Details of the Target

General Information of Target

Target ID LDTP02770
Target Name Eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)
Gene Name GSPT1
Gene ID 2935
Synonyms
ERF3A; Eukaryotic peptide chain release factor GTP-binding subunit ERF3A; Eukaryotic peptide chain release factor subunit 3a; eRF3a; EC 3.6.5.-; G1 to S phase transition protein 1 homolog
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELSEPIVENGETEMSPEESWEHKEEISEAEPGGGSLGDGRPPEESAHEMMEEEEEIPKP
KSVVAPPGAPKKEHVNVVFIGHVDAGKSTIGGQIMYLTGMVDKRTLEKYEREAKEKNRET
WYLSWALDTNQEERDKGKTVEVGRAYFETEKKHFTILDAPGHKSFVPNMIGGASQADLAV
LVISARKGEFETGFEKGGQTREHAMLAKTAGVKHLIVLINKMDDPTVNWSNERYEECKEK
LVPFLKKVGFNPKKDIHFMPCSGLTGANLKEQSDFCPWYIGLPFIPYLDNLPNFNRSVDG
PIRLPIVDKYKDMGTVVLGKLESGSICKGQQLVMMPNKHNVEVLGILSDDVETDTVAPGE
NLKIRLKGIEEEEILPGFILCDPNNLCHSGRTFDAQIVIIEHKSIICPGYNAVLHIHTCI
EEVEITALICLVDKKSGEKSKTRPRFVKQDQVCIARLRTAGTICLETFKDFPQMGRFTLR
DEGKTIAIGKVLKLVPEKD
Target Bioclass
Enzyme
Family
TRAFAC class translation factor GTPase superfamily, Classic translation factor GTPase family, ERF3 subfamily
Function
GTPase component of the eRF1-eRF3-GTP ternary complex, a ternary complex that mediates translation termination in response to the termination codons UAA, UAG and UGA. GSPT1/ERF3A mediates ETF1/ERF1 delivery to stop codons: The eRF1-eRF3-GTP complex binds to a stop codon in the ribosomal A-site. GTP hydrolysis by GSPT1/ERF3A induces a conformational change that leads to its dissociation, permitting ETF1/ERF1 to accommodate fully in the A-site. Component of the transient SURF complex which recruits UPF1 to stalled ribosomes in the context of nonsense-mediated decay (NMD) of mRNAs containing premature stop codons. Required for SHFL-mediated translation termination which inhibits programmed ribosomal frameshifting (-1PRF) of mRNA from viruses and cellular genes.
Uniprot ID
P15170
Ensemble ID
ENST00000420576.6
HGNC ID
HGNC:4621
ChEMBL ID
CHEMBL4523593

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 44 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info  		50.00  LDD0214  [1]
m-APA
 Probe Info  		15.00  LDD0402  [2]
DAyne
 Probe Info  		3.42  LDD0261  [3]
CY-1
 Probe Info  		100.00  LDD0243  [4]
TH211
 Probe Info  		Y146(12.57); Y96(9.60); Y234(6.68)  LDD0257  [5]
TH216
 Probe Info  		Y146(17.55)  LDD0259  [5]
YN-1
 Probe Info  		100.00  LDD0444  [6]
BTD
 Probe Info  		C327(8.16)  LDD1699  [7]
Probe 1
 Probe Info  		Y146(336.02)  LDD3495  [8]
DBIA
 Probe Info  		C465(1.62)  LDD3312  [9]
P12
 Probe Info  		7.72  LDD0202  [10]
THZ1-DTB
 Probe Info  		C276(1.08); C237(1.04)  LDD0460  [11]
Sulforaphane-probe2
 Probe Info  		2.34  LDD0042  [12]
DA-P3
 Probe Info  		5.29  LDD0179  [13]
AHL-Pu-1
