General Information of Target

Target ID LDTP05525
Target Name KH domain-containing, RNA-binding, signal transduction-associated protein 1 (KHDRBS1)
Gene Name KHDRBS1
Gene ID 10657
Synonyms
SAM68; KH domain-containing, RNA-binding, signal transduction-associated protein 1; GAP-associated tyrosine phosphoprotein p62; Src-associated in mitosis 68 kDa protein; Sam68; p21 Ras GTPase-activating protein-associated p62; p68
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQRRDDPAARMSRSSGRSGSMDPSGAHPSVRQTPSRQPPLPHRSRGGGGGSRGGARASPA
TQPPPLLPPSATGPDATVGGPAPTPLLPPSATASVKMEPENKYLPELMAEKDSLDPSFTH
AMQLLTAEIEKIQKGDSKKDDEENYLDLFSHKNMKLKERVLIPVKQYPKFNFVGKILGPQ
GNTIKRLQEETGAKISVLGKGSMRDKAKEEELRKGGDPKYAHLNMDLHVFIEVFGPPCEA
YALMAHAMEEVKKFLVPDMMDDICQEQFLELSYLNGVPEPSRGRGVPVRGRGAAPPPPPV
PRGRGVGPPRGALVRGTPVRGAITRGATVTRGVPPPPTVRGAPAPRARTAGIQRIPLPPP
PAPETYEEYGYDDTYAEQSYEGYEGYYSQSQGDSEYYDYGHGEVQDSYEAYGQDDWNGTR
PSLKAPPARPVKGAYREHPYGRY
Target Type
Literature-reported
Target Bioclass
Other
Family
KHDRBS family
Subcellular location
Nucleus
Function
Recruited and tyrosine phosphorylated by several receptor systems, for example the T-cell, leptin and insulin receptors. Once phosphorylated, functions as an adapter protein in signal transduction cascades by binding to SH2 and SH3 domain-containing proteins. Role in G2-M progression in the cell cycle. Represses CBP-dependent transcriptional activation apparently by competing with other nuclear factors for binding to CBP. Also acts as a putative regulator of mRNA stability and/or translation rates and mediates mRNA nuclear export. Positively regulates the association of constitutive transport element (CTE)-containing mRNA with large polyribosomes and translation initiation. According to some authors, is not involved in the nucleocytoplasmic export of unspliced (CTE)-containing RNA species according to. RNA-binding protein that plays a role in the regulation of alternative splicing and influences mRNA splice site selection and exon inclusion. Binds to RNA containing 5'-[AU]UAA-3' as a bipartite motif spaced by more than 15 nucleotides. Binds poly(A). Can regulate CD44 alternative splicing in a Ras pathway-dependent manner. In cooperation with HNRNPA1 modulates alternative splicing of BCL2L1 by promoting splicing toward isoform Bcl-X(S), and of SMN1. Can regulate alternative splicing of NRXN1 and NRXN3 in the laminin G-like domain 6 containing the evolutionary conserved neurexin alternative spliced segment 4 (AS4) involved in neurexin selective targeting to postsynaptic partners. In a neuronal activity-dependent manner cooperates synergistically with KHDRBS2/SLIM-1 in regulation of NRXN1 exon skipping at AS4. The cooperation with KHDRBS2/SLIM-1 is antagonistic for regulation of NXRN3 alternative splicing at AS4.; Isoform 3, which is expressed in growth-arrested cells only, inhibits S phase.
TTD ID
T80395
Uniprot ID
Q07666
DrugMap ID
TTAT6C7
Ensemble ID
ENST00000327300.12
HGNC ID
HGNC:18116

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAMA1 SNV: p.E403K .
CCK81 Deletion: p.S90RfsTer36 .
EFO27 Deletion: p.P336HfsTer4 .
GB1 SNV: p.R282C .
JURKAT SNV: p.R348Q; p.R348W .
KNS42 SNV: p.R315C DBIA    Probe Info 
OVCAR4 SNV: p.M11V .
SW403 SNV: p.K424N .
WM115 SNV: p.P426L .
