Details of the Target

General Information of Target

Target ID LDTP02235
Target Name Fumarate hydratase, mitochondrial (FH)
Gene Name FH
Gene ID 2271
Synonyms
Fumarate hydratase, mitochondrial; Fumarase; HsFH; EC 4.2.1.2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MYRALRLLARSRPLVRAPAAALASAPGLGGAAVPSFWPPNAARMASQNSFRIEYDTFGEL
KVPNDKYYGAQTVRSTMNFKIGGVTERMPTPVIKAFGILKRAAAEVNQDYGLDPKIANAI
MKAADEVAEGKLNDHFPLVVWQTGSGTQTNMNVNEVISNRAIEMLGGELGSKIPVHPNDH
VNKSQSSNDTFPTAMHIAAAIEVHEVLLPGLQKLHDALDAKSKEFAQIIKIGRTHTQDAV
PLTLGQEFSGYVQQVKYAMTRIKAAMPRIYELAAGGTAVGTGLNTRIGFAEKVAAKVAAL
TGLPFVTAPNKFEALAAHDALVELSGAMNTTACSLMKIANDIRFLGSGPRSGLGELILPE
NEPGSSIMPGKVNPTQCEAMTMVAAQVMGNHVAVTVGGSNGHFELNVFKPMMIKNVLHSA
RLLGDASVSFTENCVVGIQANTERINKLMNESLMLVTALNPHIGYDKAAKIAKTAHKNGS
TLKETAIELGYLTAEQFDEWVKPKDMLGPK
Target Bioclass
Enzyme
Family
Class-II fumarase/aspartase family, Fumarase subfamily
Subcellular location
Cytoplasm, cytosol; Mitochondrion
Function
Catalyzes the reversible stereospecific interconversion of fumarate to L-malate. Experiments in other species have demonstrated that specific isoforms of this protein act in defined pathways and favor one direction over the other (Probable).; [Isoform Mitochondrial]: Catalyzes the hydration of fumarate to L-malate in the tricarboxylic acid (TCA) cycle to facilitate a transition step in the production of energy in the form of NADH.; [Isoform Cytoplasmic]: Catalyzes the dehydration of L-malate to fumarate. Fumarate metabolism in the cytosol plays a role during urea cycle and arginine metabolism; fumarate being a by-product of the urea cycle and amino-acid catabolism. Also plays a role in DNA repair by promoting non-homologous end-joining (NHEJ). In response to DNA damage and phosphorylation by PRKDC, translocates to the nucleus and accumulates at DNA double-strand breaks (DSBs): acts by catalyzing formation of fumarate, an inhibitor of KDM2B histone demethylase activity, resulting in enhanced dimethylation of histone H3 'Lys-36' (H3K36me2).
Uniprot ID
P07954
Ensemble ID
ENST00000366560.4
HGNC ID
HGNC:3700

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
IGROV1 SNV: p.A45T DBIA    Probe Info 
OVKATE SNV: p.H204Y .

