Details of the Target

General Information of Target

Target ID LDTP02743
Target Name Insulin-degrading enzyme (IDE)
Gene Name IDE
Gene ID 3416
Synonyms
Insulin-degrading enzyme; EC 3.4.24.56; Abeta-degrading protease; Insulin protease; Insulinase; Insulysin
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRYRLAWLLHPALPSTFRSVLGARLPPPERLCGFQKKTYSKMNNPAIKRIGNHITKSPED
KREYRGLELANGIKVLLISDPTTDKSSAALDVHIGSLSDPPNIAGLSHFCEHMLFLGTKK
YPKENEYSQFLSEHAGSSNAFTSGEHTNYYFDVSHEHLEGALDRFAQFFLCPLFDESCKD
REVNAVDSEHEKNVMNDAWRLFQLEKATGNPKHPFSKFGTGNKYTLETRPNQEGIDVRQE
LLKFHSAYYSSNLMAVCVLGRESLDDLTNLVVKLFSEVENKNVPLPEFPEHPFQEEHLKQ
LYKIVPIKDIRNLYVTFPIPDLQKYYKSNPGHYLGHLIGHEGPGSLLSELKSKGWVNTLV
GGQKEGARGFMFFIINVDLTEEGLLHVEDIILHMFQYIQKLRAEGPQEWVFQECKDLNAV
AFRFKDKERPRGYTSKIAGILHYYPLEEVLTAEYLLEEFRPDLIEMVLDKLRPENVRVAI
VSKSFEGKTDRTEEWYGTQYKQEAIPDEVIKKWQNADLNGKFKLPTKNEFIPTNFEILPL
EKEATPYPALIKDTAMSKLWFKQDDKFFLPKACLNFEFFSPFAYVDPLHCNMAYLYLELL
KDSLNEYAYAAELAGLSYDLQNTIYGMYLSVKGYNDKQPILLKKIIEKMATFEIDEKRFE
IIKEAYMRSLNNFRAEQPHQHAMYYLRLLMTEVAWTKDELKEALDDVTLPRLKAFIPQLL
SRLHIEALLHGNITKQAALGIMQMVEDTLIEHAHTKPLLPSQLVRYREVQLPDRGWFVYQ
QRNEVHNNCGIEIYYQTDMQSTSENMFLELFCQIISEPCFNTLRTKEQLGYIVFSGPRRA
NGIQGLRFIIQSEKPPHYLESRVEAFLITMEKSIEDMTEEAFQKHIQALAIRRLDKPKKL
SAECAKYWGEIISQQYNFDRDNTEVAYLKTLTKEDIIKFYKEMLAVDAPRRHKVSVHVLA
REMDSCPVVGEFPCQNDINLSQAPALPQPEVIQNMTEFKRGLPLFPLVKPHINFMAAKL
Target Type
Successful
Target Bioclass
Enzyme
Family
Peptidase M16 family
Subcellular location
Cytoplasm, cytosol
Function
Plays a role in the cellular breakdown of insulin, APP peptides, IAPP peptides, natriuretic peptides, glucagon, bradykinin, kallidin, and other peptides, and thereby plays a role in intercellular peptide signaling. Substrate binding induces important conformation changes, making it possible to bind and degrade larger substrates, such as insulin. Contributes to the regulation of peptide hormone signaling cascades and regulation of blood glucose homeostasis via its role in the degradation of insulin, glucagon and IAPP. Plays a role in the degradation and clearance of APP-derived amyloidogenic peptides that are secreted by neurons and microglia (Probable). Degrades the natriuretic peptides ANP, BNP and CNP, inactivating their ability to raise intracellular cGMP. Also degrades an aberrant frameshifted 40-residue form of NPPA (fsNPPA) which is associated with familial atrial fibrillation in heterozygous patients. Involved in antigen processing. Produces both the N terminus and the C terminus of MAGEA3-derived antigenic peptide (EVDPIGHLY) that is presented to cytotoxic T lymphocytes by MHC class I.; (Microbial infection) The membrane-associated isoform acts as an entry receptor for varicella-zoster virus (VZV).
TTD ID
T81900
Uniprot ID
P14735
DrugMap ID
TT2EDHU
Ensemble ID
ENST00000265986.11
HGNC ID
HGNC:5381
ChEMBL ID
CHEMBL1293287

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 Deletion: p.L116WfsTer43 .
CAL51 Deletion: p.L116WfsTer43 .
DU145 SNV: p.A135V .
HEC1 SNV: p.P717H DBIA    Probe Info 
HEC1B SNV: p.P717H .
JURKAT SNV: p.A438T .
NCIH1155 SNV: p.L114I .
RKO Deletion: p.L569CfsTer45 .
RL952 Deletion: p.L569CfsTer45 .
SNGM Deletion: p.L569CfsTer45
SNV: p.R668Q		 DBIA    Probe Info 
WM115 SNV: p.T380I .
WM2664 Insertion: p.N635KfsTer2
SNV: p.T380I		 .