WM2664 SNV: p.P426L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 38 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
15.00  LDD0402  [1]
P2
 Probe Info 
10.00  LDD0449  [2]
P3
 Probe Info 
10.00  LDD0450  [2]
P8
 Probe Info 
1.53  LDD0451  [2]
A-EBA
 Probe Info 
3.07  LDD0215  [3]
CY-1
 Probe Info 
100.00  LDD0243  [4]
CY4
 Probe Info 
100.00  LDD0244  [4]
N1
 Probe Info 
100.00  LDD0242  [4]
W1
 Probe Info 
26.50  LDD0235  [5]
TH211
 Probe Info 
Y145(20.00); Y435(16.56); Y440(10.88)  LDD0257  [6]
TH214
 Probe Info 
Y145(20.00); Y435(5.22)  LDD0258  [6]
TH216
 Probe Info 
Y145(20.00); Y435(20.00)  LDD0259  [6]
YN-1
 Probe Info 
100.00  LDD0444  [7]
ONAyne
 Probe Info 
K169(10.00); K424(10.00)  LDD0275  [8]
Probe 1
 Probe Info 
Y145(24.43); Y435(17.67)  LDD3495  [9]
DBIA
 Probe Info 
C264(1.58)  LDD3323  [10]
AHL-Pu-1
 Probe Info 
C264(2.96)  LDD0168  [11]
Alkyne-RA190
 Probe Info 
2.81  LDD0300  [12]
HHS-475
 Probe Info 
Y435(0.85); Y103(1.00)  LDD0264  [13]
HHS-465
 Probe Info 
Y435(10.00)  LDD2237  [14]
5E-2FA
 Probe Info 
H151(0.00); H27(0.00)  LDD2235  [15]
ATP probe
 Probe Info 
K165(0.00); K194(0.00); K152(0.00); K155(0.00)  LDD0199  [16]
4-Iodoacetamidophenylacetylene
 Probe Info 
N.A.  LDD0038  [17]
IA-alkyne
 Probe Info 
N.A.  LDD0036  [17]
Lodoacetamide azide
 Probe Info 
N.A.  LDD0037  [17]
ATP probe
 Probe Info 
N.A.  LDD0035  [18]
NAIA_4
 Probe Info 
N.A.  LDD2226  [19]
1d-yne
 Probe Info 
N.A.  LDD0356  [20]
IPM
 Probe Info 
N.A.  LDD2156  [21]
NHS
 Probe Info 
K139(0.00); K165(0.00); K175(0.00); K102(0.00)  LDD0010  [22]
SF
 Probe Info 
K206(0.00); K432(0.00); Y103(0.00); Y167(0.00)  LDD0028  [23]
STPyne
 Probe Info 
K169(0.00); K194(0.00)  LDD0009  [22]
1c-yne
 Probe Info 
K152(0.00); K102(0.00); K175(0.00); K111(0.00)  LDD0228  [20]
Acrolein
 Probe Info 
H120(0.00); H151(0.00); H27(0.00)  LDD0217  [24]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [24]
AOyne
 Probe Info 
7.50  LDD0443  [25]
NAIA_5
 Probe Info 
N.A.  LDD2223  [19]
HHS-482
 Probe Info 
Y103(1.95); Y435(0.77); Y440(0.76)  LDD2239  [14]
PAL-AfBPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C165
 Probe Info 
12.82  LDD1845  [26]
C191
 Probe Info 
10.70  LDD1868  [26]
C232
 Probe Info 
39.12  LDD1905  [26]
C338
 Probe Info 
14.12  LDD2001  [26]
FFF probe11
 Probe Info 
7.96  LDD0471  [27]
FFF probe13
 Probe Info 
15.91  LDD0475  [27]
FFF probe14
 Probe Info 
14.57  LDD0477  [27]
FFF probe2
 Probe Info 
11.68  LDD0463  [27]
FFF probe3
 Probe Info 
13.98  LDD0464  [27]
FFF probe6
 Probe Info 
10.00  LDD0482  [27]
JN0003
 Probe Info 
12.44  LDD0469  [27]
STS-2
 Probe Info 
1.00  LDD0139  [28]
VE-P
 Probe Info 
N.A.  LDD0396  [29]
OEA-DA
 Probe Info 
3.61  LDD0046  [30]
STS-1
 Probe Info 
N.A.  LDD0068  [31]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C264(2.96)  LDD0168  [11]
 LDCM0026  4SU-RNA+native RNA HEK-293T C264(6.03)  LDD0169  [11]
 LDCM0214  AC1 PaTu 8988t C264(2.06)  LDD1093  [32]