 Probe Info  		C453(2.15); C387(2.35); C237(2.09); C327(2.10)  LDD0169  [14]
HHS-482
 Probe Info  		Y146(0.86)  LDD0285  [15]
HHS-475
 Probe Info  		Y96(0.85); Y146(1.48)  LDD0264  [16]
HHS-465
 Probe Info  		Y96(10.00)  LDD2237  [17]
5E-2FA
 Probe Info  		N.A.  LDD2235  [18]
AMP probe
 Probe Info  		K490(0.00); K448(0.00)  LDD0200  [19]
ATP probe
 Probe Info  		K490(0.00); K448(0.00); K71(0.00); K72(0.00)  LDD0199  [19]
1d-yne
 Probe Info  		K72(0.00); K270(0.00)  LDD0358  [20]
4-Iodoacetamidophenylacetylene
 Probe Info  		C261(0.00); C327(0.00); C453(0.00); C464(0.00)  LDD0038  [21]
IA-alkyne
 Probe Info  		C237(0.00); C327(0.00); C453(0.00); C381(0.00)  LDD0032  [22]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [23]
IPIAA_L
 Probe Info  		C464(0.00); C381(0.00); C237(0.00)  LDD0031  [23]
Lodoacetamide azide
 Probe Info  		C261(0.00); C276(0.00); C327(0.00); C237(0.00)  LDD0037  [21]
ATP probe
 Probe Info  		K208(0.00); K247(0.00)  LDD0035  [24]
TFBX
 Probe Info  		N.A.  LDD0027  [25]
WYneN
 Probe Info  		N.A.  LDD0021  [26]
WYneO
 Probe Info  		C327(0.00); C453(0.00)  LDD0022  [26]
ENE
 Probe Info  		C453(0.00); C327(0.00)  LDD0006  [26]
IPM
 Probe Info  		N.A.  LDD0005  [26]
NHS
 Probe Info  		K196(0.00); K71(0.00)  LDD0010  [26]
PF-06672131
 Probe Info  		N.A.  LDD0017  [27]
SF
 Probe Info  		Y109(0.00); K246(0.00); K247(0.00); K490(0.00)  LDD0028  [28]
STPyne
 Probe Info  		N.A.  LDD0009  [26]
VSF
 Probe Info  		N.A.  LDD0007  [26]
1c-yne
 Probe Info  		K448(0.00); K254(0.00)  LDD0228  [20]
Acrolein
 Probe Info  		C327(0.00); H402(0.00); C381(0.00); C237(0.00)  LDD0217  [29]
Methacrolein
 Probe Info  		N.A.  LDD0218  [29]
W1
 Probe Info  		C381(0.00); C387(0.00); C327(0.00); C453(0.00)  LDD0236  [30]
AOyne
 Probe Info  		15.00  LDD0443  [31]
NAIA_5
 Probe Info  		C261(0.00); C327(0.00); C276(0.00); C453(0.00)  LDD2223  [32]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		8.97  LDD0475  [33]
FFF probe3
 Probe Info  		5.75  LDD0465  [33]
VE-P
 Probe Info  		N.A.  LDD0396  [34]
Probe 3
 Probe Info  		N.A.  LDD0195  [35]

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 C327(0.72)  LDD2142  [7]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C327(0.99); C261(0.89)  LDD2112  [7]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C327(0.71); C453(0.65); C464(0.56)  LDD2095  [7]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C327(1.07); C453(0.85); C464(1.16)  LDD2130  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C327(0.97); C261(1.16); C237(0.94)  LDD2117  [7]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C327(1.17); C237(2.13)  LDD2152  [7]
