Details of the Target

General Information of Target

Target ID LDTP04927
Target Name Transforming protein RhoA (RHOA)
Gene Name RHOA
Gene ID 387
Synonyms
ARH12; ARHA; RHO12; Transforming protein RhoA; EC 3.6.5.2; Rho cDNA clone 12; h12
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAIRKKLVIVGDGACGKTCLLIVFSKDQFPEVYVPTVFENYVADIEVDGKQVELALWDT
AGQEDYDRLRPLSYPDTDVILMCFSIDSPDSLENIPEKWTPEVKHFCPNVPIILVGNKKD
LRNDEHTRRELAKMKQEPVKPEEGRDMANRIGAFGYMECSAKTKDGVREVFEMATRAALQ
ARRGKKKSGCLVL
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Small GTPase superfamily, Rho family
Subcellular location
Cell membrane
Function
Small GTPase which cycles between an active GTP-bound and an inactive GDP-bound state. Mainly associated with cytoskeleton organization, in active state binds to a variety of effector proteins to regulate cellular responses such as cytoskeletal dynamics, cell migration and cell cycle. Regulates a signal transduction pathway linking plasma membrane receptors to the assembly of focal adhesions and actin stress fibers. Involved in a microtubule-dependent signal that is required for the myosin contractile ring formation during cell cycle cytokinesis. Plays an essential role in cleavage furrow formation. Required for the apical junction formation of keratinocyte cell-cell adhesion. Essential for the SPATA13-mediated regulation of cell migration and adhesion assembly and disassembly. The MEMO1-RHOA-DIAPH1 signaling pathway plays an important role in ERBB2-dependent stabilization of microtubules at the cell cortex. It controls the localization of APC and CLASP2 to the cell membrane, via the regulation of GSK3B activity. In turn, membrane-bound APC allows the localization of the MACF1 to the cell membrane, which is required for microtubule capture and stabilization. Regulates KCNA2 potassium channel activity by reducing its location at the cell surface in response to CHRM1 activation; promotes KCNA2 endocytosis. Acts as an allosteric activator of guanine nucleotide exchange factor ECT2 by binding in its activated GTP-bound form to the PH domain of ECT2 which stimulates the release of PH inhibition and promotes the binding of substrate RHOA to the ECT2 catalytic center. May be an activator of PLCE1. In neurons, involved in the inhibition of the initial spine growth. Upon activation by CaMKII, modulates dendritic spine structural plasticity by relaying CaMKII transient activation to synapse-specific, long-term signaling. Acts as a regulator of platelet alpha-granule release during activation and aggregation of platelets.; (Microbial infection) Serves as a target for the yopT cysteine peptidase from Yersinia pestis, vector of the plague.
TTD ID
T58474
Uniprot ID
P61586
DrugMap ID
TTFNDGV
Ensemble ID
ENST00000418115.6
HGNC ID
HGNC:667
ChEMBL ID
CHEMBL6052

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 32 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		7.16  LDD0402  [1]
CY4
 Probe Info  		100.00  LDD0244  [2]
N1
 Probe Info  		100.00  LDD0242  [2]
C-Sul
 Probe Info  		3.80  LDD0066  [3]
TH211
 Probe Info  		Y66(20.00)  LDD0257  [4]
STPyne
 Probe Info  		K104(1.83); K135(2.42); K6(7.69); K7(0.97)  LDD0277  [5]
JZ128-DTB
 Probe Info  		C159(0.00); C16(0.00)  LDD0462  [6]
BTD
 Probe Info  		C159(2.09)  LDD1700  [7]
Johansson_61
 Probe Info  		_(20.00)  LDD1490  [8]
HHS-475
 Probe Info  		Y34(0.35); Y66(3.40)  LDD0264  [9]
DBIA
 Probe Info  		C16(0.95); C107(0.86)  LDD0078  [10]
ATP probe
 Probe Info  		K162(0.00); K164(0.00); K135(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info  		C107(0.00); C159(0.00); C16(0.00); C83(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info  		C20(0.00); C107(0.00); C16(0.00); C159(0.00)  LDD0032  [13]
IPIAA_H
 Probe Info  		C20(0.00); C83(0.00); C16(0.00)  LDD0030  [14]
IPIAA_L
 Probe Info  		C83(0.00); C16(0.00); C20(0.00); C107(0.00)  LDD0031  [14]
Lodoacetamide azide