 LDCM0215  AC10 PaTu 8988t C264(1.62)  LDD1094  [32]
 LDCM0216  AC100 PaTu 8988t C264(1.40)  LDD1095  [32]
 LDCM0217  AC101 PaTu 8988t C264(1.08)  LDD1096  [32]
 LDCM0218  AC102 PaTu 8988t C264(1.17)  LDD1097  [32]
 LDCM0219  AC103 PaTu 8988t C264(1.40)  LDD1098  [32]
 LDCM0220  AC104 PaTu 8988t C264(0.91)  LDD1099  [32]
 LDCM0221  AC105 PaTu 8988t C264(0.98)  LDD1100  [32]
 LDCM0222  AC106 PaTu 8988t C264(1.12)  LDD1101  [32]
 LDCM0223  AC107 PaTu 8988t C264(1.13)  LDD1102  [32]
 LDCM0224  AC108 PaTu 8988t C264(1.11)  LDD1103  [32]
 LDCM0225  AC109 PaTu 8988t C264(1.61)  LDD1104  [32]
 LDCM0226  AC11 PaTu 8988t C264(0.99)  LDD1105  [32]
 LDCM0227  AC110 PaTu 8988t C264(1.45)  LDD1106  [32]
 LDCM0228  AC111 PaTu 8988t C264(1.15)  LDD1107  [32]
 LDCM0229  AC112 PaTu 8988t C264(1.16)  LDD1108  [32]
 LDCM0230  AC113 PaTu 8988t C264(0.66)  LDD1109  [32]
 LDCM0231  AC114 PaTu 8988t C264(0.60)  LDD1110  [32]
 LDCM0232  AC115 PaTu 8988t C264(0.61)  LDD1111  [32]
 LDCM0233  AC116 PaTu 8988t C264(0.68)  LDD1112  [32]
 LDCM0234  AC117 PaTu 8988t C264(0.90)  LDD1113  [32]
 LDCM0235  AC118 PaTu 8988t C264(0.72)  LDD1114  [32]
 LDCM0236  AC119 PaTu 8988t C264(0.56)  LDD1115  [32]
 LDCM0237  AC12 PaTu 8988t C264(1.10)  LDD1116  [32]
 LDCM0238  AC120 PaTu 8988t C264(0.60)  LDD1117  [32]
 LDCM0239  AC121 PaTu 8988t C264(0.58)  LDD1118  [32]
 LDCM0240  AC122 PaTu 8988t C264(0.60)  LDD1119  [32]
 LDCM0241  AC123 PaTu 8988t C264(0.61)  LDD1120  [32]
 LDCM0242  AC124 PaTu 8988t C264(0.68)  LDD1121  [32]
 LDCM0243  AC125 PaTu 8988t C264(0.85)  LDD1122  [32]
 LDCM0244  AC126 PaTu 8988t C264(0.95)  LDD1123  [32]
 LDCM0245  AC127 PaTu 8988t C264(0.69)  LDD1124  [32]
 LDCM0246  AC128 PaTu 8988t C264(1.43)  LDD1125  [32]
 LDCM0247  AC129 PaTu 8988t C264(1.03)  LDD1126  [32]
 LDCM0249  AC130 PaTu 8988t C264(0.90)  LDD1128  [32]
 LDCM0250  AC131 PaTu 8988t C264(0.98)  LDD1129  [32]
 LDCM0251  AC132 PaTu 8988t C264(1.46)  LDD1130  [32]
 LDCM0252  AC133 PaTu 8988t C264(1.40)  LDD1131  [32]
 LDCM0253  AC134 PaTu 8988t C264(1.21)  LDD1132  [32]
 LDCM0254  AC135 PaTu 8988t C264(1.04)  LDD1133  [32]
 LDCM0255  AC136 PaTu 8988t C264(1.23)  LDD1134  [32]
 LDCM0256  AC137 PaTu 8988t C264(1.09)  LDD1135  [32]
 LDCM0257  AC138 PaTu 8988t C264(1.13)  LDD1136  [32]
 LDCM0258  AC139 PaTu 8988t C264(0.94)  LDD1137  [32]
 LDCM0259  AC14 PaTu 8988t C264(0.86)  LDD1138  [32]
 LDCM0260  AC140 PaTu 8988t C264(1.48)  LDD1139  [32]
 LDCM0261  AC141 PaTu 8988t C264(1.29)  LDD1140  [32]
 LDCM0262  AC142 PaTu 8988t C264(1.56)  LDD1141  [32]
 LDCM0270  AC15 PaTu 8988t C264(0.86)  LDD1149  [32]
 LDCM0276  AC17 HEK-293T C264(0.91)  LDD1515  [33]
 LDCM0277  AC18 HEK-293T C264(0.92); C238(0.92)  LDD1516  [33]
 LDCM0278  AC19 HEK-293T C264(0.94); C238(0.79)  LDD1517  [33]
 LDCM0279  AC2 PaTu 8988t C264(2.02)  LDD1158  [32]
 LDCM0280  AC20 HEK-293T C264(1.01); C238(1.01)  LDD1519  [33]
 LDCM0281  AC21 HEK-293T C264(1.00); C238(1.01)  LDD1520  [33]
 LDCM0282  AC22 HEK-293T C264(1.18); C238(1.14)  LDD1521  [33]
