General Information of Target

Target ID LDTP03534
Target Name Peptidyl-prolyl cis-trans isomerase F, mitochondrial (PPIF)
Gene Name PPIF
Gene ID 10105
Synonyms
CYP3; Peptidyl-prolyl cis-trans isomerase F, mitochondrial; PPIase F; EC 5.2.1.8; Cyclophilin D; CyP-D; CypD; Cyclophilin F; Mitochondrial cyclophilin; CyP-M; Rotamase F
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLALRCGSRWLGLLSVPRSVPLRLPAARACSKGSGDPSSSSSSGNPLVYLDVDANGKPLG
RVVLELKADVVPKTAENFRALCTGEKGFGYKGSTFHRVIPSFMCQAGDFTNHNGTGGKSI
YGSRFPDENFTLKHVGPGVLSMANAGPNTNGSQFFICTIKTDWLDGKHVVFGHVKEGMDV
VKKIESFGSKSGRTSKKIVITDCGQLS
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Cyclophilin-type PPIase family
Subcellular location
Mitochondrion matrix
Function
PPIase that catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides and may therefore assist protein folding. Involved in regulation of the mitochondrial permeability transition pore (mPTP). It is proposed that its association with the mPTP is masking a binding site for inhibiting inorganic phosphate (Pi) and promotes the open probability of the mPTP leading to apoptosis or necrosis; the requirement of the PPIase activity for this function is debated. In cooperation with mitochondrial p53/TP53 is involved in activating oxidative stress-induced necrosis. Involved in modulation of mitochondrial membrane F(1)F(0) ATP synthase activity and regulation of mitochondrial matrix adenine nucleotide levels. Has anti-apoptotic activity independently of mPTP and in cooperation with BCL2 inhibits cytochrome c-dependent apoptosis.
TTD ID
T62746
Uniprot ID
P30405
DrugMap ID
TT95SAZ
Ensemble ID
ENST00000225174.8
HGNC ID
HGNC:9259
ChEMBL ID
CHEMBL3325306

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.L47I .
COLO678 SNV: p.G122E .
NCIH716 SNV: p.G122E .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 28 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
N1
 Probe Info 
100.00  LDD0242  [1]
YN-1
 Probe Info 
100.00  LDD0444  [2]
ONAyne
 Probe Info 
N.A.  LDD0273  [3]
IPM
 Probe Info 
C104(0.00); C203(0.00)  LDD0241  [4]
DBIA
 Probe Info 
C104(1.56)  LDD3318  [5]
JZ128-DTB
 Probe Info 
N.A.  LDD0462  [6]
BTD
 Probe Info 
C104(2.16)  LDD2092  [7]
5E-2FA
 Probe Info 
H134(0.00); H173(0.00); H112(0.00)  LDD2235  [8]
ATP probe
 Probe Info 
K86(0.00); K175(0.00); K197(0.00)  LDD0199  [9]
m-APA
 Probe Info 
H112(0.00); H173(0.00)  LDD2231  [8]
CY-1
 Probe Info 
D69(0.00); E65(0.00)  LDD0246  [1]
4-Iodoacetamidophenylacetylene
 Probe Info 
C157(0.00); C203(0.00); C104(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info 
C157(0.00); C104(0.00)  LDD0032  [11]
Lodoacetamide azide
 Probe Info 
C203(0.00); C104(0.00); C157(0.00)  LDD0037  [10]
ATP probe
 Probe Info 
K160(0.00); K190(0.00)  LDD0035  [12]
JW-RF-010
 Probe Info 
C203(0.00); C104(0.00)  LDD0026  [13]
TFBX
 Probe Info 
C203(0.00); C104(0.00)  LDD0027  [13]
NHS
 Probe Info 
K73(0.00); K57(0.00); K67(0.00)  LDD0010  [14]
OSF
 Probe Info 
N.A.  LDD0029  [15]
SF
 Probe Info 
K73(0.00); K183(0.00); K190(0.00)  LDD0028  [15]
STPyne
 Probe Info 
K73(0.00); K67(0.00)  LDD0009  [14]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [16]
1c-yne
 Probe Info 
N.A.  LDD0228  [17]