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  		14.54  LDD0402  [1]
TH214
 Probe Info  		Y302(17.38)  LDD0258  [2]
TH216
 Probe Info  		Y302(20.00)  LDD0259  [2]
ONAyne
 Probe Info  		K854(1.11)  LDD0274  [3]
OPA-S-S-alkyne
 Probe Info  		K364(2.30)  LDD3494  [4]
Probe 1
 Probe Info  		Y224(36.73); Y547(21.53)  LDD3495  [5]
BTD
 Probe Info  		C904(1.07)  LDD1700  [6]
DA-P3
 Probe Info  		9.56  LDD0183  [7]
AHL-Pu-1
 Probe Info  		C966(3.51)  LDD0168  [8]
HHS-475
 Probe Info  		Y831(1.02)  LDD0264  [9]
HHS-465
 Probe Info  		Y831(10.00)  LDD2237  [10]
DBIA
 Probe Info  		C414(1.03)  LDD0531  [11]
5E-2FA
 Probe Info  		N.A.  LDD2235  [12]
ATP probe
 Probe Info  		K192(0.00); K899(0.00); K884(0.00); K854(0.00)  LDD0199  [13]
4-Iodoacetamidophenylacetylene
 Probe Info  		C414(0.00); C904(0.00); C178(0.00); C171(0.00)  LDD0038  [14]
IA-alkyne
 Probe Info  		C414(0.00); C178(0.00); C171(0.00); C904(0.00)  LDD0036  [14]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [15]
Lodoacetamide azide
 Probe Info  		C414(0.00); C257(0.00); C178(0.00); C171(0.00)  LDD0037  [14]
ATP probe
 Probe Info  		N.A.  LDD0035  [16]
WYneO
 Probe Info  		N.A.  LDD0022  [17]
IPM
 Probe Info  		N.A.  LDD0147  [18]
NHS
 Probe Info  		N.A.  LDD0010  [17]
STPyne
 Probe Info  		N.A.  LDD0009  [17]
TFBX
 Probe Info  		N.A.  LDD0148  [18]
VSF
 Probe Info  		C974(0.00); C414(0.00)  LDD0007  [17]
1c-yne
 Probe Info  		K192(0.00); K854(0.00); K542(0.00)  LDD0228  [19]
Acrolein
 Probe Info  		C414(0.00); C904(0.00)  LDD0217  [20]
W1
 Probe Info  		N.A.  LDD0236  [21]
AOyne
 Probe Info  		5.30  LDD0443  [22]
MPP-AC
 Probe Info  		N.A.  LDD0428  [23]
NAIA_5
 Probe Info  		C171(0.00); C904(0.00); C110(0.00); C178(0.00)  LDD2223  [24]
TPP-AC
 Probe Info  		N.A.  LDD0427  [23]
PAL-AfBPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C140
 Probe Info  		17.75  LDD1822  [25]
FFF probe13
 Probe Info  		12.66  LDD0475  [26]
FFF probe15
 Probe Info  		5.81  LDD0478  [26]
FFF probe3
 Probe Info  		10.16  LDD0464  [26]
FFF probe4
 Probe Info  		13.68  LDD0466  [26]
JN0003
 Probe Info  		19.27  LDD0469  [26]
VE-P
 Probe Info  		N.A.  LDD0396  [27]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C904(0.54)  LDD2095  [6]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C904(1.23)  LDD2130  [6]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C904(1.01)  LDD2117  [6]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C904(1.03)  LDD2152  [6]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C904(0.50)  LDD2132  [6]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C904(1.03)  LDD2131  [6]
 LDCM0025  4SU-RNA HEK-293T C966(3.51)  LDD0168  [8]
 LDCM0026  4SU-RNA+native RNA HEK-293T C974(5.19); C966(6.50)  LDD0169  [8]
 LDCM0214  AC1 HCT 116 C414(1.03)  LDD0531  [11]
 LDCM0215  AC10 HCT 116 C171(0.81); C178(0.81); C414(0.98)  LDD0532  [11]
 LDCM0216  AC100 HEK-293T C974(1.15)  LDD0814  [11]
 LDCM0217  AC101 HEK-293T C974(1.07)  LDD0815  [11]
 LDCM0218  AC102 HEK-293T C974(1.21)  LDD0816  [11]
 LDCM0219  AC103 HEK-293T C974(1.21)  LDD0817  [11]
 LDCM0220  AC104 HEK-293T C974(1.14)  LDD0818  [11]
 LDCM0221  AC105 HEK-293T C974(1.02)  LDD0819  [11]
 LDCM0222  AC106 HEK-293T C974(1.04)  LDD0820  [11]
 LDCM0223  AC107 HEK-293T C974(1.19)  LDD0821  [11]
 LDCM0224  AC108 HEK-293T C974(1.07)  LDD0822  [11]
 LDCM0225  AC109 HEK-293T C974(1.05)  LDD0823  [11]
 LDCM0226  AC11 HCT 116 C171(0.66); C178(0.66); C414(1.04)  LDD0543  [11]
 LDCM0227  AC110 HEK-293T C974(1.38)  LDD0825  [11]
 LDCM0228  AC111 HEK-293T C974(1.51)  LDD0826  [11]
 LDCM0229  AC112 HEK-293T C974(1.50)  LDD0827  [11]
 LDCM0230  AC113 HCT 116 C414(1.06)  LDD0547  [11]
 LDCM0231  AC114 HCT 116 C414(0.93)  LDD0548  [11]
 LDCM0232  AC115 HCT 116 C414(1.02)  LDD0549  [11]
 LDCM0233  AC116 HCT 116 C414(1.02)  LDD0550  [11]
 LDCM0234  AC117 HCT 116 C414(1.20)  LDD0551  [11]