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
A-EBA
 Probe Info  		2.84  LDD0215  [1]
CY4
 Probe Info  		100.00  LDD0244  [2]
N1
 Probe Info  		100.00  LDD0242  [2]
C-Sul
 Probe Info  		3.52  LDD0066  [3]
TH216
 Probe Info  		Y67(5.46)  LDD0259  [4]
YN-1
 Probe Info  		100.00  LDD0444  [5]
STPyne
 Probe Info  		K100(5.00); K115(0.98); K122(0.91); K172(5.00)  LDD0277  [6]
AZ-9
 Probe Info  		E59(0.88)  LDD2208  [7]
OPA-S-S-alkyne
 Probe Info  		K80(1.87); K66(2.79)  LDD3494  [8]
Probe 1
 Probe Info  		Y54(66.32); Y110(11.55)  LDD3495  [9]
DBIA
 Probe Info  		C333(4.86)  LDD0209  [10]
HHS-482
 Probe Info  		Y465(1.08)  LDD0285  [11]
HHS-475
 Probe Info  		Y491(0.74); Y67(0.83); Y54(0.98); Y465(1.03)  LDD0264  [12]
HHS-465
 Probe Info  		Y465(9.40)  LDD2237  [13]
5E-2FA
 Probe Info  		H318(0.00); H180(0.00); H176(0.00); H462(0.00)  LDD2235  [14]
ATP probe
 Probe Info  		K61(0.00); K223(0.00)  LDD0199  [15]
m-APA
 Probe Info  		H462(0.00); H135(0.00); H196(0.00); H476(0.00)  LDD2231  [14]
4-Iodoacetamidophenylacetylene
 Probe Info  		C333(0.00); C434(0.00); C377(0.00)  LDD0038  [16]
IA-alkyne
 Probe Info  		C333(0.00); C377(0.00); C434(0.00)  LDD0036  [16]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [17]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [17]
Lodoacetamide azide
 Probe Info  		C434(0.00); C333(0.00); C377(0.00)  LDD0037  [16]
ATP probe
 Probe Info  		K94(0.00); K292(0.00)  LDD0035  [18]
NAIA_4
 Probe Info  		N.A.  LDD2226  [19]
IPM
 Probe Info  		N.A.  LDD2156  [20]
NHS
 Probe Info  		K61(0.00); K296(0.00); K292(0.00); K122(0.00)  LDD0010  [21]
SF
 Probe Info  		Y68(0.00); K473(0.00); Y54(0.00); K292(0.00)  LDD0028  [22]
Ox-W18
 Probe Info  		N.A.  LDD2175  [23]
1c-yne
 Probe Info  		K115(0.00); K131(0.00); K447(0.00); K256(0.00)  LDD0228  [24]
Acrolein
 Probe Info  		H176(0.00); H462(0.00)  LDD0217  [25]
Crotonaldehyde
 Probe Info  		H180(0.00); H176(0.00)  LDD0219  [25]
NAIA_5
 Probe Info  		C333(0.00); C377(0.00)  LDD2223  [19]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe4
 Probe Info  		20.00  LDD0466  [26]
JN0003
 Probe Info  		20.00  LDD0469  [26]
VE-P
 Probe Info  		N.A.  LDD0396  [27]
DA-2
 Probe Info  		N.A.  LDD0070  [28]
STS-1
 Probe Info  		N.A.  LDD0069  [29]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C333(0.98); C434(1.24)  LDD1507  [30]
 LDCM0215  AC10 HEK-293T C333(1.04); C434(1.01)  LDD1508  [30]
 LDCM0226  AC11 HEK-293T C333(0.96); C434(1.22)  LDD1509  [30]
 LDCM0237  AC12 HEK-293T C333(0.97); C434(1.00); C377(1.04)  LDD1510  [30]
 LDCM0259  AC14 HEK-293T C333(1.01); C434(1.06); C377(1.23)  LDD1512  [30]
 LDCM0270  AC15 HEK-293T C333(0.97); C434(1.20)  LDD1513  [30]