Acrolein
 Probe Info 
C104(0.00); C203(0.00); H173(0.00)  LDD0217  [18]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [18]
Methacrolein
 Probe Info 
N.A.  LDD0218  [18]
NAIA_5
 Probe Info 
C82(0.00); C104(0.00)  LDD2223  [19]
HHS-465
 Probe Info 
K67(0.00); K118(0.00); K183(0.00); K91(0.00)  LDD2240  [20]

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 C104(0.26)  LDD2142  [7]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C104(0.42)  LDD2112  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C104(0.99)  LDD2117  [7]
 LDCM0214  AC1 HEK-293T C157(0.93)  LDD1507  [21]
 LDCM0226  AC11 HEK-293T C104(1.03)  LDD1509  [21]
 LDCM0270  AC15 HEK-293T C104(0.97); C157(1.01)  LDD1513  [21]
 LDCM0276  AC17 HEK-293T C157(1.06)  LDD1515  [21]
 LDCM0278  AC19 HEK-293T C104(1.20)  LDD1517  [21]
 LDCM0281  AC21 HEK-293T C157(1.06)  LDD1520  [21]
 LDCM0283  AC23 HEK-293T C104(0.87); C157(1.30)  LDD1522  [21]
 LDCM0284  AC24 HEK-293T C104(1.06)  LDD1523  [21]
 LDCM0285  AC25 HEK-293T C157(0.95)  LDD1524  [21]
 LDCM0287  AC27 HEK-293T C104(1.04)  LDD1526  [21]
 LDCM0289  AC29 HEK-293T C157(1.17)  LDD1528  [21]
 LDCM0290  AC3 HEK-293T C104(1.10)  LDD1529  [21]
 LDCM0292  AC31 HEK-293T C104(0.97); C157(0.88)  LDD1531  [21]
 LDCM0293  AC32 HEK-293T C104(0.99)  LDD1532  [21]
 LDCM0294  AC33 HEK-293T C157(0.94)  LDD1533  [21]
 LDCM0296  AC35 HEK-293T C104(1.20)  LDD1535  [21]
 LDCM0298  AC37 HEK-293T C157(1.18)  LDD1537  [21]
 LDCM0300  AC39 HEK-293T C104(0.96); C157(1.00)  LDD1539  [21]
 LDCM0302  AC40 HEK-293T C104(1.07)  LDD1541  [21]
 LDCM0303  AC41 HEK-293T C157(1.01)  LDD1542  [21]
 LDCM0305  AC43 HEK-293T C104(0.93)  LDD1544  [21]
 LDCM0307  AC45 HEK-293T C157(1.09)  LDD1546  [21]
 LDCM0309  AC47 HEK-293T C104(1.24); C157(1.24)  LDD1548  [21]
 LDCM0310  AC48 HEK-293T C104(1.10)  LDD1549  [21]
 LDCM0311  AC49 HEK-293T C157(1.01)  LDD1550  [21]
 LDCM0312  AC5 HEK-293T C157(1.27)  LDD1551  [21]
 LDCM0314  AC51 HEK-293T C104(1.01)  LDD1553  [21]
 LDCM0316  AC53 HEK-293T C157(1.18)  LDD1555  [21]
 LDCM0318  AC55 HEK-293T C104(0.95); C157(1.18)  LDD1557  [21]
 LDCM0319  AC56 HEK-293T C104(1.12)  LDD1558  [21]
 LDCM0320  AC57 HEK-293T C157(0.98)  LDD1559  [21]
 LDCM0322  AC59 HEK-293T C104(1.13)  LDD1561  [21]
 LDCM0325  AC61 HEK-293T C157(1.14)  LDD1564  [21]
 LDCM0327  AC63 HEK-293T C104(1.03); C157(0.90)  LDD1566  [21]
 LDCM0328  AC64 HEK-293T C104(0.96)  LDD1567  [21]
 LDCM0334  AC7 HEK-293T C104(1.09); C157(0.81)  LDD1568  [21]
 LDCM0345  AC8 HEK-293T C104(1.01)  LDD1569  [21]
 LDCM0248  AKOS034007472 HEK-293T C157(1.16)  LDD1511  [21]
 LDCM0356  AKOS034007680 HEK-293T C157(1.07)  LDD1570  [21]
 LDCM0275  AKOS034007705 HEK-293T C104(1.10)  LDD1514  [21]
 LDCM0108  Chloroacetamide HeLa C104(0.00); C203(0.00)  LDD0222  [18]
 LDCM0367  CL1 HEK-293T C104(1.25)  LDD1571  [21]
 LDCM0370  CL101 HEK-293T C104(1.06)  LDD1574  [21]
 LDCM0372  CL103 HEK-293T C104(0.91)  LDD1576  [21]
 LDCM0374  CL105 HEK-293T C104(0.96)  LDD1578  [21]
 LDCM0376  CL107 HEK-293T C104(0.97)  LDD1580  [21]
 LDCM0378  CL109 HEK-293T C104(1.09)  LDD1582  [21]
 LDCM0379  CL11 HEK-293T C104(1.02); C157(0.92)  LDD1583  [21]
 LDCM0381  CL111 HEK-293T C104(1.10)  LDD1585  [21]