 LDCM0283  AC23 HEK-293T C264(0.94); C238(0.98)  LDD1522  [33]
 LDCM0284  AC24 HEK-293T C264(0.96)  LDD1523  [33]
 LDCM0285  AC25 PaTu 8988t C264(0.79)  LDD1164  [32]
 LDCM0286  AC26 PaTu 8988t C264(1.26)  LDD1165  [32]
 LDCM0287  AC27 PaTu 8988t C264(1.11)  LDD1166  [32]
 LDCM0288  AC28 PaTu 8988t C264(1.27)  LDD1167  [32]
 LDCM0289  AC29 PaTu 8988t C264(1.15)  LDD1168  [32]
 LDCM0290  AC3 PaTu 8988t C264(1.17)  LDD1169  [32]
 LDCM0291  AC30 PaTu 8988t C264(1.03)  LDD1170  [32]
 LDCM0292  AC31 PaTu 8988t C264(0.79)  LDD1171  [32]
 LDCM0293  AC32 PaTu 8988t C264(1.28)  LDD1172  [32]
 LDCM0294  AC33 PaTu 8988t C264(1.17)  LDD1173  [32]
 LDCM0295  AC34 PaTu 8988t C264(1.35)  LDD1174  [32]
 LDCM0296  AC35 PaTu 8988t C264(1.18)  LDD1175  [32]
 LDCM0297  AC36 PaTu 8988t C264(1.56)  LDD1176  [32]
 LDCM0298  AC37 PaTu 8988t C264(1.66)  LDD1177  [32]
 LDCM0299  AC38 PaTu 8988t C264(1.64)  LDD1178  [32]
 LDCM0300  AC39 PaTu 8988t C264(1.78)  LDD1179  [32]
 LDCM0301  AC4 PaTu 8988t C264(0.88)  LDD1180  [32]
 LDCM0302  AC40 PaTu 8988t C264(2.18)  LDD1181  [32]
 LDCM0303  AC41 PaTu 8988t C264(1.54)  LDD1182  [32]
 LDCM0304  AC42 PaTu 8988t C264(1.90)  LDD1183  [32]
 LDCM0305  AC43 PaTu 8988t C264(1.33)  LDD1184  [32]
 LDCM0306  AC44 PaTu 8988t C264(2.41)  LDD1185  [32]
 LDCM0307  AC45 PaTu 8988t C264(1.90)  LDD1186  [32]
 LDCM0308  AC46 PaTu 8988t C264(1.02)  LDD1187  [32]
 LDCM0309  AC47 PaTu 8988t C264(1.03)  LDD1188  [32]
 LDCM0310  AC48 PaTu 8988t C264(1.23)  LDD1189  [32]
 LDCM0311  AC49 PaTu 8988t C264(1.03)  LDD1190  [32]
 LDCM0312  AC5 PaTu 8988t C264(1.76)  LDD1191  [32]
 LDCM0313  AC50 PaTu 8988t C264(1.21)  LDD1192  [32]
 LDCM0314  AC51 PaTu 8988t C264(0.98)  LDD1193  [32]
 LDCM0315  AC52 PaTu 8988t C264(1.32)  LDD1194  [32]
 LDCM0316  AC53 PaTu 8988t C264(1.29)  LDD1195  [32]
 LDCM0317  AC54 PaTu 8988t C264(1.64)  LDD1196  [32]
 LDCM0318  AC55 PaTu 8988t C264(0.95)  LDD1197  [32]
 LDCM0319  AC56 PaTu 8988t C264(1.25)  LDD1198  [32]
 LDCM0320  AC57 PaTu 8988t C264(1.09)  LDD1199  [32]
 LDCM0321  AC58 PaTu 8988t C264(0.93)  LDD1200  [32]
 LDCM0322  AC59 PaTu 8988t C264(0.82)  LDD1201  [32]
 LDCM0323  AC6 PaTu 8988t C264(1.11)  LDD1202  [32]
 LDCM0324  AC60 PaTu 8988t C264(0.84)  LDD1203  [32]
 LDCM0325  AC61 PaTu 8988t C264(1.25)  LDD1204  [32]
 LDCM0326  AC62 PaTu 8988t C264(0.96)  LDD1205  [32]
 LDCM0327  AC63 PaTu 8988t C264(1.19)  LDD1206  [32]
 LDCM0328  AC64 PaTu 8988t C264(1.09)  LDD1207  [32]
 LDCM0329  AC65 PaTu 8988t C264(0.89)  LDD1208  [32]
 LDCM0330  AC66 PaTu 8988t C264(0.89)  LDD1209  [32]
 LDCM0331  AC67 PaTu 8988t C264(1.09)  LDD1210  [32]
 LDCM0332  AC68 PaTu 8988t C264(1.69)  LDD1211  [32]
 LDCM0333  AC69 PaTu 8988t C264(1.04)  LDD1212  [32]
 LDCM0334  AC7 PaTu 8988t C264(1.11)  LDD1213  [32]
 LDCM0335  AC70 PaTu 8988t C264(0.73)  LDD1214  [32]
 LDCM0336  AC71 PaTu 8988t C264(1.60)  LDD1215  [32]
 LDCM0337  AC72 PaTu 8988t C264(0.86)  LDD1216  [32]