 Probe Info  		C107(0.00); C159(0.00); C16(0.00); C83(0.00)  LDD0037  [12]
IPM
 Probe Info  		C16(0.00); C159(0.00)  LDD0025  [15]
JW-RF-010
 Probe Info  		C107(0.00); C159(0.00)  LDD0026  [15]
TFBX
 Probe Info  		C16(0.00); C159(0.00)  LDD0027  [15]
WYneN
 Probe Info  		C16(0.00); C159(0.00)  LDD0021  [16]
Compound 10
 Probe Info  		C107(0.00); C159(0.00); C16(0.00)  LDD2216  [17]
NHS
 Probe Info  		N.A.  LDD0010  [16]
PF-06672131
 Probe Info  		N.A.  LDD0152  [18]
Acrolein
 Probe Info  		N.A.  LDD0217  [19]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [19]
Methacrolein
 Probe Info  		N.A.  LDD0218  [19]
W1
 Probe Info  		N.A.  LDD0236  [20]
AOyne
 Probe Info  		8.70  LDD0443  [21]
NAIA_5
 Probe Info  		N.A.  LDD2223  [22]
TER-AC
 Probe Info  		N.A.  LDD0426  [23]
HHS-465
 Probe Info  		N.A.  LDD2240  [24]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe3
 Probe Info  		12.71  LDD0464  [25]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C16(1.03); C159(0.73)  LDD2142  [7]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C16(0.80); C159(0.95)  LDD2112  [7]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C16(1.57); C159(0.57)  LDD2095  [7]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C16(0.78); C159(1.13)  LDD2130  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C159(1.20)  LDD2117  [7]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C16(1.06); C159(1.39)  LDD2152  [7]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C16(0.86); C159(1.69)  LDD2103  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C159(0.66)  LDD2132  [7]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C16(0.70); C159(0.76)  LDD2131  [7]
 LDCM0026  4SU-RNA+native RNA HEK-293T C83(2.39)  LDD0372  [26]
 LDCM0214  AC1 HCT 116 C159(1.63)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C159(1.24)  LDD0532  [10]
 LDCM0216  AC100 HCT 116 C159(1.15)  LDD0533  [10]
 LDCM0217  AC101 HCT 116 C159(0.89)  LDD0534  [10]
 LDCM0218  AC102 HCT 116 C159(0.84)  LDD0535  [10]
 LDCM0219  AC103 HCT 116 C159(0.69)  LDD0536  [10]
 LDCM0220  AC104 HCT 116 C159(0.71)  LDD0537  [10]
 LDCM0221  AC105 HCT 116 C159(0.71)  LDD0538  [10]
 LDCM0222  AC106 HCT 116 C159(0.66)  LDD0539  [10]
 LDCM0223  AC107 HCT 116 C159(0.62)  LDD0540  [10]
 LDCM0224  AC108 HCT 116 C159(0.74)  LDD0541  [10]
 LDCM0225  AC109 HCT 116 C159(0.78)  LDD0542  [10]
 LDCM0226  AC11 HCT 116 C159(1.41)  LDD0543  [10]
 LDCM0227  AC110 HCT 116 C159(0.78)  LDD0544  [10]
 LDCM0228  AC111 HCT 116 C159(0.64)  LDD0545  [10]
 LDCM0229  AC112 HCT 116 C159(0.70)  LDD0546  [10]
 LDCM0230  AC113 HCT 116 C159(1.14)  LDD0547  [10]
 LDCM0231  AC114 HCT 116 C159(1.13)  LDD0548  [10]
 LDCM0232  AC115 HCT 116 C159(0.81)  LDD0549  [10]
 LDCM0233  AC116 HCT 116 C159(0.67)  LDD0550  [10]
 LDCM0234  AC117 HCT 116 C159(0.75)  LDD0551  [10]
 LDCM0235  AC118 HCT 116 C159(1.00)  LDD0552  [10]
 LDCM0236  AC119 HCT 116 C159(1.27)  LDD0553  [10]
 LDCM0237  AC12 HCT 116 C159(1.23)  LDD0554  [10]
 LDCM0238  AC120 HCT 116 C159(1.05)  LDD0555  [10]
 LDCM0239  AC121 HCT 116 C159(1.15)  LDD0556  [10]
 LDCM0240  AC122 HCT 116 C159(0.81)  LDD0557  [10]
 LDCM0241  AC123 HCT 116 C159(1.64)  LDD0558  [10]
 LDCM0242  AC124 HCT 116 C159(1.11)  LDD0559  [10]
 LDCM0243  AC125 HCT 116 C159(1.38)  LDD0560  [10]
 LDCM0244  AC126 HCT 116 C159(1.40)  LDD0561  [10]
 LDCM0245  AC127 HCT 116 C159(1.33)  LDD0562  [10]
 LDCM0246  AC128 HCT 116 C159(0.32)  LDD0563  [10]
 LDCM0247  AC129 HCT 116 C159(1.37)  LDD0564  [10]
 LDCM0249  AC130 HCT 116 C159(0.61)  LDD0566  [10]
 LDCM0250  AC131 HCT 116 C159(0.75)  LDD0567  [10]
 LDCM0251  AC132 HCT 116 C159(1.19)  LDD0568  [10]
 LDCM0252  AC133 HCT 116 C159(0.76)  LDD0569  [10]
 LDCM0253  AC134 HCT 116 C159(0.63)  LDD0570  [10]
 LDCM0254  AC135 HCT 116 C159(0.67)  LDD0571  [10]
 LDCM0255  AC136 HCT 116 C159(0.84)  LDD0572  [10]
 LDCM0256  AC137 HCT 116 C159(0.80)  LDD0573  [10]
 LDCM0257  AC138 HCT 116 C159(0.81)  LDD0574  [10]