 LDCM0276  AC17 HEK-293T C333(1.05); C434(1.02)  LDD1515  [30]
 LDCM0277  AC18 HEK-293T C333(1.02); C434(1.03)  LDD1516  [30]
 LDCM0278  AC19 HEK-293T C333(0.85); C434(1.01)  LDD1517  [30]
 LDCM0279  AC2 HEK-293T C333(1.02); C434(1.07)  LDD1518  [30]
 LDCM0280  AC20 HEK-293T C333(0.99); C434(1.09); C377(1.12)  LDD1519  [30]
 LDCM0281  AC21 HEK-293T C333(0.99); C434(1.00)  LDD1520  [30]
 LDCM0282  AC22 HEK-293T C333(1.07); C434(1.08); C377(1.24)  LDD1521  [30]
 LDCM0283  AC23 HEK-293T C333(0.99); C434(0.92)  LDD1522  [30]
 LDCM0284  AC24 HEK-293T C333(0.99); C434(1.06); C377(1.12)  LDD1523  [30]
 LDCM0285  AC25 HEK-293T C333(1.01); C434(1.09)  LDD1524  [30]
 LDCM0286  AC26 HEK-293T C333(1.03); C434(0.99)  LDD1525  [30]
 LDCM0287  AC27 HEK-293T C333(0.96); C434(1.12)  LDD1526  [30]
 LDCM0288  AC28 HEK-293T C333(0.96); C434(0.96); C377(0.96)  LDD1527  [30]
 LDCM0289  AC29 HEK-293T C333(0.98); C434(1.01)  LDD1528  [30]
 LDCM0290  AC3 HEK-293T C333(0.96); C434(0.99)  LDD1529  [30]
 LDCM0291  AC30 HEK-293T C333(0.94); C434(1.13); C377(1.08)  LDD1530  [30]
 LDCM0292  AC31 HEK-293T C333(0.95); C434(1.23)  LDD1531  [30]
 LDCM0293  AC32 HEK-293T C333(0.94); C434(0.92); C377(1.19)  LDD1532  [30]
 LDCM0294  AC33 HEK-293T C333(0.99); C434(0.95)  LDD1533  [30]
 LDCM0295  AC34 HEK-293T C333(0.99); C434(1.07)  LDD1534  [30]
 LDCM0296  AC35 HEK-293T C333(0.96); C434(0.99)  LDD1535  [30]
 LDCM0297  AC36 HEK-293T C333(1.04); C434(0.94); C377(1.04)  LDD1536  [30]
 LDCM0298  AC37 HEK-293T C333(0.95); C434(1.10)  LDD1537  [30]
 LDCM0299  AC38 HEK-293T C333(0.96); C434(1.31); C377(0.98)  LDD1538  [30]
 LDCM0300  AC39 HEK-293T C333(0.99); C434(1.26)  LDD1539  [30]
 LDCM0301  AC4 HEK-293T C333(1.03); C434(1.02); C377(1.15)  LDD1540  [30]
 LDCM0302  AC40 HEK-293T C333(1.00); C434(1.06); C377(1.19)  LDD1541  [30]
 LDCM0303  AC41 HEK-293T C333(1.00); C434(0.98)  LDD1542  [30]
 LDCM0304  AC42 HEK-293T C333(0.99); C434(1.04)  LDD1543  [30]
 LDCM0305  AC43 HEK-293T C333(0.97); C434(1.05)  LDD1544  [30]
 LDCM0306  AC44 HEK-293T C333(0.97); C434(1.10); C377(0.98)  LDD1545  [30]
 LDCM0307  AC45 HEK-293T C333(1.02); C434(1.05)  LDD1546  [30]
 LDCM0308  AC46 HCT 116 C333(1.06)  LDD0625  [31]
 LDCM0309  AC47 HCT 116 C333(1.00)  LDD0626  [31]
 LDCM0310  AC48 HCT 116 C333(1.15)  LDD0627  [31]
 LDCM0311  AC49 HCT 116 C333(0.25)  LDD0628  [31]
 LDCM0312  AC5 HEK-293T C333(0.96); C434(1.06)  LDD1551  [30]
 LDCM0313  AC50 HCT 116 C333(0.37)  LDD0630  [31]
 LDCM0314  AC51 HCT 116 C333(0.98)  LDD0631  [31]
 LDCM0315  AC52 HCT 116 C333(0.90)  LDD0632  [31]
 LDCM0316  AC53 HCT 116 C333(0.60)  LDD0633  [31]
 LDCM0317  AC54 HCT 116 C333(0.60)  LDD0634  [31]
 LDCM0318  AC55 HCT 116 C333(0.27)  LDD0635  [31]