 LDCM0235  AC118 HCT 116 C414(1.03)  LDD0552  [11]
 LDCM0236  AC119 HCT 116 C414(1.02)  LDD0553  [11]
 LDCM0237  AC12 HCT 116 C171(0.80); C178(0.80); C414(0.92)  LDD0554  [11]
 LDCM0238  AC120 HCT 116 C414(0.94)  LDD0555  [11]
 LDCM0239  AC121 HCT 116 C414(0.85)  LDD0556  [11]
 LDCM0240  AC122 HCT 116 C414(0.98)  LDD0557  [11]
 LDCM0241  AC123 HCT 116 C414(0.84)  LDD0558  [11]
 LDCM0242  AC124 HCT 116 C414(0.87)  LDD0559  [11]
 LDCM0243  AC125 HCT 116 C414(0.88)  LDD0560  [11]
 LDCM0244  AC126 HCT 116 C414(0.94)  LDD0561  [11]
 LDCM0245  AC127 HCT 116 C414(0.92)  LDD0562  [11]
 LDCM0246  AC128 HEK-293T C974(0.77)  LDD0844  [11]
 LDCM0247  AC129 HEK-293T C974(0.91)  LDD0845  [11]
 LDCM0249  AC130 HEK-293T C974(1.00)  LDD0847  [11]
 LDCM0250  AC131 HEK-293T C974(0.86)  LDD0848  [11]
 LDCM0251  AC132 HEK-293T C974(0.84)  LDD0849  [11]
 LDCM0252  AC133 HEK-293T C974(1.06)  LDD0850  [11]
 LDCM0253  AC134 HEK-293T C974(1.00)  LDD0851  [11]
 LDCM0254  AC135 HEK-293T C974(1.06)  LDD0852  [11]
 LDCM0255  AC136 HEK-293T C974(1.05)  LDD0853  [11]
 LDCM0256  AC137 HEK-293T C974(1.07)  LDD0854  [11]
 LDCM0257  AC138 HEK-293T C974(1.28)  LDD0855  [11]
 LDCM0258  AC139 HEK-293T C974(0.98)  LDD0856  [11]
 LDCM0259  AC14 HCT 116 C171(0.79); C178(0.79); C414(1.03)  LDD0576  [11]
 LDCM0260  AC140 HEK-293T C974(1.04)  LDD0858  [11]
 LDCM0261  AC141 HEK-293T C974(1.17)  LDD0859  [11]
 LDCM0262  AC142 HEK-293T C974(0.92)  LDD0860  [11]
 LDCM0263  AC143 HEK-293T C178(0.98); C974(1.22)  LDD0861  [11]
 LDCM0264  AC144 HEK-293T C178(0.60); C974(1.20)  LDD0862  [11]
 LDCM0265  AC145 HEK-293T C178(0.76); C974(1.26)  LDD0863  [11]
 LDCM0266  AC146 HEK-293T C178(0.56); C974(1.35)  LDD0864  [11]
 LDCM0267  AC147 HEK-293T C178(0.70); C974(1.52)  LDD0865  [11]
 LDCM0268  AC148 HEK-293T C178(0.42); C974(1.28)  LDD0866  [11]
 LDCM0269  AC149 HEK-293T C178(1.11); C974(1.16)  LDD0867  [11]
 LDCM0270  AC15 HCT 116 C171(0.77); C178(0.77); C414(0.99)  LDD0587  [11]
 LDCM0271  AC150 HEK-293T C178(0.71); C974(1.24)  LDD0869  [11]
 LDCM0272  AC151 HEK-293T C178(0.48); C974(1.26)  LDD0870  [11]
 LDCM0273  AC152 HEK-293T C178(0.54); C974(1.14)  LDD0871  [11]
 LDCM0274  AC153 HEK-293T C178(0.69); C974(1.11)  LDD0872  [11]
 LDCM0621  AC154 HEK-293T C178(0.73); C974(1.04)  LDD2162  [11]
 LDCM0622  AC155 HEK-293T C178(0.65); C974(1.25)  LDD2163  [11]
 LDCM0623  AC156 HEK-293T C178(0.53); C974(1.25)  LDD2164  [11]
 LDCM0624  AC157 HEK-293T C178(0.71); C974(1.49)  LDD2165  [11]
 LDCM0276  AC17 HCT 116 C414(1.05)  LDD0593  [11]
 LDCM0277  AC18 HCT 116 C414(1.06)  LDD0594  [11]
 LDCM0278  AC19 HCT 116 C414(1.17)  LDD0595  [11]
 LDCM0279  AC2 HCT 116 C414(1.10)  LDD0596  [11]
 LDCM0280  AC20 HCT 116 C414(1.08)  LDD0597  [11]
 LDCM0281  AC21 HCT 116 C414(0.96)  LDD0598  [11]
 LDCM0282  AC22 HCT 116 C414(0.94)  LDD0599  [11]
 LDCM0283  AC23 HCT 116 C414(0.84)  LDD0600  [11]
 LDCM0284  AC24 HCT 116 C414(0.96)  LDD0601  [11]
 LDCM0285  AC25 HEK-293T C966(1.02); C974(0.81)  LDD0883  [11]
 LDCM0286  AC26 HEK-293T C966(0.92); C974(0.77)  LDD0884  [11]
 LDCM0287  AC27 HEK-293T C966(0.99); C974(0.88)  LDD0885  [11]
 LDCM0288  AC28 HEK-293T C966(0.74); C974(0.84)  LDD0886  [11]
 LDCM0289  AC29 HEK-293T C966(1.02); C974(0.91)  LDD0887  [11]
 LDCM0290  AC3 HCT 116 C414(0.96)  LDD0607  [11]
 LDCM0291  AC30 HEK-293T C966(0.93); C974(0.77)  LDD0889  [11]
 LDCM0292  AC31 HEK-293T C966(0.76); C974(0.72)  LDD0890  [11]
 LDCM0293  AC32 HEK-293T C966(0.95); C974(0.77)  LDD0891  [11]
 LDCM0294  AC33 HEK-293T C966(0.90); C974(0.81)  LDD0892  [11]
 LDCM0295  AC34 HEK-293T C966(0.82); C974(0.75)  LDD0893  [11]
 LDCM0296  AC35 HCT 116 C171(1.11); C178(1.11)  LDD0613  [11]
 LDCM0297  AC36 HCT 116 C171(1.03); C178(1.03)  LDD0614  [11]
 LDCM0298  AC37 HCT 116 C171(1.42); C178(1.42)  LDD0615  [11]
 LDCM0299  AC38 HCT 116 C171(1.28); C178(1.28)  LDD0616  [11]