 LDCM0258  AC139 HCT 116 C159(1.03)  LDD0575  [10]
 LDCM0259  AC14 HCT 116 C159(1.31)  LDD0576  [10]
 LDCM0260  AC140 HCT 116 C159(0.67)  LDD0577  [10]
 LDCM0261  AC141 HCT 116 C159(0.71)  LDD0578  [10]
 LDCM0262  AC142 HCT 116 C159(1.15)  LDD0579  [10]
 LDCM0263  AC143 HCT 116 C159(0.81)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C159(0.84)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C159(0.86)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C159(0.84)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C159(0.92)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C159(0.79)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C159(0.83)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C159(1.25)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C159(0.99)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C159(0.95)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C159(0.88)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C159(0.69)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C159(0.97)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C159(0.83)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C159(0.93)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C159(0.90)  LDD2161  [10]
 LDCM0276  AC17 HEK-293T C159(0.96)  LDD1515  [27]
 LDCM0277  AC18 HEK-293T C159(0.96)  LDD1516  [27]
 LDCM0278  AC19 HEK-293T C159(0.96)  LDD1517  [27]
 LDCM0279  AC2 HCT 116 C159(1.11)  LDD0596  [10]
 LDCM0280  AC20 HEK-293T C159(1.02)  LDD1519  [27]
 LDCM0281  AC21 HEK-293T C159(1.02)  LDD1520  [27]
 LDCM0282  AC22 HEK-293T C159(1.19)  LDD1521  [27]
 LDCM0283  AC23 HEK-293T C159(0.95)  LDD1522  [27]
 LDCM0284  AC24 HEK-293T C159(0.94)  LDD1523  [27]
 LDCM0285  AC25 HCT 116 C159(0.89)  LDD0602  [10]
 LDCM0286  AC26 HCT 116 C159(0.91)  LDD0603  [10]
 LDCM0287  AC27 HCT 116 C159(0.94)  LDD0604  [10]
 LDCM0288  AC28 HCT 116 C159(1.03)  LDD0605  [10]
 LDCM0289  AC29 HCT 116 C159(0.81)  LDD0606  [10]
 LDCM0290  AC3 HCT 116 C159(1.40)  LDD0607  [10]
 LDCM0291  AC30 HCT 116 C159(0.77)  LDD0608  [10]
 LDCM0292  AC31 HCT 116 C159(0.70)  LDD0609  [10]
 LDCM0293  AC32 HCT 116 C159(0.71)  LDD0610  [10]
 LDCM0294  AC33 HCT 116 C159(1.03)  LDD0611  [10]
 LDCM0295  AC34 HCT 116 C159(0.81)  LDD0612  [10]
 LDCM0296  AC35 HEK-293T C159(1.49)  LDD0894  [10]
 LDCM0297  AC36 HEK-293T C159(1.40)  LDD0895  [10]
 LDCM0298  AC37 HEK-293T C159(1.47)  LDD0896  [10]
 LDCM0299  AC38 HEK-293T C159(1.23)  LDD0897  [10]
 LDCM0300  AC39 HEK-293T C159(1.12)  LDD0898  [10]
 LDCM0301  AC4 HCT 116 C159(1.60)  LDD0618  [10]
 LDCM0302  AC40 HEK-293T C159(0.86)  LDD0900  [10]
 LDCM0303  AC41 HEK-293T C159(0.91)  LDD0901  [10]
 LDCM0304  AC42 HEK-293T C159(1.00)  LDD0902  [10]
 LDCM0305  AC43 HEK-293T C159(1.04)  LDD0903  [10]
 LDCM0306  AC44 HEK-293T C159(0.88)  LDD0904  [10]
 LDCM0307  AC45 HEK-293T C159(0.98)  LDD0905  [10]
 LDCM0308  AC46 HEK-293T C159(1.23)  LDD0906  [10]
 LDCM0309  AC47 HEK-293T C159(1.20)  LDD0907  [10]
 LDCM0310  AC48 HEK-293T C159(1.16)  LDD0908  [10]
 LDCM0311  AC49 HEK-293T C159(0.84)  LDD0909  [10]
 LDCM0312  AC5 HCT 116 C159(1.43)  LDD0629  [10]
 LDCM0313  AC50 HEK-293T C159(0.98)  LDD0911  [10]
 LDCM0314  AC51 HEK-293T C159(1.05)  LDD0912  [10]
 LDCM0315  AC52 HEK-293T C159(0.97)  LDD0913  [10]
 LDCM0316  AC53 HEK-293T C159(1.23)  LDD0914  [10]
 LDCM0317  AC54 HEK-293T C159(1.00)  LDD0915  [10]
 LDCM0318  AC55 HEK-293T C159(0.97)  LDD0916  [10]
 LDCM0319  AC56 HEK-293T C159(1.02)  LDD0917  [10]
 LDCM0320  AC57 HCT 116 C159(0.75)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C159(0.56)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C159(0.57)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C159(0.95)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C159(0.73)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C159(0.92)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C159(0.73)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C159(0.82)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C159(0.66)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C159(0.71)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C159(0.77)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C159(0.53)  LDD0648  [10]