 LDCM0319  AC56 HCT 116 C333(0.16)  LDD0636  [31]
 LDCM0320  AC57 HEK-293T C333(1.02); C434(0.99)  LDD1559  [30]
 LDCM0321  AC58 HEK-293T C333(1.01); C434(1.05)  LDD1560  [30]
 LDCM0322  AC59 HEK-293T C333(0.95); C434(1.13)  LDD1561  [30]
 LDCM0323  AC6 HEK-293T C333(0.99); C434(1.08); C377(1.02)  LDD1562  [30]
 LDCM0324  AC60 HEK-293T C333(0.99); C434(1.06); C377(1.21)  LDD1563  [30]
 LDCM0325  AC61 HEK-293T C333(1.02); C434(1.02)  LDD1564  [30]
 LDCM0326  AC62 HEK-293T C333(0.96); C434(1.09); C377(1.21)  LDD1565  [30]
 LDCM0327  AC63 HEK-293T C333(0.97); C434(0.99)  LDD1566  [30]
 LDCM0328  AC64 HEK-293T C333(0.99); C434(1.08); C377(1.16)  LDD1567  [30]
 LDCM0332  AC68 HCT 116 C333(0.88)  LDD0649  [31]
 LDCM0333  AC69 HCT 116 C333(0.95)  LDD0650  [31]
 LDCM0334  AC7 HEK-293T C333(1.00); C434(1.11)  LDD1568  [30]
 LDCM0335  AC70 HCT 116 C333(0.41)  LDD0652  [31]
 LDCM0336  AC71 HCT 116 C333(0.57)  LDD0653  [31]
 LDCM0337  AC72 HCT 116 C333(0.90)  LDD0654  [31]
 LDCM0338  AC73 HCT 116 C333(0.19)  LDD0655  [31]
 LDCM0339  AC74 HCT 116 C333(0.24)  LDD0656  [31]
 LDCM0340  AC75 HCT 116 C333(0.18)  LDD0657  [31]
 LDCM0341  AC76 HCT 116 C333(0.63)  LDD0658  [31]
 LDCM0342  AC77 HCT 116 C333(0.55)  LDD0659  [31]
 LDCM0343  AC78 HCT 116 C333(0.92)  LDD0660  [31]
 LDCM0344  AC79 HCT 116 C333(0.94)  LDD0661  [31]
 LDCM0345  AC8 HEK-293T C333(1.01); C434(1.05); C377(1.17)  LDD1569  [30]
 LDCM0346  AC80 HCT 116 C333(0.72)  LDD0663  [31]
 LDCM0347  AC81 HCT 116 C333(0.75)  LDD0664  [31]
 LDCM0348  AC82 HCT 116 C333(0.20)  LDD0665  [31]
 LDCM0248  AKOS034007472 HEK-293T C333(0.99); C434(0.98)  LDD1511  [30]
 LDCM0356  AKOS034007680 HEK-293T C333(0.99); C434(0.97)  LDD1570  [30]
 LDCM0275  AKOS034007705 HEK-293T C333(0.97); C434(0.93); C377(1.11)  LDD1514  [30]
 LDCM0108  Chloroacetamide HeLa H462(0.00); H180(0.00); H215(0.00); H176(0.00)  LDD0222  [25]
 LDCM0367  CL1 HEK-293T C333(0.96); C434(0.95)  LDD1571  [30]
 LDCM0368  CL10 HEK-293T C333(0.97); C434(0.69); C377(0.49)  LDD1572  [30]
 LDCM0369  CL100 HEK-293T C333(0.92); C434(0.94)  LDD1573  [30]
 LDCM0370  CL101 HEK-293T C333(0.98); C434(1.08)  LDD1574  [30]
 LDCM0371  CL102 HEK-293T C333(0.90); C434(1.09); C377(1.25)  LDD1575  [30]
 LDCM0372  CL103 HEK-293T C333(0.93); C434(0.98); C377(1.06)  LDD1576  [30]
 LDCM0373  CL104 HEK-293T C333(0.94); C434(0.96)  LDD1577  [30]
 LDCM0374  CL105 HEK-293T C333(0.97); C434(1.09)  LDD1578  [30]
 LDCM0375  CL106 HEK-293T C333(0.91); C434(0.98); C377(1.00)  LDD1579  [30]
 LDCM0376  CL107 HEK-293T C333(0.95); C434(1.20); C377(1.11)  LDD1580  [30]
 LDCM0377  CL108 HEK-293T C333(0.95); C434(0.96)  LDD1581  [30]
 LDCM0378  CL109 HEK-293T C333(0.92); C434(1.07)  LDD1582  [30]