 LDCM0300  AC39 HCT 116 C171(1.00); C178(1.00)  LDD0617  [11]
 LDCM0301  AC4 HCT 116 C414(1.04)  LDD0618  [11]
 LDCM0302  AC40 HCT 116 C171(0.88); C178(0.88)  LDD0619  [11]
 LDCM0303  AC41 HCT 116 C171(0.93); C178(0.93)  LDD0620  [11]
 LDCM0304  AC42 HCT 116 C171(0.91); C178(0.91)  LDD0621  [11]
 LDCM0305  AC43 HCT 116 C171(1.32); C178(1.32)  LDD0622  [11]
 LDCM0306  AC44 HCT 116 C171(1.11); C178(1.11)  LDD0623  [11]
 LDCM0307  AC45 HCT 116 C171(0.63); C178(0.63)  LDD0624  [11]
 LDCM0308  AC46 HCT 116 C171(1.28); C178(1.28); C414(1.31)  LDD0625  [11]
 LDCM0309  AC47 HCT 116 C414(0.83); C171(1.15); C178(1.15)  LDD0626  [11]
 LDCM0310  AC48 HCT 116 C414(1.35); C171(1.90); C178(1.90)  LDD0627  [11]
 LDCM0311  AC49 HCT 116 C414(0.85); C171(1.32); C178(1.32)  LDD0628  [11]
 LDCM0312  AC5 HCT 116 C414(1.03)  LDD0629  [11]
 LDCM0313  AC50 HCT 116 C414(1.02); C171(1.90); C178(1.90)  LDD0630  [11]
 LDCM0314  AC51 HCT 116 C171(1.04); C178(1.04); C414(1.10)  LDD0631  [11]
 LDCM0315  AC52 HCT 116 C414(0.90); C171(1.05); C178(1.05)  LDD0632  [11]
 LDCM0316  AC53 HCT 116 C414(1.02); C171(1.40); C178(1.40)  LDD0633  [11]
 LDCM0317  AC54 HCT 116 C414(1.00); C171(1.05); C178(1.05)  LDD0634  [11]
 LDCM0318  AC55 HCT 116 C414(0.91); C171(1.79); C178(1.79)  LDD0635  [11]
 LDCM0319  AC56 HCT 116 C414(0.74); C171(2.92); C178(2.92)  LDD0636  [11]
 LDCM0320  AC57 HCT 116 C414(0.92); C171(1.14); C178(1.14)  LDD0637  [11]
 LDCM0321  AC58 HCT 116 C414(0.84); C171(1.12); C178(1.12)  LDD0638  [11]
 LDCM0322  AC59 HCT 116 C171(0.86); C178(0.86); C414(1.15)  LDD0639  [11]
 LDCM0323  AC6 HCT 116 C171(0.81); C178(0.81); C414(1.02)  LDD0640  [11]
 LDCM0324  AC60 HCT 116 C414(0.98); C171(1.16); C178(1.16)  LDD0641  [11]
 LDCM0325  AC61 HCT 116 C414(1.05); C171(1.25); C178(1.25)  LDD0642  [11]
 LDCM0326  AC62 HCT 116 C171(0.92); C178(0.92); C414(1.06)  LDD0643  [11]
 LDCM0327  AC63 HCT 116 C414(0.99); C171(1.05); C178(1.05)  LDD0644  [11]
 LDCM0328  AC64 HCT 116 C414(1.05); C171(1.13); C178(1.13)  LDD0645  [11]
 LDCM0329  AC65 HCT 116 C414(0.93); C171(1.28); C178(1.28)  LDD0646  [11]
 LDCM0330  AC66 HCT 116 C414(0.89); C171(1.30); C178(1.30)  LDD0647  [11]
 LDCM0331  AC67 HCT 116 C171(1.03); C178(1.03); C414(1.03)  LDD0648  [11]
 LDCM0332  AC68 HCT 116 C414(0.97); C171(1.12); C178(1.12)  LDD0649  [11]
 LDCM0333  AC69 HCT 116 C414(1.05); C171(1.32); C178(1.32)  LDD0650  [11]
 LDCM0334  AC7 HCT 116 C171(0.69); C178(0.69); C414(0.96)  LDD0651  [11]
 LDCM0335  AC70 HCT 116 C414(0.69); C171(0.79); C178(0.79)  LDD0652  [11]
 LDCM0336  AC71 HCT 116 C171(1.02); C178(1.02); C414(1.13)  LDD0653  [11]
 LDCM0337  AC72 HCT 116 C414(0.81); C171(1.59); C178(1.59)  LDD0654  [11]
 LDCM0338  AC73 HCT 116 C414(0.54); C171(1.18); C178(1.18)  LDD0655  [11]
 LDCM0339  AC74 HCT 116 C414(0.57); C171(1.15); C178(1.15)  LDD0656  [11]
 LDCM0340  AC75 HCT 116 C414(0.42); C171(1.09); C178(1.09)  LDD0657  [11]
 LDCM0341  AC76 HCT 116 C414(0.75); C171(1.22); C178(1.22)  LDD0658  [11]
 LDCM0342  AC77 HCT 116 C414(0.68); C171(1.14); C178(1.14)  LDD0659  [11]
 LDCM0343  AC78 HCT 116 C414(0.94); C171(1.21); C178(1.21)  LDD0660  [11]
 LDCM0344  AC79 HCT 116 C414(1.06); C171(1.16); C178(1.16)  LDD0661  [11]
 LDCM0345  AC8 HCT 116 C171(0.80); C178(0.80); C414(0.87)  LDD0662  [11]
 LDCM0346  AC80 HCT 116 C414(0.94); C171(0.95); C178(0.95)  LDD0663  [11]
 LDCM0347  AC81 HCT 116 C171(0.29); C178(0.29); C414(0.86)  LDD0664  [11]
 LDCM0348  AC82 HCT 116 C414(0.33); C171(0.73); C178(0.73)  LDD0665  [11]
 LDCM0349  AC83 HCT 116 C414(0.96)  LDD0666  [11]
 LDCM0350  AC84 HCT 116 C414(0.98)  LDD0667  [11]
 LDCM0351  AC85 HCT 116 C414(1.03)  LDD0668  [11]
 LDCM0352  AC86 HCT 116 C414(0.91)  LDD0669  [11]
 LDCM0353  AC87 HCT 116 C414(1.00)  LDD0670  [11]
 LDCM0354  AC88 HCT 116 C414(0.93)  LDD0671  [11]
 LDCM0355  AC89 HCT 116 C414(0.96)  LDD0672  [11]