 LDCM0332  AC68 HEK-293T C159(0.89)  LDD0930  [10]
 LDCM0333  AC69 HEK-293T C159(0.85)  LDD0931  [10]
 LDCM0334  AC7 HCT 116 C159(1.24)  LDD0651  [10]
 LDCM0335  AC70 HEK-293T C159(0.95)  LDD0933  [10]
 LDCM0336  AC71 HEK-293T C159(1.00)  LDD0934  [10]
 LDCM0337  AC72 HEK-293T C159(0.72)  LDD0935  [10]
 LDCM0338  AC73 HEK-293T C159(1.07)  LDD0936  [10]
 LDCM0339  AC74 HEK-293T C159(0.81)  LDD0937  [10]
 LDCM0340  AC75 HEK-293T C159(0.66)  LDD0938  [10]
 LDCM0341  AC76 HEK-293T C159(0.69)  LDD0939  [10]
 LDCM0342  AC77 HEK-293T C159(0.72)  LDD0940  [10]
 LDCM0343  AC78 HEK-293T C159(0.79)  LDD0941  [10]
 LDCM0344  AC79 HEK-293T C159(0.91)  LDD0942  [10]
 LDCM0345  AC8 HCT 116 C159(0.95)  LDD0662  [10]
 LDCM0346  AC80 HEK-293T C159(0.94)  LDD0944  [10]
 LDCM0347  AC81 HEK-293T C159(0.86)  LDD0945  [10]
 LDCM0348  AC82 HEK-293T C159(1.00)  LDD0946  [10]
 LDCM0349  AC83 HCT 116 C159(0.30)  LDD0666  [10]
 LDCM0350  AC84 HCT 116 C159(0.49)  LDD0667  [10]
 LDCM0351  AC85 HCT 116 C159(1.09)  LDD0668  [10]
 LDCM0352  AC86 HCT 116 C159(0.95)  LDD0669  [10]
 LDCM0353  AC87 HCT 116 C159(1.04)  LDD0670  [10]
 LDCM0354  AC88 HCT 116 C159(1.00)  LDD0671  [10]
 LDCM0355  AC89 HCT 116 C159(0.68)  LDD0672  [10]
 LDCM0357  AC90 HCT 116 C159(1.74)  LDD0674  [10]
 LDCM0358  AC91 HCT 116 C159(0.26)  LDD0675  [10]
 LDCM0359  AC92 HCT 116 C159(0.42)  LDD0676  [10]
 LDCM0360  AC93 HCT 116 C159(1.05)  LDD0677  [10]
 LDCM0361  AC94 HCT 116 C159(1.42)  LDD0678  [10]
 LDCM0362  AC95 HCT 116 C159(1.02)  LDD0679  [10]
 LDCM0363  AC96 HCT 116 C159(0.78)  LDD0680  [10]
 LDCM0364  AC97 HCT 116 C159(0.58)  LDD0681  [10]
 LDCM0365  AC98 HCT 116 C159(0.35)  LDD0682  [10]
 LDCM0366  AC99 HCT 116 C159(0.78)  LDD0683  [10]
 LDCM0545  Acetamide MDA-MB-231 C16(0.26); C159(0.86)  LDD2138  [7]
 LDCM0520  AKOS000195272 MDA-MB-231 C16(0.97); C159(0.97)  LDD2113  [7]
 LDCM0248  AKOS034007472 HCT 116 C159(1.34)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C159(1.36)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C159(0.88)  LDD0592  [10]
 LDCM0156  Aniline NCI-H1299 11.40  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C16(0.95); C107(0.86)  LDD0078  [10]
 LDCM0498  BS-3668 MDA-MB-231 C16(0.49); C159(0.92)  LDD2091  [7]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [19]
 LDCM0367  CL1 HCT 116 C159(0.79)  LDD0684  [10]
 LDCM0368  CL10 HCT 116 C159(0.48)  LDD0685  [10]
 LDCM0369  CL100 HCT 116 C159(1.58)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C159(1.09)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C159(1.15)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C159(1.34)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C159(1.16)  LDD0690  [10]
 LDCM0374  CL105 HEK-293T C159(0.83)  LDD1578  [27]
 LDCM0375  CL106 HEK-293T C159(0.95)  LDD1579  [27]
 LDCM0376  CL107 HEK-293T C159(0.91)  LDD1580  [27]
 LDCM0377  CL108 HEK-293T C159(1.05)  LDD1581  [27]
 LDCM0378  CL109 HEK-293T C159(0.91)  LDD1582  [27]
 LDCM0379  CL11 HCT 116 C159(0.31)  LDD0696  [10]
 LDCM0380  CL110 HEK-293T C159(1.03)  LDD1584  [27]
 LDCM0381  CL111 HEK-293T C159(0.90)  LDD1585  [27]
 LDCM0382  CL112 HCT 116 C159(1.08)  LDD0699  [10]
 LDCM0383  CL113 HCT 116 C159(0.80)  LDD0700  [10]
 LDCM0384  CL114 HCT 116 C159(0.67)  LDD0701  [10]
 LDCM0385  CL115 HCT 116 C159(0.94)  LDD0702  [10]
 LDCM0386  CL116 HCT 116 C159(1.18)  LDD0703  [10]
 LDCM0387  CL117 HEK-293T C159(1.65)  LDD0985  [10]
 LDCM0388  CL118 HEK-293T C159(1.39)  LDD0986  [10]
 LDCM0389  CL119 HEK-293T C159(0.85)  LDD0987  [10]
 LDCM0390  CL12 HCT 116 C159(0.25)  LDD0707  [10]
 LDCM0391  CL120 HEK-293T C159(0.96)  LDD0989  [10]
 LDCM0392  CL121 HEK-293T C159(1.03)  LDD0990  [10]