 LDCM0379  CL11 HEK-293T C333(1.01); C434(0.92)  LDD1583  [30]
 LDCM0380  CL110 HEK-293T C333(0.80); C434(1.01); C377(0.96)  LDD1584  [30]
 LDCM0381  CL111 HEK-293T C333(0.94); C434(1.19); C377(0.91)  LDD1585  [30]
 LDCM0382  CL112 HEK-293T C333(1.01); C434(0.94)  LDD1586  [30]
 LDCM0383  CL113 HEK-293T C333(1.01); C434(1.02)  LDD1587  [30]
 LDCM0384  CL114 HEK-293T C333(0.86); C434(1.14); C377(1.07)  LDD1588  [30]
 LDCM0385  CL115 HEK-293T C333(0.98); C434(0.99); C377(1.08)  LDD1589  [30]
 LDCM0386  CL116 HEK-293T C333(0.96); C434(0.89)  LDD1590  [30]
 LDCM0387  CL117 HEK-293T C333(0.98); C434(1.04)  LDD1591  [30]
 LDCM0388  CL118 HEK-293T C333(0.97); C434(1.19); C377(0.90)  LDD1592  [30]
 LDCM0389  CL119 HEK-293T C333(0.99); C434(0.96); C377(0.92)  LDD1593  [30]
 LDCM0390  CL12 HEK-293T C333(1.08); C434(0.98); C377(0.54)  LDD1594  [30]
 LDCM0391  CL120 HEK-293T C333(0.95); C434(0.98)  LDD1595  [30]
 LDCM0392  CL121 HCT 116 C333(0.65)  LDD0709  [31]
 LDCM0393  CL122 HCT 116 C333(1.09)  LDD0710  [31]
 LDCM0394  CL123 HCT 116 C333(0.61)  LDD0711  [31]
 LDCM0395  CL124 HCT 116 C333(0.40)  LDD0712  [31]
 LDCM0396  CL125 HEK-293T C333(1.00); C434(1.13)  LDD1600  [30]
 LDCM0397  CL126 HEK-293T C333(0.97); C434(0.90); C377(1.18)  LDD1601  [30]
 LDCM0398  CL127 HEK-293T C333(0.98); C434(1.19); C377(0.93)  LDD1602  [30]
 LDCM0399  CL128 HEK-293T C333(0.96); C434(1.03)  LDD1603  [30]
 LDCM0400  CL13 HEK-293T C333(1.03); C434(1.29)  LDD1604  [30]
 LDCM0401  CL14 HEK-293T C333(0.93); C434(1.07); C377(0.88)  LDD1605  [30]
 LDCM0402  CL15 HEK-293T C333(0.82); C434(0.98); C377(0.87)  LDD1606  [30]
 LDCM0403  CL16 HEK-293T C333(0.96); C434(1.03)  LDD1607  [30]
 LDCM0404  CL17 HEK-293T C333(0.93); C434(0.87)  LDD1608  [30]
 LDCM0405  CL18 HEK-293T C333(1.07); C434(1.16)  LDD1609  [30]
 LDCM0406  CL19 HEK-293T C333(1.03); C434(1.14)  LDD1610  [30]
 LDCM0407  CL2 HEK-293T C333(1.00); C434(1.12); C377(1.02)  LDD1611  [30]
 LDCM0408  CL20 HEK-293T C333(1.08); C434(1.10); C377(0.51)  LDD1612  [30]
 LDCM0409  CL21 HEK-293T C333(0.96); C434(1.05)  LDD1613  [30]
 LDCM0410  CL22 HEK-293T C333(1.02); C434(0.72); C377(0.58)  LDD1614  [30]
 LDCM0411  CL23 HEK-293T C333(1.13); C434(1.08)  LDD1615  [30]
 LDCM0412  CL24 HEK-293T C333(1.17); C434(1.05); C377(0.57)  LDD1616  [30]
 LDCM0413  CL25 HEK-293T C333(0.90); C434(1.05)  LDD1617  [30]
 LDCM0414  CL26 HEK-293T C333(0.97); C434(1.20); C377(0.92)  LDD1618  [30]
 LDCM0415  CL27 HEK-293T C333(0.94); C434(1.02); C377(1.02)  LDD1619  [30]
 LDCM0416  CL28 HEK-293T C333(0.92); C434(0.77)  LDD1620  [30]
 LDCM0417  CL29 HEK-293T C333(1.00); C434(1.10)  LDD1621  [30]
 LDCM0418  CL3 HEK-293T C333(0.98); C434(1.00); C377(0.80)  LDD1622  [30]