 LDCM0338  AC73 PaTu 8988t C264(0.60)  LDD1217  [32]
 LDCM0339  AC74 PaTu 8988t C264(1.39)  LDD1218  [32]
 LDCM0340  AC75 PaTu 8988t C264(1.63)  LDD1219  [32]
 LDCM0341  AC76 PaTu 8988t C264(0.80)  LDD1220  [32]
 LDCM0342  AC77 PaTu 8988t C264(1.71)  LDD1221  [32]
 LDCM0343  AC78 PaTu 8988t C264(1.07)  LDD1222  [32]
 LDCM0344  AC79 PaTu 8988t C264(0.90)  LDD1223  [32]
 LDCM0345  AC8 PaTu 8988t C264(0.73)  LDD1224  [32]
 LDCM0346  AC80 PaTu 8988t C264(0.85)  LDD1225  [32]
 LDCM0347  AC81 PaTu 8988t C264(0.89)  LDD1226  [32]
 LDCM0348  AC82 PaTu 8988t C264(1.78)  LDD1227  [32]
 LDCM0365  AC98 PaTu 8988t C264(0.96)  LDD1244  [32]
 LDCM0366  AC99 PaTu 8988t C264(0.98)  LDD1245  [32]
 LDCM0248  AKOS034007472 PaTu 8988t C264(1.02)  LDD1127  [32]
 LDCM0356  AKOS034007680 PaTu 8988t C264(1.28)  LDD1235  [32]
 LDCM0275  AKOS034007705 PaTu 8988t C264(1.19)  LDD1154  [32]
 LDCM0156  Aniline NCI-H1299 12.09  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C264(1.43)  LDD2214  [34]
 LDCM0108  Chloroacetamide HeLa H151(0.00); H27(0.00)  LDD0222  [24]
 LDCM0367  CL1 HEK-293T C264(1.02); C238(0.82)  LDD1571  [33]
 LDCM0368  CL10 HEK-293T C264(1.03); C238(1.02)  LDD1572  [33]
 LDCM0369  CL100 PaTu 8988t C264(1.62)  LDD1248  [32]
 LDCM0370  CL101 PaTu 8988t C264(0.84)  LDD1249  [32]
 LDCM0371  CL102 PaTu 8988t C264(1.43)  LDD1250  [32]
 LDCM0372  CL103 PaTu 8988t C264(1.12)  LDD1251  [32]
 LDCM0373  CL104 PaTu 8988t C264(0.85)  LDD1252  [32]
 LDCM0374  CL105 HEK-293T C264(0.88); C238(0.92)  LDD1578  [33]
 LDCM0375  CL106 HEK-293T C264(0.94)  LDD1579  [33]
 LDCM0376  CL107 HEK-293T C264(0.87); C238(1.04)  LDD1580  [33]
 LDCM0377  CL108 HEK-293T C264(1.01); C238(1.08)  LDD1581  [33]
 LDCM0378  CL109 HEK-293T C264(0.85); C238(0.93)  LDD1582  [33]
 LDCM0379  CL11 HEK-293T C264(0.89); C238(1.03)  LDD1583  [33]
 LDCM0380  CL110 HEK-293T C264(0.99)  LDD1584  [33]
 LDCM0381  CL111 HEK-293T C264(0.90); C238(0.96)  LDD1585  [33]
 LDCM0382  CL112 PaTu 8988t C264(0.85)  LDD1261  [32]
 LDCM0383  CL113 PaTu 8988t C264(0.93)  LDD1262  [32]
 LDCM0384  CL114 PaTu 8988t C264(1.09)  LDD1263  [32]
 LDCM0385  CL115 PaTu 8988t C264(1.01)  LDD1264  [32]
 LDCM0386  CL116 PaTu 8988t C264(1.08)  LDD1265  [32]
 LDCM0387  CL117 PaTu 8988t C264(1.44)  LDD1266  [32]
 LDCM0388  CL118 PaTu 8988t C264(1.41)  LDD1267  [32]
 LDCM0389  CL119 PaTu 8988t C264(1.69)  LDD1268  [32]
 LDCM0390  CL12 HEK-293T C264(0.93)  LDD1594  [33]
 LDCM0391  CL120 PaTu 8988t C264(1.64)  LDD1270  [32]
 LDCM0392  CL121 PaTu 8988t C264(1.04)  LDD1271  [32]
 LDCM0393  CL122 PaTu 8988t C264(1.48)  LDD1272  [32]
 LDCM0394  CL123 PaTu 8988t C264(1.37)  LDD1273  [32]
 LDCM0395  CL124 PaTu 8988t C264(1.11)  LDD1274  [32]
 LDCM0396  CL125 PaTu 8988t C264(0.97)  LDD1275  [32]
 LDCM0397  CL126 PaTu 8988t C264(1.03)  LDD1276  [32]
 LDCM0398  CL127 PaTu 8988t C264(0.94)  LDD1277  [32]
 LDCM0399  CL128 PaTu 8988t C264(1.02)  LDD1278  [32]
 LDCM0400  CL13 HEK-293T C264(0.87); C238(0.91)  LDD1604  [33]