 LDCM0393  CL122 HEK-293T C159(0.97)  LDD0991  [10]
 LDCM0394  CL123 HEK-293T C159(1.06)  LDD0992  [10]
 LDCM0395  CL124 HEK-293T C159(0.92)  LDD0993  [10]
 LDCM0396  CL125 HCT 116 C159(0.86)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C159(0.68)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C159(0.70)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C159(0.62)  LDD0716  [10]
 LDCM0400  CL13 HCT 116 C159(0.62)  LDD0717  [10]
 LDCM0401  CL14 HCT 116 C159(0.83)  LDD0718  [10]
 LDCM0402  CL15 HCT 116 C159(0.34)  LDD0719  [10]
 LDCM0403  CL16 HCT 116 C159(0.84)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C159(0.81)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C159(1.16)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C159(0.97)  LDD0723  [10]
 LDCM0407  CL2 HCT 116 C159(0.99)  LDD0724  [10]
 LDCM0408  CL20 HCT 116 C159(0.68)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C159(0.62)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C159(0.55)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C159(0.82)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C159(0.68)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C159(0.62)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C159(0.92)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C159(0.98)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C159(0.76)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C159(0.80)  LDD0734  [10]
 LDCM0418  CL3 HCT 116 C159(0.95)  LDD0735  [10]
 LDCM0419  CL30 HCT 116 C159(1.14)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C159(0.89)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C159(0.86)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C159(0.74)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C159(0.47)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C159(0.50)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C159(0.54)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C159(0.48)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C159(0.56)  LDD0745  [10]
 LDCM0429  CL4 HCT 116 C159(0.81)  LDD0746  [10]
 LDCM0430  CL40 HCT 116 C159(0.48)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C159(0.79)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C159(0.38)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C159(0.47)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C159(0.73)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C159(0.65)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C159(1.17)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C159(1.14)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C159(1.14)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C159(1.01)  LDD0756  [10]
 LDCM0440  CL5 HCT 116 C159(0.88)  LDD0757  [10]
 LDCM0441  CL50 HCT 116 C159(1.13)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C159(1.16)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C159(1.13)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C159(1.03)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C159(1.00)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C159(1.08)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C159(0.92)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C159(1.14)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C159(1.19)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C159(1.10)  LDD0767  [10]
 LDCM0451  CL6 HCT 116 C159(0.88)  LDD0768  [10]
 LDCM0452  CL60 HCT 116 C159(1.04)  LDD0769  [10]
 LDCM0453  CL61 HCT 116 C159(0.99)  LDD0770  [10]
 LDCM0454  CL62 HCT 116 C159(0.98)  LDD0771  [10]
 LDCM0455  CL63 HCT 116 C159(1.06)  LDD0772  [10]
 LDCM0456  CL64 HCT 116 C159(1.18)  LDD0773  [10]
 LDCM0457  CL65 HCT 116 C159(0.96)  LDD0774  [10]
 LDCM0458  CL66 HCT 116 C159(0.97)  LDD0775  [10]
 LDCM0459  CL67 HCT 116 C159(1.19)  LDD0776  [10]
 LDCM0460  CL68 HCT 116 C159(0.83)  LDD0777  [10]
 LDCM0461  CL69 HCT 116 C159(0.98)  LDD0778  [10]