 LDCM0357  AC90 HCT 116 C414(0.97)  LDD0674  [11]
 LDCM0358  AC91 HCT 116 C414(0.92)  LDD0675  [11]
 LDCM0359  AC92 HCT 116 C414(0.91)  LDD0676  [11]
 LDCM0360  AC93 HCT 116 C414(0.99)  LDD0677  [11]
 LDCM0361  AC94 HCT 116 C414(0.98)  LDD0678  [11]
 LDCM0362  AC95 HCT 116 C414(0.98)  LDD0679  [11]
 LDCM0363  AC96 HCT 116 C414(1.02)  LDD0680  [11]
 LDCM0364  AC97 HCT 116 C414(0.95)  LDD0681  [11]
 LDCM0365  AC98 HEK-293T C974(1.06)  LDD0963  [11]
 LDCM0366  AC99 HEK-293T C974(1.05)  LDD0964  [11]
 LDCM0545  Acetamide MDA-MB-231 C904(1.18)  LDD2138  [6]
 LDCM0248  AKOS034007472 HCT 116 C171(1.03); C178(1.03); C414(1.16)  LDD0565  [11]
 LDCM0356  AKOS034007680 HCT 116 C171(0.85); C178(0.85); C414(0.86)  LDD0673  [11]
 LDCM0275  AKOS034007705 HCT 116 C171(0.28); C178(0.28); C414(0.94)  LDD0592  [11]
 LDCM0156  Aniline NCI-H1299 N.A.  LDD0405  [1]
 LDCM0498  BS-3668 MDA-MB-231 C904(0.44)  LDD2091  [6]
 LDCM0630  CCW28-3 231MFP C974(1.57)  LDD2214  [28]
 LDCM0108  Chloroacetamide HeLa C904(0.00); H957(0.00)  LDD0222  [20]
 LDCM0367  CL1 HCT 116 C414(0.93); C171(1.03); C178(1.03)  LDD0684  [11]
 LDCM0368  CL10 HCT 116 C414(0.89); C171(1.00); C178(1.00)  LDD0685  [11]
 LDCM0369  CL100 HCT 116 C414(1.06)  LDD0686  [11]
 LDCM0370  CL101 HCT 116 C171(0.62); C178(0.62); C414(1.07)  LDD0687  [11]
 LDCM0371  CL102 HCT 116 C171(0.66); C178(0.66); C414(1.10)  LDD0688  [11]
 LDCM0372  CL103 HCT 116 C171(0.76); C178(0.76); C414(1.19)  LDD0689  [11]
 LDCM0373  CL104 HCT 116 C171(0.77); C178(0.77); C414(1.00)  LDD0690  [11]
 LDCM0374  CL105 HCT 116 C414(0.97)  LDD0691  [11]
 LDCM0375  CL106 HCT 116 C414(1.05)  LDD0692  [11]
 LDCM0376  CL107 HCT 116 C414(1.02)  LDD0693  [11]
 LDCM0377  CL108 HCT 116 C414(0.81)  LDD0694  [11]
 LDCM0378  CL109 HCT 116 C414(0.99)  LDD0695  [11]
 LDCM0379  CL11 HCT 116 C414(0.70); C171(0.70); C178(0.70)  LDD0696  [11]
 LDCM0380  CL110 HCT 116 C414(1.07)  LDD0697  [11]
 LDCM0381  CL111 HCT 116 C414(0.94)  LDD0698  [11]
 LDCM0382  CL112 HEK-293T C966(1.15); C974(0.82)  LDD0980  [11]
 LDCM0383  CL113 HEK-293T C966(0.86); C974(0.77)  LDD0981  [11]
 LDCM0384  CL114 HEK-293T C966(1.44); C974(1.09)  LDD0982  [11]
 LDCM0385  CL115 HEK-293T C966(1.17); C974(0.89)  LDD0983  [11]
 LDCM0386  CL116 HEK-293T C966(1.00); C974(0.85)  LDD0984  [11]
 LDCM0387  CL117 HCT 116 C171(0.51); C178(0.51)  LDD0704  [11]
 LDCM0388  CL118 HCT 116 C171(0.98); C178(0.98)  LDD0705  [11]
 LDCM0389  CL119 HCT 116 C171(0.97); C178(0.97)  LDD0706  [11]
 LDCM0390  CL12 HCT 116 C414(0.73); C171(0.78); C178(0.78)  LDD0707  [11]
 LDCM0391  CL120 HCT 116 C171(1.00); C178(1.00)  LDD0708  [11]
 LDCM0392  CL121 HCT 116 C171(0.73); C178(0.73); C414(0.85)  LDD0709  [11]
 LDCM0393  CL122 HCT 116 C414(1.06); C171(1.56); C178(1.56)  LDD0710  [11]
 LDCM0394  CL123 HCT 116 C414(0.96); C171(1.55); C178(1.55)  LDD0711  [11]
 LDCM0395  CL124 HCT 116 C414(0.92); C171(1.60); C178(1.60)  LDD0712  [11]
 LDCM0396  CL125 HCT 116 C171(0.88); C178(0.88); C414(1.01)  LDD0713  [11]
 LDCM0397  CL126 HCT 116 C414(0.89); C171(0.97); C178(0.97)  LDD0714  [11]
 LDCM0398  CL127 HCT 116 C414(1.09); C171(1.16); C178(1.16)  LDD0715  [11]
 LDCM0399  CL128 HCT 116 C414(0.98); C171(1.19); C178(1.19)  LDD0716  [11]
 LDCM0400  CL13 HCT 116 C414(1.00); C171(1.06); C178(1.06)  LDD0717  [11]
 LDCM0401  CL14 HCT 116 C414(1.00); C171(1.13); C178(1.13)  LDD0718  [11]
 LDCM0402  CL15 HCT 116 C414(0.92); C171(1.16); C178(1.16)  LDD0719  [11]
 LDCM0403  CL16 HCT 116 C171(0.80); C178(0.80)  LDD0720  [11]
 LDCM0404  CL17 HCT 116 C171(0.93); C178(0.93)  LDD0721  [11]
 LDCM0405  CL18 HCT 116 C171(1.18); C178(1.18)  LDD0722  [11]
 LDCM0406  CL19 HCT 116 C171(1.17); C178(1.17)  LDD0723  [11]
 LDCM0407  CL2 HCT 116 C414(0.95); C171(1.14); C178(1.14)  LDD0724  [11]
 LDCM0408  CL20 HCT 116 C171(0.88); C178(0.88)  LDD0725  [11]
 LDCM0409  CL21 HCT 116 C171(0.71); C178(0.71)  LDD0726  [11]
