C80(0.98)  LDD2195  [21]
 LDCM0582  Fragment23 Ramos C80(0.85)  LDD2196  [21]
 LDCM0578  Fragment27 Ramos C80(1.20)  LDD2197  [21]
 LDCM0586  Fragment28 Ramos C80(0.75)  LDD2198  [21]
 LDCM0588  Fragment30 Ramos C80(1.00)  LDD2199  [21]
 LDCM0589  Fragment31 Ramos C80(1.21)  LDD2200  [21]
 LDCM0590  Fragment32 Ramos C80(1.37)  LDD2201  [21]
 LDCM0468  Fragment33 PaTu 8988t C80(1.08)  LDD1347  [20]
 LDCM0596  Fragment38 Ramos C80(1.26)  LDD2203  [21]
 LDCM0566  Fragment4 Ramos C80(0.84)  LDD2184  [21]
 LDCM0427  Fragment51 PaTu 8988t C80(1.04)  LDD1306  [20]
 LDCM0610  Fragment52 Ramos C80(1.58)  LDD2204  [21]
 LDCM0614  Fragment56 Ramos C80(1.59)  LDD2205  [21]
 LDCM0569  Fragment7 Ramos C80(0.97)  LDD2186  [21]
 LDCM0571  Fragment9 Ramos C80(0.73)  LDD2188  [21]
 LDCM0022  KB02 HEK-293T C80(1.06)  LDD1492  [19]
 LDCM0023  KB03 HEK-293T C80(1.00)  LDD1497  [19]
 LDCM0024  KB05 MKN-1 C80(1.49)  LDD3331  [5]
 LDCM0003  Sulforaphane MDA-MB-231 3.71  LDD0160  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Peroxiredoxin-1 (PRDX1) Peroxiredoxin family Q06830
RAC-alpha serine/threonine-protein kinase (AKT1) AGC Ser/Thr protein kinase family P31749
Serine/threonine-protein kinase 3 (STK3) STE Ser/Thr protein kinase family Q13188
Serine/threonine-protein kinase 4 (STK4) STE Ser/Thr protein kinase family Q13043
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Gamma-aminobutyric acid receptor-associated protein (GABARAP) ATG8 family O95166
Other
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Gamma-aminobutyric acid receptor-associated protein-like 1 (GABARAPL1) ATG8 family Q9H0R8
Gamma-aminobutyric acid receptor-associated protein-like 2 (GABARAPL2) ATG8 family P60520
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) ATG8 family Q9GZQ8
DNA damage-inducible transcript 4-like protein (DDIT4L) DDIT4 family Q96D03
MOB kinase activator 1A (MOB1A) MOB1/phocein family Q9H8S9
MOB kinase activator 1B (MOB1B) MOB1/phocein family Q7L9L4
Sarcolemmal membrane-associated protein (SLMAP) SLMAP family Q14BN4
PRKCA-binding protein (PICK1) . Q9NRD5
Protein salvador homolog 1 (SAV1) . Q9H4B6
Ras association domain-containing protein 2 (RASSF2) . P50749
Ras association domain-containing protein 3 (RASSF3) . Q86WH2
Ras association domain-containing protein 4 (RASSF4) . Q9H2L5
Ras association domain-containing protein 5 (RASSF5) . Q8WWW0
Ras association domain-containing protein 6 (RASSF6) . Q6ZTQ3

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tat-120 . D0A7HY

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 Design and synthesis of tailored human caseinolytic protease P inhibitors. Chem Commun (Camb). 2018 Aug 28;54(70):9833-9836. doi: 10.1039/c8cc05265d.
Mass spectrometry data entry: PXD010277
4 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
5 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
6 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
7 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
8 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
9 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
10 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
11 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
12 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
13 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
14 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
15 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.
16 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
17 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
18 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
19 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
20 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
21 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578