 LDCM0419  CL30 HEK-293T C333(0.99); C434(1.00)  LDD1623  [30]
 LDCM0420  CL31 HCT 116 C333(0.99)  LDD0737  [31]
 LDCM0421  CL32 HCT 116 C333(0.79)  LDD0738  [31]
 LDCM0422  CL33 HCT 116 C333(0.81)  LDD0739  [31]
 LDCM0423  CL34 HCT 116 C333(0.73)  LDD0740  [31]
 LDCM0424  CL35 HCT 116 C333(0.58)  LDD0741  [31]
 LDCM0425  CL36 HCT 116 C333(0.73)  LDD0742  [31]
 LDCM0426  CL37 HCT 116 C333(0.36)  LDD0743  [31]
 LDCM0428  CL39 HCT 116 C333(0.60)  LDD0745  [31]
 LDCM0429  CL4 HEK-293T C333(0.93); C434(1.10)  LDD1633  [30]
 LDCM0430  CL40 HCT 116 C333(0.70)  LDD0747  [31]
 LDCM0431  CL41 HCT 116 C333(0.73)  LDD0748  [31]
 LDCM0432  CL42 HCT 116 C333(0.16)  LDD0749  [31]
 LDCM0433  CL43 HCT 116 C333(0.32)  LDD0750  [31]
 LDCM0434  CL44 HCT 116 C333(1.05)  LDD0751  [31]
 LDCM0435  CL45 HCT 116 C333(0.89)  LDD0752  [31]
 LDCM0436  CL46 HEK-293T C333(1.08); C434(0.59); C377(0.49)  LDD1640  [30]
 LDCM0437  CL47 HEK-293T C333(1.08); C434(0.95)  LDD1641  [30]
 LDCM0438  CL48 HEK-293T C333(1.15); C434(0.98); C377(0.49)  LDD1642  [30]
 LDCM0439  CL49 HEK-293T C333(1.00); C434(1.02)  LDD1643  [30]
 LDCM0440  CL5 HEK-293T C333(1.02); C434(1.07)  LDD1644  [30]
 LDCM0441  CL50 HEK-293T C333(0.97); C434(1.25); C377(1.07)  LDD1645  [30]
 LDCM0443  CL52 HEK-293T C333(0.93); C434(1.00)  LDD1646  [30]
 LDCM0444  CL53 HEK-293T C333(0.94); C434(1.16)  LDD1647  [30]
 LDCM0445  CL54 HEK-293T C333(0.91); C434(0.95)  LDD1648  [30]
 LDCM0446  CL55 HEK-293T C333(1.02); C434(1.01)  LDD1649  [30]
 LDCM0447  CL56 HEK-293T C333(0.99); C434(1.02); C377(0.57)  LDD1650  [30]
 LDCM0448  CL57 HEK-293T C333(0.97); C434(0.96)  LDD1651  [30]
 LDCM0449  CL58 HEK-293T C333(1.01); C434(0.76); C377(0.60)  LDD1652  [30]
 LDCM0450  CL59 HEK-293T C333(1.09); C434(1.17)  LDD1653  [30]
 LDCM0451  CL6 HEK-293T C333(0.84); C434(0.99)  LDD1654  [30]
 LDCM0452  CL60 HEK-293T C333(1.12); C434(1.07); C377(0.60)  LDD1655  [30]
 LDCM0453  CL61 HEK-293T C333(0.98); C434(1.18)  LDD1656  [30]
 LDCM0454  CL62 HEK-293T C333(0.93); C434(1.21); C377(1.26)  LDD1657  [30]
 LDCM0455  CL63 HEK-293T C333(0.96); C434(1.08); C377(0.93)  LDD1658  [30]
 LDCM0456  CL64 HEK-293T C333(0.90); C434(0.91)  LDD1659  [30]
 LDCM0457  CL65 HEK-293T C333(1.01); C434(1.05)  LDD1660  [30]
 LDCM0458  CL66 HEK-293T C333(1.00); C434(0.92)  LDD1661  [30]
 LDCM0459  CL67 HEK-293T C333(1.00); C434(1.02)  LDD1662  [30]
 LDCM0460  CL68 HEK-293T C333(0.94); C434(0.99); C377(0.59)  LDD1663  [30]
 LDCM0461  CL69 HEK-293T C333(1.03); C434(1.07)  LDD1664  [30]
 LDCM0462  CL7 HEK-293T C333(1.01); C434(1.04)  LDD1665  [30]
 LDCM0463  CL70 HEK-293T C333(1.09); C434(0.65); C377(0.57)  LDD1666  [30]
 LDCM0464  CL71 HEK-293T C333(1.09); C434(0.99)  LDD1667  [30]