 LDCM0410  CL22 HCT 116 C171(0.71); C178(0.71)  LDD0727  [11]
 LDCM0411  CL23 HCT 116 C171(0.93); C178(0.93)  LDD0728  [11]
 LDCM0412  CL24 HCT 116 C171(0.70); C178(0.70)  LDD0729  [11]
 LDCM0413  CL25 HCT 116 C171(0.73); C178(0.73)  LDD0730  [11]
 LDCM0414  CL26 HCT 116 C171(1.05); C178(1.05)  LDD0731  [11]
 LDCM0415  CL27 HCT 116 C171(0.90); C178(0.90)  LDD0732  [11]
 LDCM0416  CL28 HCT 116 C171(0.86); C178(0.86)  LDD0733  [11]
 LDCM0417  CL29 HCT 116 C171(0.90); C178(0.90)  LDD0734  [11]
 LDCM0418  CL3 HCT 116 C171(0.99); C178(0.99); C414(0.98)  LDD0735  [11]
 LDCM0419  CL30 HCT 116 C171(0.91); C178(0.91)  LDD0736  [11]
 LDCM0420  CL31 HCT 116 C171(0.85)  LDD0737  [11]
 LDCM0421  CL32 HCT 116 C171(1.07)  LDD0738  [11]
 LDCM0422  CL33 HCT 116 C171(1.01)  LDD0739  [11]
 LDCM0423  CL34 HCT 116 C171(0.53)  LDD0740  [11]
 LDCM0424  CL35 HCT 116 C171(0.46)  LDD0741  [11]
 LDCM0425  CL36 HCT 116 C171(0.61)  LDD0742  [11]
 LDCM0426  CL37 HCT 116 C171(0.49)  LDD0743  [11]
 LDCM0428  CL39 HCT 116 C171(0.55)  LDD0745  [11]
 LDCM0429  CL4 HCT 116 C171(1.28); C178(1.28); C414(0.92)  LDD0746  [11]
 LDCM0430  CL40 HCT 116 C171(0.54)  LDD0747  [11]
 LDCM0431  CL41 HCT 116 C171(0.72)  LDD0748  [11]
 LDCM0432  CL42 HCT 116 C171(0.37)  LDD0749  [11]
 LDCM0433  CL43 HCT 116 C171(0.52)  LDD0750  [11]
 LDCM0434  CL44 HCT 116 C171(0.77)  LDD0751  [11]
 LDCM0435  CL45 HCT 116 C171(0.53)  LDD0752  [11]
 LDCM0436  CL46 HCT 116 C414(0.94)  LDD0753  [11]
 LDCM0437  CL47 HCT 116 C414(0.87)  LDD0754  [11]
 LDCM0438  CL48 HCT 116 C414(0.86)  LDD0755  [11]
 LDCM0439  CL49 HCT 116 C414(0.82)  LDD0756  [11]
 LDCM0440  CL5 HCT 116 C171(1.08); C178(1.08); C414(1.23)  LDD0757  [11]
 LDCM0441  CL50 HCT 116 C414(0.90)  LDD0758  [11]
 LDCM0442  CL51 HCT 116 C414(0.92)  LDD0759  [11]
 LDCM0443  CL52 HCT 116 C414(0.93)  LDD0760  [11]
 LDCM0444  CL53 HCT 116 C414(0.88)  LDD0761  [11]
 LDCM0445  CL54 HCT 116 C414(0.85)  LDD0762  [11]
 LDCM0446  CL55 HCT 116 C414(0.85)  LDD0763  [11]
 LDCM0447  CL56 HCT 116 C414(0.88)  LDD0764  [11]
 LDCM0448  CL57 HCT 116 C414(0.92)  LDD0765  [11]
 LDCM0449  CL58 HCT 116 C414(0.86)  LDD0766  [11]
 LDCM0450  CL59 HCT 116 C414(0.90)  LDD0767  [11]
 LDCM0451  CL6 HCT 116 C171(1.29); C178(1.29); C414(1.06)  LDD0768  [11]
 LDCM0452  CL60 HCT 116 C414(0.80)  LDD0769  [11]
 LDCM0453  CL61 HCT 116 C414(0.98)  LDD0770  [11]
 LDCM0454  CL62 HCT 116 C414(0.86)  LDD0771  [11]
 LDCM0455  CL63 HCT 116 C414(0.96)  LDD0772  [11]
 LDCM0456  CL64 HCT 116 C414(0.91)  LDD0773  [11]
 LDCM0457  CL65 HCT 116 C414(1.04)  LDD0774  [11]
 LDCM0458  CL66 HCT 116 C414(0.73)  LDD0775  [11]
 LDCM0459  CL67 HCT 116 C414(0.83)  LDD0776  [11]
 LDCM0460  CL68 HCT 116 C414(0.91)  LDD0777  [11]
 LDCM0461  CL69 HCT 116 C414(1.09)  LDD0778  [11]
 LDCM0462  CL7 HCT 116 C171(0.74); C178(0.74); C414(0.86)  LDD0779  [11]
 LDCM0463  CL70 HCT 116 C414(0.99)  LDD0780  [11]
 LDCM0464  CL71 HCT 116 C414(0.88)  LDD0781  [11]
 LDCM0465  CL72 HCT 116 C414(0.93)  LDD0782  [11]
 LDCM0466  CL73 HCT 116 C414(0.89)  LDD0783  [11]
 LDCM0467  CL74 HCT 116 C414(0.83)  LDD0784  [11]
 LDCM0469  CL76 HCT 116 C171(1.29); C178(1.21); C414(1.09)  LDD0786  [11]
 LDCM0470  CL77 HCT 116 C171(1.16); C178(1.02); C414(0.98)  LDD0787  [11]
 LDCM0471  CL78 HCT 116 C171(1.11); C178(0.99); C414(1.08)  LDD0788  [11]
 LDCM0472  CL79 HCT 116 C171(0.79); C178(0.81); C414(0.85)  LDD0789  [11]
 LDCM0473  CL8 HCT 116 C171(0.76); C178(0.76); C414(0.69)  LDD0790  [11]
 LDCM0474  CL80 HCT 116 C171(1.26); C178(1.09); C414(1.05)  LDD0791  [11]
 LDCM0475  CL81 HCT 116 C171(1.17); C178(1.11); C414(1.01)  LDD0792  [11]
 LDCM0476  CL82 HCT 116 C171(0.65); C178(0.73); C414(0.59)  LDD0793  [11]
 LDCM0477  CL83 HCT 116 C171(0.74); C178(0.72); C414(0.69)  LDD0794  [11]
 LDCM0478  CL84 HCT 116 C171(0.61); C178(0.69); C414(0.60)  LDD0795  [11]