 LDCM0462  CL7 HCT 116 C159(0.44)  LDD0779  [10]
 LDCM0463  CL70 HCT 116 C159(0.94)  LDD0780  [10]
 LDCM0464  CL71 HCT 116 C159(0.96)  LDD0781  [10]
 LDCM0465  CL72 HCT 116 C159(0.86)  LDD0782  [10]
 LDCM0466  CL73 HCT 116 C159(0.93)  LDD0783  [10]
 LDCM0467  CL74 HCT 116 C159(1.11)  LDD0784  [10]
 LDCM0469  CL76 HCT 116 C159(0.78)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C159(0.66)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C159(0.73)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C159(0.35)  LDD0789  [10]
 LDCM0473  CL8 HCT 116 C159(0.23)  LDD0790  [10]
 LDCM0474  CL80 HCT 116 C159(1.01)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C159(0.66)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C159(0.20)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C159(0.26)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C159(0.10)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C159(0.71)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C159(0.97)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C159(0.69)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C159(0.26)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C159(0.09)  LDD0800  [10]
 LDCM0484  CL9 HCT 116 C159(0.66)  LDD0801  [10]
 LDCM0485  CL90 HCT 116 C159(0.61)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C159(0.52)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C159(1.04)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C159(1.20)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C159(1.23)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C159(0.93)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C159(0.88)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C159(0.94)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C159(1.35)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C159(1.41)  LDD0811  [10]
 LDCM0495  E2913 HEK-293T C159(1.06)  LDD1698  [27]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C159(3.24)  LDD1702  [7]
 LDCM0625  F8 Ramos C16(0.66); C159(0.45); C20(0.37); C107(1.74)  LDD2187  [28]
 LDCM0572  Fragment10 Ramos C16(0.93); C159(0.66); C107(0.47)  LDD2189  [28]
 LDCM0573  Fragment11 Ramos C16(0.22); C159(0.08); C107(0.07)  LDD2190  [28]
 LDCM0574  Fragment12 Ramos C16(1.21); C159(1.01); C107(0.17)  LDD2191  [28]
 LDCM0575  Fragment13 Ramos C16(1.18); C159(1.14); C107(0.20)  LDD2192  [28]
 LDCM0576  Fragment14 Ramos C16(1.18); C159(0.69); C20(0.80); C107(0.88)  LDD2193  [28]
 LDCM0579  Fragment20 Ramos C16(1.05); C159(0.94); C107(0.23)  LDD2194  [28]
 LDCM0580  Fragment21 Ramos C16(1.31); C159(1.25); C107(0.20)  LDD2195  [28]
 LDCM0582  Fragment23 Ramos C16(0.44); C159(0.51); C107(0.24)  LDD2196  [28]
 LDCM0578  Fragment27 Ramos C16(1.19); C159(1.22); C107(0.80)  LDD2197  [28]
 LDCM0586  Fragment28 Ramos C16(0.96); C159(0.73); C107(0.61)  LDD2198  [28]
 LDCM0588  Fragment30 Ramos C16(1.25); C159(1.04); C107(0.28)  LDD2199  [28]
 LDCM0589  Fragment31 Ramos C16(1.15); C159(1.44); C107(0.63)  LDD2200  [28]
 LDCM0590  Fragment32 Ramos C16(0.96); C159(0.62); C107(0.35)  LDD2201  [28]
 LDCM0468  Fragment33 HCT 116 C159(1.03)  LDD0785  [10]
 LDCM0596  Fragment38 Ramos C16(0.99); C159(1.08); C107(0.38)  LDD2203  [28]
 LDCM0566  Fragment4 Ramos C16(0.94); C159(0.96); C20(0.54); C107(0.97)  LDD2184  [28]
 LDCM0427  Fragment51 HCT 116 C159(0.36)  LDD0744  [10]
 LDCM0610  Fragment52 Ramos C16(1.30); C159(0.95); C107(0.56)  LDD2204  [28]
 LDCM0614  Fragment56 Ramos C16(1.19); C159(0.89); C107(0.20)  LDD2205  [28]
 LDCM0617  Fragment63-S Jurkat _(20.00)  LDD1490  [8]
 LDCM0569  Fragment7 Ramos C16(0.77); C159(0.76); C20(0.44); C107(0.73)  LDD2186  [28]
 LDCM0571  Fragment9 Ramos C16(1.09); C159(0.84); C107(0.17)  LDD2188  [28]
 LDCM0116  HHS-0101 DM93 Y34(0.35); Y66(3.40)  LDD0264  [9]
 LDCM0117  HHS-0201 DM93 Y34(0.40); Y66(1.30)  LDD0265  [9]
 LDCM0118  HHS-0301 DM93 Y66(0.52); Y34(0.68)  LDD0266  [9]