 LDCM0465  CL72 HEK-293T C333(1.05); C434(1.04); C377(0.55)  LDD1668  [30]
 LDCM0466  CL73 HEK-293T C333(0.96); C434(1.02)  LDD1669  [30]
 LDCM0467  CL74 HEK-293T C333(0.99); C434(1.00); C377(1.00)  LDD1670  [30]
 LDCM0469  CL76 HCT 116 C333(1.02)  LDD0786  [31]
 LDCM0470  CL77 HCT 116 C333(1.03)  LDD0787  [31]
 LDCM0471  CL78 HCT 116 C333(2.49)  LDD0788  [31]
 LDCM0472  CL79 HCT 116 C333(1.16)  LDD0789  [31]
 LDCM0473  CL8 HEK-293T C333(0.82); C434(0.80); C377(0.44)  LDD1676  [30]
 LDCM0474  CL80 HCT 116 C333(2.21)  LDD0791  [31]
 LDCM0475  CL81 HCT 116 C333(1.43)  LDD0792  [31]
 LDCM0476  CL82 HCT 116 C333(0.77)  LDD0793  [31]
 LDCM0477  CL83 HCT 116 C333(0.93)  LDD0794  [31]
 LDCM0478  CL84 HCT 116 C333(0.42)  LDD0795  [31]
 LDCM0479  CL85 HCT 116 C333(0.97)  LDD0796  [31]
 LDCM0480  CL86 HCT 116 C333(1.25)  LDD0797  [31]
 LDCM0481  CL87 HCT 116 C333(1.11)  LDD0798  [31]
 LDCM0482  CL88 HCT 116 C333(1.09)  LDD0799  [31]
 LDCM0483  CL89 HCT 116 C333(0.39)  LDD0800  [31]
 LDCM0484  CL9 HEK-293T C333(1.09); C434(1.04)  LDD1687  [30]
 LDCM0485  CL90 HCT 116 C333(0.93)  LDD0802  [31]
 LDCM0486  CL91 HEK-293T C333(0.95); C434(1.13)  LDD1689  [30]
 LDCM0487  CL92 HEK-293T C333(0.92); C434(1.13); C377(0.75)  LDD1690  [30]
 LDCM0488  CL93 HEK-293T C333(0.98); C434(0.86)  LDD1691  [30]
 LDCM0489  CL94 HEK-293T C333(0.98); C434(0.85); C377(0.66)  LDD1692  [30]
 LDCM0490  CL95 HEK-293T C333(0.84); C434(0.92)  LDD1693  [30]
 LDCM0491  CL96 HEK-293T C333(1.00); C434(0.99); C377(0.74)  LDD1694  [30]
 LDCM0492  CL97 HEK-293T C333(0.96); C434(1.07)  LDD1695  [30]
 LDCM0493  CL98 HEK-293T C333(0.96); C434(0.94); C377(1.21)  LDD1696  [30]
 LDCM0494  CL99 HEK-293T C333(0.93); C434(1.08); C377(1.25)  LDD1697  [30]
 LDCM0495  E2913 HEK-293T C333(0.98); C434(1.00); C377(1.16)  LDD1698  [30]
 LDCM0468  Fragment33 HEK-293T C333(0.94); C434(1.04); C377(0.85)  LDD1671  [30]
 LDCM0427  Fragment51 HCT 116 C333(0.19)  LDD0744  [31]
 LDCM0116  HHS-0101 DM93 Y491(0.74); Y67(0.83); Y54(0.98); Y465(1.03)  LDD0264  [12]
 LDCM0117  HHS-0201 DM93 Y54(0.67); Y491(1.11); Y67(1.60); Y465(1.66)  LDD0265  [12]
 LDCM0118  HHS-0301 DM93 Y54(0.52); Y491(0.69); Y465(0.91); Y67(0.92)  LDD0266  [12]
 LDCM0119  HHS-0401 DM93 Y54(0.40); Y491(1.08); Y465(1.31); Y67(1.86)  LDD0267  [12]
 LDCM0120  HHS-0701 DM93 Y54(0.71); Y491(1.01); Y465(1.11); Y67(1.46)  LDD0268  [12]
 LDCM0107  IAA HeLa H176(0.00); H180(0.00); H215(0.00); H462(0.00)  LDD0221  [25]
 LDCM0123  JWB131 DM93 Y465(1.08)  LDD0285  [11]
 LDCM0124  JWB142 DM93 Y465(0.52)  LDD0286  [11]
 LDCM0125  JWB146 DM93 Y465(1.15)  LDD0287  [11]
 LDCM0126  JWB150 DM93 Y465(2.04)  LDD0288  [11]
 LDCM0127  JWB152 DM93 Y465(1.24)  LDD0289  [11]