 LDCM0479  CL85 HCT 116 C171(1.05); C178(1.03); C414(1.23)  LDD0796  [11]
 LDCM0480  CL86 HCT 116 C171(1.36); C178(1.17); C414(1.21)  LDD0797  [11]
 LDCM0481  CL87 HCT 116 C171(1.07); C178(0.97); C414(1.17)  LDD0798  [11]
 LDCM0482  CL88 HCT 116 C171(0.69); C178(0.81); C414(0.75)  LDD0799  [11]
 LDCM0483  CL89 HCT 116 C171(0.49); C178(0.62); C414(0.58)  LDD0800  [11]
 LDCM0484  CL9 HCT 116 C171(1.00); C178(1.00); C414(1.02)  LDD0801  [11]
 LDCM0485  CL90 HCT 116 C171(1.22); C178(1.02); C414(0.82)  LDD0802  [11]
 LDCM0486  CL91 HCT 116 C414(0.91)  LDD0803  [11]
 LDCM0487  CL92 HCT 116 C414(0.86)  LDD0804  [11]
 LDCM0488  CL93 HCT 116 C414(0.90)  LDD0805  [11]
 LDCM0489  CL94 HCT 116 C414(1.04)  LDD0806  [11]
 LDCM0490  CL95 HCT 116 C414(0.83)  LDD0807  [11]
 LDCM0491  CL96 HCT 116 C414(1.04)  LDD0808  [11]
 LDCM0492  CL97 HCT 116 C414(1.09)  LDD0809  [11]
 LDCM0493  CL98 HCT 116 C414(0.95)  LDD0810  [11]
 LDCM0494  CL99 HCT 116 C414(1.03)  LDD0811  [11]
 LDCM0185  Compound 17 HEK-293T 5.17  LDD0512  [26]
 LDCM0191  Compound 21 HEK-293T 5.21  LDD0508  [26]
 LDCM0190  Compound 34 HEK-293T 4.56  LDD0510  [26]
 LDCM0192  Compound 35 HEK-293T 4.27  LDD0509  [26]
 LDCM0193  Compound 36 HEK-293T 3.92  LDD0511  [26]
 LDCM0495  E2913 HEK-293T C110(1.09); C178(0.99); C974(0.76); C171(0.88)  LDD1698  [29]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C904(0.56)  LDD1702  [6]
 LDCM0031  Epigallocatechin gallate HEK-293T 9.56  LDD0183  [7]
 LDCM0625  F8 Ramos C904(1.11); 0.21  LDD2187  [30]
 LDCM0572  Fragment10 Ramos C904(0.61)  LDD2189  [30]
 LDCM0573  Fragment11 Ramos C904(7.04)  LDD2190  [30]
 LDCM0574  Fragment12 Ramos C904(0.65)  LDD2191  [30]
 LDCM0575  Fragment13 Ramos C904(1.13)  LDD2192  [30]
 LDCM0576  Fragment14 Ramos C904(0.28); 1.55  LDD2193  [30]
 LDCM0579  Fragment20 Ramos C904(0.55)  LDD2194  [30]
 LDCM0580  Fragment21 Ramos C904(0.88)  LDD2195  [30]
 LDCM0582  Fragment23 Ramos C904(1.02)  LDD2196  [30]
 LDCM0578  Fragment27 Ramos C904(1.12)  LDD2197  [30]
 LDCM0586  Fragment28 Ramos C904(0.55); 0.93  LDD2198  [30]
 LDCM0588  Fragment30 Ramos C904(1.60)  LDD2199  [30]
 LDCM0589  Fragment31 Ramos C904(1.05)  LDD2200  [30]
 LDCM0590  Fragment32 Ramos C904(0.78)  LDD2201  [30]
 LDCM0468  Fragment33 HCT 116 C414(0.94)  LDD0785  [11]
 LDCM0596  Fragment38 Ramos C904(1.09)  LDD2203  [30]
 LDCM0566  Fragment4 Ramos C904(0.53); 0.28  LDD2184  [30]
 LDCM0427  Fragment51 HCT 116 C171(0.34)  LDD0744  [11]
 LDCM0610  Fragment52 Ramos C904(1.76)  LDD2204  [30]
 LDCM0614  Fragment56 Ramos C904(1.34)  LDD2205  [30]
 LDCM0569  Fragment7 Ramos C904(0.48)  LDD2186  [30]
 LDCM0571  Fragment9 Ramos C904(0.42)  LDD2188  [30]
 LDCM0116  HHS-0101 DM93 Y831(1.02)  LDD0264  [9]
 LDCM0117  HHS-0201 DM93 Y831(0.87)  LDD0265  [9]
 LDCM0118  HHS-0301 DM93 Y831(1.60)  LDD0266  [9]
 LDCM0119  HHS-0401 DM93 Y831(0.87)  LDD0267  [9]
 LDCM0120  HHS-0701 DM93 Y831(0.99)  LDD0268  [9]
 LDCM0107  IAA HeLa N.A.  LDD0221  [20]
 LDCM0022  KB02 HEK-293T C904(0.93); C414(0.96); C178(0.92); C171(1.02)  LDD1492  [29]
 LDCM0023  KB03 HEK-293T C904(1.01); C414(0.93); C178(0.93); C171(1.01)  LDD1497  [29]
 LDCM0024  KB05 MKN45 C904(1.10)  LDD3332  [31]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C904(0.70)  LDD2089  [6]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C904(0.85)  LDD2093  [6]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C904(0.74)  LDD2099  [6]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C904(0.97)  LDD2101  [6]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C904(0.99)  LDD2107  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C904(0.61)  LDD2109  [6]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C904(0.67)  LDD2111  [6]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C904(1.30)  LDD2119  [6]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C904(0.72)  LDD2123  [6]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C904(0.74)  LDD2125  [6]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C904(0.86)  LDD2127  [6]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C904(0.85)  LDD2129  [6]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C904(0.44)  LDD2134  [6]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C904(0.87)  LDD2135  [6]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C904(1.04)  LDD2136  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C904(0.91)  LDD2137  [6]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C904(1.07)  LDD1700  [6]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C904(0.87)  LDD2140  [6]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C904(0.60)  LDD2146  [6]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C904(0.41)  LDD2148  [6]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C904(0.31)  LDD2150  [6]
 LDCM0170  Structure8 Ramos 5.21  LDD0433  [32]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

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
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-C motif chemokine 3 (CCL3) Intercrine beta (chemokine CC) family P10147
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Islet amyloid polypeptide (IAPP) Calcitonin family P10997
Pro-glucagon (GCG) Glucagon family P01275
Insulin (INS) Insulin family P01308

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Insulin Detemir BiotechDrug DB01307
Insulin Human BiotechDrug DB00030
Insulin Lispro BiotechDrug DB00046
Insulin Pork BiotechDrug DB00071
Bacitracin Small molecular drug D0M1IO
Insulin Beef . DB09456
Insulin Degludec . DB09564
Zinc Acetate . DB14487
Zinc Chloride . DB14533
Zinc Sulfate Unspecified Form . DB14548
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pro-001 . D0K6HE
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gnf-pf-4478 Small molecular drug D06DKB
Nte-1 Small molecular drug D0N9YP
Nte-2 Small molecular drug D0N0ED
Quinoline 2 Small molecular drug D0E9JD

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 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.
3 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
4 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
5 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.
6 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
7 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
8 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
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 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.
11 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.
12 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
13 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.
14 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
15 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
16 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
17 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
18 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
19 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.
20 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.
21 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.
22 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.
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 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
25 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
26 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.
27 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.
28 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.
29 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
30 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
31 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
32 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.