 LDCM0383  CL113 HEK-293T C104(0.91)  LDD1587  [21]
 LDCM0385  CL115 HEK-293T C104(1.00)  LDD1589  [21]
 LDCM0387  CL117 HEK-293T C104(0.98)  LDD1591  [21]
 LDCM0389  CL119 HEK-293T C104(0.92)  LDD1593  [21]
 LDCM0390  CL12 HEK-293T C104(0.61)  LDD1594  [21]
 LDCM0392  CL121 HEK-293T C104(1.01)  LDD1596  [21]
 LDCM0394  CL123 HEK-293T C104(1.21)  LDD1598  [21]
 LDCM0396  CL125 HEK-293T C104(1.03)  LDD1600  [21]
 LDCM0398  CL127 HEK-293T C104(0.95)  LDD1602  [21]
 LDCM0400  CL13 HEK-293T C104(1.05)  LDD1604  [21]
 LDCM0402  CL15 HEK-293T C104(1.17)  LDD1606  [21]
 LDCM0404  CL17 HEK-293T C157(0.96)  LDD1608  [21]
 LDCM0406  CL19 HEK-293T C104(0.98)  LDD1610  [21]
 LDCM0409  CL21 HEK-293T C157(1.01)  LDD1613  [21]
 LDCM0411  CL23 HEK-293T C104(0.98); C157(0.86)  LDD1615  [21]
 LDCM0412  CL24 HEK-293T C104(0.91)  LDD1616  [21]
 LDCM0413  CL25 HEK-293T C104(1.21)  LDD1617  [21]
 LDCM0415  CL27 HEK-293T C104(0.94)  LDD1619  [21]
 LDCM0417  CL29 HEK-293T C157(0.86)  LDD1621  [21]
 LDCM0418  CL3 HEK-293T C104(1.01)  LDD1622  [21]
 LDCM0420  CL31 HEK-293T C104(1.00)  LDD1624  [21]
 LDCM0422  CL33 HEK-293T C157(0.94)  LDD1626  [21]
 LDCM0424  CL35 HEK-293T C104(0.88); C157(0.78)  LDD1628  [21]
 LDCM0425  CL36 HEK-293T C104(0.88)  LDD1629  [21]
 LDCM0426  CL37 HEK-293T C104(1.08)  LDD1630  [21]
 LDCM0428  CL39 HEK-293T C104(0.91)  LDD1632  [21]
 LDCM0431  CL41 HEK-293T C157(1.17)  LDD1635  [21]
 LDCM0433  CL43 HEK-293T C104(0.90)  LDD1637  [21]
 LDCM0435  CL45 HEK-293T C157(1.07)  LDD1639  [21]
 LDCM0437  CL47 HEK-293T C104(0.94); C157(0.84)  LDD1641  [21]
 LDCM0438  CL48 HEK-293T C104(0.93)  LDD1642  [21]
 LDCM0439  CL49 HEK-293T C104(1.07)  LDD1643  [21]
 LDCM0440  CL5 HEK-293T C157(1.38)  LDD1644  [21]
 LDCM0444  CL53 HEK-293T C157(0.95)  LDD1647  [21]
 LDCM0446  CL55 HEK-293T C104(0.95)  LDD1649  [21]
 LDCM0448  CL57 HEK-293T C157(0.84)  LDD1651  [21]
 LDCM0450  CL59 HEK-293T C104(1.16); C157(0.86)  LDD1653  [21]
 LDCM0452  CL60 HEK-293T C104(0.90)  LDD1655  [21]
 LDCM0453  CL61 HEK-293T C104(1.17)  LDD1656  [21]
 LDCM0455  CL63 HEK-293T C104(0.77)  LDD1658  [21]
 LDCM0457  CL65 HEK-293T C157(1.00)  LDD1660  [21]
 LDCM0459  CL67 HEK-293T C104(0.94)  LDD1662  [21]
 LDCM0461  CL69 HEK-293T C157(0.98)  LDD1664  [21]
 LDCM0462  CL7 HEK-293T C104(1.06)  LDD1665  [21]
 LDCM0464  CL71 HEK-293T C104(1.11); C157(0.81)  LDD1667  [21]
 LDCM0465  CL72 HEK-293T C104(1.08)  LDD1668  [21]
 LDCM0466  CL73 HEK-293T C104(1.04)  LDD1669  [21]
 LDCM0470  CL77 HEK-293T C157(0.97)  LDD1673  [21]
 LDCM0472  CL79 HEK-293T C104(0.96)  LDD1675  [21]
 LDCM0475  CL81 HEK-293T C157(1.10)  LDD1678  [21]
 LDCM0477  CL83 HEK-293T C104(1.05); C157(0.91)  LDD1680  [21]
 LDCM0478  CL84 HEK-293T C104(0.96)  LDD1681  [21]
 LDCM0479  CL85 HEK-293T C104(1.31)  LDD1682  [21]
 LDCM0481  CL87 HEK-293T C104(1.06)  LDD1684  [21]
 LDCM0483  CL89 HEK-293T C157(1.03)  LDD1686  [21]
 LDCM0484  CL9 HEK-293T C157(0.97)  LDD1687  [21]
 LDCM0486  CL91 HEK-293T C104(1.02)  LDD1689  [21]
 LDCM0488  CL93 HEK-293T C157(1.08)  LDD1691  [21]
 LDCM0490  CL95 HEK-293T C104(1.16); C157(0.97)  LDD1693  [21]
 LDCM0491  CL96 HEK-293T C104(0.90)  LDD1694  [21]