 LDCM0128  JWB198 DM93 Y465(0.40)  LDD0290  [11]
 LDCM0129  JWB202 DM93 Y465(0.70)  LDD0291  [11]
 LDCM0130  JWB211 DM93 Y465(0.94)  LDD0292  [11]
 LDCM0022  KB02 HEK-293T C333(1.02)  LDD1492  [30]
 LDCM0023  KB03 Jurkat C333(4.86)  LDD0209  [10]
 LDCM0024  KB05 IGR37 C333(1.02)  LDD3314  [32]
 LDCM0109  NEM HeLa H180(0.00); H462(0.00); H215(0.00)  LDD0223  [25]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Diamine acetyltransferase 1 (SAT1) Acetyltransferase family P21673
DNA-directed RNA polymerases I and III subunit RPAC1 (POLR1C) Archaeal Rpo3/eukaryotic RPB3 RNA polymerase subunit family O15160
Serine/threonine-protein kinase pim-1 (PIM1) CAMK Ser/Thr protein kinase family P11309
Exosome complex component RRP46 (EXOSC5) RNase PH family Q9NQT4
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein DGCR6 (DGCR6) Gonadal family Q14129
Histone H2A.Z (H2AZ1) Histone H2A family P0C0S5
Lamin-B2 (LMNB2) Intermediate filament family Q03252
Tetratricopeptide repeat protein 19, mitochondrial (TTC19) TTC19 family Q6DKK2
Coiled-coil domain-containing protein 102B (CCDC102B) . Q68D86
Kelch-like protein 6 (KLHL6) . Q8WZ60

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 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 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.
6 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
7 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
8 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
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 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
11 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.
12 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.
13 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.
14 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
15 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.
16 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
17 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
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 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
21 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
22 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
23 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
24 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.
25 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.
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 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
29 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.
30 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
31 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.
32 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