 LDCM0119  HHS-0401 DM93 Y34(0.72); Y66(0.77)  LDD0267  [9]
 LDCM0120  HHS-0701 DM93 Y34(0.50); Y66(2.34)  LDD0268  [9]
 LDCM0107  IAA HeLa N.A.  LDD0221  [19]
 LDCM0179  JZ128 PC-3 C159(0.00); C16(0.00)  LDD0462  [6]
 LDCM0022  KB02 HEK-293T C159(1.01)  LDD1492  [27]
 LDCM0023  KB03 HEK-293T C159(0.92)  LDD1497  [27]
 LDCM0024  KB05 COLO792 C159(1.31)  LDD3310  [29]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C16(0.71); C159(1.57)  LDD2102  [7]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C159(0.87)  LDD2121  [7]
 LDCM0109  NEM HeLa N.A.  LDD0230  [19]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C159(1.01)  LDD2089  [7]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C16(0.87); C159(1.43)  LDD2090  [7]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C16(0.76); C159(1.24); C107(0.99)  LDD2092  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C16(0.74); C159(1.50)  LDD2093  [7]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C16(0.85); C159(1.59); C107(1.12)  LDD2094  [7]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C159(1.18)  LDD2097  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C16(1.04); C159(1.18)  LDD2098  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C159(0.99)  LDD2099  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C16(1.41); C159(1.84)  LDD2100  [7]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C16(0.69); C159(0.93)  LDD2101  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C16(0.99); C159(3.83)  LDD2104  [7]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C159(1.66); C107(1.27)  LDD2105  [7]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C16(1.32); C159(0.84)  LDD2106  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C159(0.95)  LDD2107  [7]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C16(0.87); C159(2.44)  LDD2108  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C16(0.81); C159(0.91); C107(2.01)  LDD2109  [7]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C16(1.18)  LDD2110  [7]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C16(0.88); C159(1.14)  LDD2111  [7]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C16(0.83)  LDD2114  [7]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C159(0.61)  LDD2115  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C16(2.43); C159(1.43)  LDD2119  [7]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C16(0.95); C159(0.87)  LDD2120  [7]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C159(0.24)  LDD2122  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C159(1.13)  LDD2123  [7]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C16(2.58); C159(0.22)  LDD2124  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C16(0.65); C159(1.21)  LDD2125  [7]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C16(0.33); C159(0.23)  LDD2126  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C16(0.85); C159(1.17)  LDD2127  [7]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C16(1.11); C159(1.14)  LDD2128  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C16(0.62); C159(1.68)  LDD2129  [7]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C16(0.63)  LDD2133  [7]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C159(0.64)  LDD2134  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C16(1.03); C159(1.53)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C16(0.98); C159(1.59)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C159(0.98)  LDD2137  [7]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C159(2.09)  LDD1700  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C16(0.54); C159(0.96)  LDD2140  [7]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C16(0.95); C159(1.29)  LDD2141  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C16(1.05); C159(0.95)  LDD2143  [7]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C16(1.78); C159(2.11)  LDD2144  [7]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C16(11.71)  LDD2145  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C16(0.65); C159(1.06)  LDD2146  [7]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C16(3.64); C159(1.82)  LDD2147  [7]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C16(0.65); C159(0.58)  LDD2148  [7]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C159(0.14)  LDD2149  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C16(0.44); C159(0.79)  LDD2150  [7]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C16(1.31); C159(2.13)  LDD2153  [7]