 LDCM0492  CL97 HEK-293T C104(1.07)  LDD1695  [21]
 LDCM0494  CL99 HEK-293T C104(0.98)  LDD1697  [21]
 LDCM0495  E2913 HEK-293T C104(1.02)  LDD1698  [21]
 LDCM0625  F8 Ramos C104(1.58); C157(3.46)  LDD2187  [22]
 LDCM0572  Fragment10 Ramos C104(0.72); C157(0.29)  LDD2189  [22]
 LDCM0573  Fragment11 Ramos C104(5.79); C157(3.93)  LDD2190  [22]
 LDCM0574  Fragment12 Ramos C104(0.79); C157(0.23)  LDD2191  [22]
 LDCM0575  Fragment13 Ramos C104(1.10); C157(0.54)  LDD2192  [22]
 LDCM0576  Fragment14 Ramos C104(1.15); C157(1.69)  LDD2193  [22]
 LDCM0579  Fragment20 Ramos C104(0.66); C157(0.25)  LDD2194  [22]
 LDCM0580  Fragment21 Ramos C104(0.96); C157(0.58)  LDD2195  [22]
 LDCM0582  Fragment23 Ramos C104(1.00)  LDD2196  [22]
 LDCM0578  Fragment27 Ramos C104(1.03)  LDD2197  [22]
 LDCM0586  Fragment28 Ramos C104(0.88); C157(3.97)  LDD2198  [22]
 LDCM0588  Fragment30 Ramos C104(1.24); C157(0.16)  LDD2199  [22]
 LDCM0589  Fragment31 Ramos C104(1.06)  LDD2200  [22]
 LDCM0590  Fragment32 Ramos C104(0.70); C157(0.28)  LDD2201  [22]
 LDCM0468  Fragment33 HEK-293T C104(0.95)  LDD1671  [21]
 LDCM0596  Fragment38 Ramos C104(0.98)  LDD2203  [22]
 LDCM0566  Fragment4 Ramos C104(0.79); C157(0.89)  LDD2184  [22]
 LDCM0610  Fragment52 Ramos C104(1.22); C157(0.62)  LDD2204  [22]
 LDCM0614  Fragment56 Ramos C104(1.05)  LDD2205  [22]
 LDCM0569  Fragment7 Ramos C104(0.70); C157(1.22)  LDD2186  [22]
 LDCM0571  Fragment9 Ramos C104(0.68); C157(0.14)  LDD2188  [22]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [6]
 LDCM0022  KB02 HEK-293T C157(0.95)  LDD1492  [21]
 LDCM0023  KB03 HEK-293T C157(0.97)  LDD1497  [21]
 LDCM0024  KB05 MELHO C104(1.56)  LDD3318  [5]
 LDCM0109  NEM HeLa C104(0.00); C203(0.00)  LDD0223  [18]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C104(2.16)  LDD2092  [7]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C157(1.11)  LDD2096  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C104(1.40)  LDD2098  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C104(1.09)  LDD2099  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C104(0.32)  LDD2100  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C104(0.35)  LDD2104  [7]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C104(1.06)  LDD2105  [7]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C104(0.26)  LDD2106  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C104(0.89)  LDD2107  [7]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C104(0.38)  LDD2108  [7]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C104(0.39)  LDD2110  [7]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C104(0.31)  LDD2114  [7]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C104(0.19)  LDD2118  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C104(2.09)  LDD2119  [7]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C104(0.50)  LDD2120  [7]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C104(0.23); C157(0.80)  LDD2122  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C104(0.99)  LDD2123  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C104(1.00)  LDD2125  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C104(1.20)  LDD2127  [7]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C104(0.91)  