 LDCM0401  CL14 HEK-293T C264(1.05)  LDD1605  [33]
 LDCM0402  CL15 HEK-293T C264(0.90); C238(0.83)  LDD1606  [33]
 LDCM0403  CL16 HEK-293T C264(0.95); C238(1.15)  LDD1607  [33]
 LDCM0404  CL17 HEK-293T C264(0.91)  LDD1608  [33]
 LDCM0405  CL18 HEK-293T C264(1.01); C238(0.99)  LDD1609  [33]
 LDCM0406  CL19 HEK-293T C264(1.02); C238(1.04)  LDD1610  [33]
 LDCM0407  CL2 HEK-293T C264(1.16)  LDD1611  [33]
 LDCM0408  CL20 HEK-293T C264(1.06); C238(0.89)  LDD1612  [33]
 LDCM0409  CL21 HEK-293T C264(0.92); C238(1.11)  LDD1613  [33]
 LDCM0410  CL22 HEK-293T C264(1.11); C238(1.15)  LDD1614  [33]
 LDCM0411  CL23 HEK-293T C264(0.80); C238(1.16)  LDD1615  [33]
 LDCM0412  CL24 HEK-293T C264(0.99)  LDD1616  [33]
 LDCM0413  CL25 HEK-293T C264(0.76); C238(0.85)  LDD1617  [33]
 LDCM0414  CL26 HEK-293T C264(0.93)  LDD1618  [33]
 LDCM0415  CL27 HEK-293T C264(0.91); C238(1.03)  LDD1619  [33]
 LDCM0416  CL28 HEK-293T C264(1.01); C238(1.08)  LDD1620  [33]
 LDCM0417  CL29 HEK-293T C264(1.04)  LDD1621  [33]
 LDCM0418  CL3 HEK-293T C264(1.05); C238(0.92)  LDD1622  [33]
 LDCM0419  CL30 HEK-293T C264(0.95); C238(0.96)  LDD1623  [33]
 LDCM0420  CL31 PaTu 8988t C264(0.90)  LDD1299  [32]
 LDCM0421  CL32 PaTu 8988t C264(0.97)  LDD1300  [32]
 LDCM0422  CL33 PaTu 8988t C264(1.68)  LDD1301  [32]
 LDCM0423  CL34 PaTu 8988t C264(1.35)  LDD1302  [32]
 LDCM0424  CL35 PaTu 8988t C264(1.14)  LDD1303  [32]
 LDCM0425  CL36 PaTu 8988t C264(1.37)  LDD1304  [32]
 LDCM0426  CL37 PaTu 8988t C264(1.74)  LDD1305  [32]
 LDCM0428  CL39 PaTu 8988t C264(1.39)  LDD1307  [32]
 LDCM0429  CL4 HEK-293T C264(0.93); C238(1.04)  LDD1633  [33]
 LDCM0430  CL40 PaTu 8988t C264(0.92)  LDD1309  [32]
 LDCM0431  CL41 PaTu 8988t C264(1.21)  LDD1310  [32]
 LDCM0432  CL42 PaTu 8988t C264(1.48)  LDD1311  [32]
 LDCM0433  CL43 PaTu 8988t C264(2.33)  LDD1312  [32]
 LDCM0434  CL44 PaTu 8988t C264(1.39)  LDD1313  [32]
 LDCM0435  CL45 PaTu 8988t C264(1.11)  LDD1314  [32]
 LDCM0436  CL46 PaTu 8988t C264(1.30)  LDD1315  [32]
 LDCM0437  CL47 PaTu 8988t C264(1.13)  LDD1316  [32]
 LDCM0438  CL48 PaTu 8988t C264(1.12)  LDD1317  [32]
 LDCM0439  CL49 PaTu 8988t C264(1.16)  LDD1318  [32]
 LDCM0440  CL5 HEK-293T C264(1.06)  LDD1644  [33]
 LDCM0441  CL50 PaTu 8988t C264(1.23)  LDD1320  [32]
 LDCM0442  CL51 PaTu 8988t C264(1.34)  LDD1321  [32]
 LDCM0443  CL52 PaTu 8988t C264(1.23)  LDD1322  [32]
 LDCM0444  CL53 PaTu 8988t C264(0.94)  LDD1323  [32]
 LDCM0445  CL54 PaTu 8988t C264(1.13)  LDD1324  [32]
 LDCM0446  CL55 PaTu 8988t C264(1.23)  LDD1325  [32]
 LDCM0447  CL56 PaTu 8988t C264(0.68)  LDD1326  [32]
 LDCM0448  CL57 PaTu 8988t C264(1.69)  LDD1327  [32]
 LDCM0449  CL58 PaTu 8988t C264(1.32)  LDD1328  [32]
 LDCM0450  CL59 PaTu 8988t C264(1.42)  LDD1329  [32]
 LDCM0451  CL6 HEK-293T C264(0.99); C238(0.95)  LDD1654  [33]
 LDCM0452  CL60 PaTu 8988t C264(1.64)  LDD1331  [32]
 LDCM0453  CL61 PaTu 8988t C264(0.43)  LDD1332  [32]
 LDCM0454  CL62 PaTu 8988t C264(0.28)  LDD1333  [32]
 LDCM0455  CL63 PaTu 8988t C264(0.50)  LDD1334  [32]