 LDCM0131  RA190 MM1.R C159(1.31)  LDD0304  [30]
 LDCM0111  W14 Hep-G2 K7(0.53)  LDD0238  [20]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Rho-associated protein kinase 1 (ROCK1) AGC Ser/Thr protein kinase family Q13464
Rho family-interacting cell polarization regulator 2 (RIPOR2) RIPOR family Q9Y4F9
RIPOR family member 3 (RIPOR3) RIPOR family Q96MK2
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mothers against decapentaplegic homolog 2 (SMAD2) Dwarfin/SMAD family Q15796
Zinc finger protein Aiolos (IKZF3) Ikaros C2H2-type zinc-finger protein family Q9UKT9
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Advanced glycosylation end product-specific receptor (AGER) . Q15109
Other
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-dependent kinase inhibitor 1B (CDKN1B) CDI family P46527
Disheveled-associated activator of morphogenesis 1 (DAAM1) Formin homology family Q9Y4D1
Protein diaphanous homolog 1 (DIAPH1) Formin homology family O60610
Rho GDP-dissociation inhibitor 1 (ARHGDIA) Rho GDI family P52565
Thyroid receptor-interacting protein 6 (TRIP6) Zyxin/ajuba family Q15654
Nucleolin (NCL) . P19338
Rho GTPase-activating protein 1 (ARHGAP1) . Q07960
Rho guanine nucleotide exchange factor 11 (ARHGEF11) . O15085
Rho guanine nucleotide exchange factor 12 (ARHGEF12) . Q9NZN5
Rho guanine nucleotide exchange factor 19 (ARHGEF19) . Q8IW93
Rho guanine nucleotide exchange factor 2 (ARHGEF2) . Q92974
Rhotekin (RTKN) . Q9BST9

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
Guanosine-5'-diphosphate Small molecular drug DB04315
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Es-285 . D08SUQ

References

1 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.
2 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.
3 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
4 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.
5 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
6 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
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 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
9 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.
10 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.
11 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.
12 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
13 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
14 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
15 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
16 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
17 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
18 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
19 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.
20 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.
21 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.
22 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
23 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
24 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
25 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.
26 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
27 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
28 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
29 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
30 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.