LDD2128  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C104(0.92)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C104(1.24)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C104(1.06)  LDD2137  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C104(0.91)  LDD2140  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C104(0.78)  LDD2143  [7]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C104(0.66)  LDD2145  [7]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C104(0.49)  LDD2148  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C104(0.59)  LDD2150  [7]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C104(0.21)  LDD2151  [7]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C104(4.59)  LDD2153  [7]
 LDCM0131  RA190 MM1.R C203(1.14)  LDD0304  [23]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Peptidyl-prolyl cis-trans isomerase FKBP7 (FKBP7) . Q9Y680
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Synaptophysin (SYP) Synaptophysin/synaptobrevin family P08247
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CKLF-like MARVEL transmembrane domain-containing protein 5 (CMTM5) Chemokine-like factor family Q96DZ9
Other
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 2 (ABI2) ABI family Q9NYB9
Protein BANP (BANP) BANP/SMAR1 family Q8N9N5
Lipid transferase CIDEB (CIDEB) CIDE family Q9UHD4
Protein FAM25C (FAM25C) FAM25 family B3EWG5
Synaptophysin-like protein 1 (SYPL1) Synaptophysin/synaptobrevin family Q16563
Protein YIF1A (YIF1A) YIF1 family O95070
Arfaptin-2 (ARFIP2) . P53365
Basic salivary proline-rich protein 3 (PRB3) . Q04118
Melanoma-associated antigen 11 (MAGEA11) . P43364

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cyclosporine Protein/peptide DB00091
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Coumarin 120 Small molecular drug DB08168
Proline Small molecular drug DB00172
Triglyme Small molecular drug DB02078

References

1 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.
2 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.
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 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.
5 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
6 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 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
9 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
10 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
11 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
12 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
13 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
14 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
15 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
16 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
17 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.
18 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.
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 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
21 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
22 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
23 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.