 LDCM0456  CL64 PaTu 8988t C264(0.58)  LDD1335  [32]
 LDCM0457  CL65 PaTu 8988t C264(0.69)  LDD1336  [32]
 LDCM0458  CL66 PaTu 8988t C264(0.74)  LDD1337  [32]
 LDCM0459  CL67 PaTu 8988t C264(0.74)  LDD1338  [32]
 LDCM0460  CL68 PaTu 8988t C264(1.35)  LDD1339  [32]
 LDCM0461  CL69 PaTu 8988t C264(0.72)  LDD1340  [32]
 LDCM0462  CL7 HEK-293T C264(0.98); C238(1.18)  LDD1665  [33]
 LDCM0463  CL70 PaTu 8988t C264(0.66)  LDD1342  [32]
 LDCM0464  CL71 PaTu 8988t C264(0.42)  LDD1343  [32]
 LDCM0465  CL72 PaTu 8988t C264(0.37)  LDD1344  [32]
 LDCM0466  CL73 PaTu 8988t C264(0.48)  LDD1345  [32]
 LDCM0467  CL74 PaTu 8988t C264(0.57)  LDD1346  [32]
 LDCM0469  CL76 PaTu 8988t C264(0.92)  LDD1348  [32]
 LDCM0470  CL77 PaTu 8988t C264(0.82)  LDD1349  [32]
 LDCM0471  CL78 PaTu 8988t C264(0.91)  LDD1350  [32]
 LDCM0472  CL79 PaTu 8988t C264(0.83)  LDD1351  [32]
 LDCM0473  CL8 HEK-293T C264(0.89); C238(0.87)  LDD1676  [33]
 LDCM0474  CL80 PaTu 8988t C264(1.19)  LDD1353  [32]
 LDCM0475  CL81 PaTu 8988t C264(1.19)  LDD1354  [32]
 LDCM0476  CL82 PaTu 8988t C264(0.87)  LDD1355  [32]
 LDCM0477  CL83 PaTu 8988t C264(1.38)  LDD1356  [32]
 LDCM0478  CL84 PaTu 8988t C264(1.18)  LDD1357  [32]
 LDCM0479  CL85 PaTu 8988t C264(1.05)  LDD1358  [32]
 LDCM0480  CL86 PaTu 8988t C264(1.03)  LDD1359  [32]
 LDCM0481  CL87 PaTu 8988t C264(1.41)  LDD1360  [32]
 LDCM0482  CL88 PaTu 8988t C264(1.54)  LDD1361  [32]
 LDCM0483  CL89 PaTu 8988t C264(1.13)  LDD1362  [32]
 LDCM0484  CL9 HEK-293T C264(0.95); C238(1.16)  LDD1687  [33]
 LDCM0485  CL90 PaTu 8988t C264(1.25)  LDD1364  [32]
 LDCM0486  CL91 PaTu 8988t C264(1.10)  LDD1365  [32]
 LDCM0487  CL92 PaTu 8988t C264(1.68)  LDD1366  [32]
 LDCM0488  CL93 PaTu 8988t C264(1.72)  LDD1367  [32]
 LDCM0489  CL94 PaTu 8988t C264(1.75)  LDD1368  [32]
 LDCM0490  CL95 PaTu 8988t C264(1.70)  LDD1369  [32]
 LDCM0491  CL96 PaTu 8988t C264(1.42)  LDD1370  [32]
 LDCM0492  CL97 PaTu 8988t C264(1.33)  LDD1371  [32]
 LDCM0493  CL98 PaTu 8988t C264(1.52)  LDD1372  [32]
 LDCM0494  CL99 PaTu 8988t C264(1.21)  LDD1373  [32]
 LDCM0495  E2913 HEK-293T C264(0.94); C238(1.02)  LDD1698  [33]
 LDCM0468  Fragment33 PaTu 8988t C264(0.43)  LDD1347  [32]
 LDCM0427  Fragment51 PaTu 8988t C264(1.38)  LDD1306  [32]
 LDCM0116  HHS-0101 DM93 Y435(0.85); Y103(1.00)  LDD0264  [13]
 LDCM0117  HHS-0201 DM93 Y435(0.88); Y103(1.19)  LDD0265  [13]
 LDCM0118  HHS-0301 DM93 Y103(0.61); Y435(0.72)  LDD0266  [13]
 LDCM0119  HHS-0401 DM93 Y435(0.85); Y103(1.12)  LDD0267  [13]
 LDCM0120  HHS-0701 DM93 Y435(1.07); Y103(1.35)  LDD0268  [13]
 LDCM0107  IAA HeLa N.A.  LDD0221  [24]
 LDCM0022  KB02 HEK-293T C264(1.01)  LDD1492  [33]
 LDCM0023  KB03 HEK-293T C264(1.10)  LDD1497  [33]
 LDCM0024  KB05 SKMEL24 C264(1.58)  LDD3323  [10]
 LDCM0109  NEM HeLa H151(0.00); H27(0.00); H120(0.00)  LDD0223  [24]
 LDCM0131  RA190 MM1.R 2.81  LDD0300  [12]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tyrosine-protein kinase JAK3 (JAK3) Tyr protein kinase family P52333
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tyrosine-protein kinase HCK (HCK) Tyr protein kinase family P08631
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Probable global transcription activator SNF2L2 (SMARCA2) SNF2/RAD54 helicase family P51531
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 (PLCG1) . P19174
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer and activator of transcription 3 (STAT3) Transcription factor STAT family P40763
Zinc finger and BTB domain-containing protein 7A (ZBTB7A) . O95365
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenomatous polyposis coli protein (APC) Adenomatous polyposis coli (APC) family P25054
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
KH domain-containing, RNA-binding, signal transduction-associated protein 1 (KHDRBS1) KHDRBS family Q07666
Heterogeneous nuclear ribonucleoprotein A1 (HNRNPA1) . P09651
Heterogeneous nuclear ribonucleoprotein K (HNRNPK) . P61978
Proto-oncogene vav (VAV1) . P15498

References

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2 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
3 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
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
5 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
6 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
7 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
8 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
9 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
10 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
11 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
12 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.
13 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
14 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
15 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
16 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.
17 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
18 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
19 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
20 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.
21 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
22 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
23 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
24 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.
25 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.
26 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
27 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.
28 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
29 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
30 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
31 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
32 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.
33 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
34 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.