 LDCM0101  23-cGAMP HeLa N.A.  LDD0195  [35]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C327(1.36); C261(0.93)  LDD2103  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C327(0.79); C453(0.72); C464(0.64); C237(0.46)  LDD2132  [7]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C327(0.91); C453(0.69)  LDD2131  [7]
 LDCM0025  4SU-RNA DM93 C327(2.15)  LDD0170  [14]
 LDCM0026  4SU-RNA+native RNA HEK-293T C453(2.15); C387(2.35); C237(2.09); C327(2.10)  LDD0169  [14]
 LDCM0545  Acetamide MDA-MB-231 C327(0.43); C237(0.60)  LDD2138  [7]
 LDCM0520  AKOS000195272 MDA-MB-231 C327(0.64); C464(0.67); C261(0.86)  LDD2113  [7]
 LDCM0156  Aniline NCI-H1299 12.78  LDD0403  [2]
 LDCM0498  BS-3668 MDA-MB-231 C261(0.67); C237(0.47)  LDD2091  [7]
 LDCM0088  C45 HEK-293T 7.72  LDD0202  [10]
 LDCM0630  CCW28-3 231MFP C276(0.97)  LDD2214  [36]
 LDCM0108  Chloroacetamide HeLa H402(0.00); C327(0.00); C381(0.00); H339(0.00)  LDD0222  [29]
 LDCM0632  CL-Sc Hep-G2 C237(20.00); C261(4.83); C237(2.99); C327(2.35)  LDD2227  [32]
 LDCM0634  CY-0357 Hep-G2 C327(0.82)  LDD2228  [32]
 LDCM0028  Dobutamine HEK-293T 4.52  LDD0180  [13]
 LDCM0027  Dopamine HEK-293T 5.29  LDD0179  [13]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C261(1.35); C327(0.96)  LDD1702  [7]
 LDCM0031  Epigallocatechin gallate HEK-293T 84.41  LDD0183  [13]
 LDCM0625  F8 Ramos C327(0.69); C464(0.65); C453(0.18); C237(1.56)  LDD2187  [37]
 LDCM0572  Fragment10 Ramos C327(0.25); C464(0.54); C453(0.92); C237(0.39)  LDD2189  [37]
 LDCM0573  Fragment11 Ramos C327(0.76); C464(0.87); C453(20.00); C237(0.76)  LDD2190  [37]
 LDCM0574  Fragment12 Ramos C327(0.28); C464(0.65); C453(0.75); C237(0.26)  LDD2191  [37]
 LDCM0575  Fragment13 Ramos C327(1.02); C464(1.03); C453(0.75)  LDD2192  [37]
 LDCM0576  Fragment14 Ramos C327(0.63); C464(0.85); C237(0.70)  LDD2193  [37]
 LDCM0579  Fragment20 Ramos C327(0.21); C464(0.63); C453(0.48); C237(0.21)  LDD2194  [37]
 LDCM0580  Fragment21 Ramos C327(1.48); C464(1.08); C453(0.86); C237(0.43)  LDD2195  [37]
 LDCM0582  Fragment23 Ramos C327(0.24); C464(0.29); C453(0.27); C237(0.37)  LDD2196  [37]
 LDCM0578  Fragment27 Ramos C327(1.29); C464(1.28); C453(0.62); C237(0.84)  LDD2197  [37]
 LDCM0586  Fragment28 Ramos C327(0.48); C464(2.02); C453(1.06)  LDD2198  [37]
 LDCM0588  Fragment30 Ramos C327(0.99); C464(0.78); C453(0.63); C237(0.48)  LDD2199  [37]
 LDCM0589  Fragment31 Ramos C327(0.49); C464(1.27); C453(1.01); C237(0.87)  LDD2200  [37]
 LDCM0590  Fragment32 Ramos C327(0.29); C464(0.56); C453(0.44); C237(0.42)  LDD2201  [37]
 LDCM0468  Fragment33 Ramos C327(0.89); C464(0.88); C453(0.64); C237(0.58)  LDD2202  [37]
 LDCM0596  Fragment38 Ramos C327(0.78); C464(0.71); C453(0.83); C237(0.33)  LDD2203  [37]
 LDCM0566  Fragment4 Ramos C327(0.62); C464(0.66); C453(0.46); C237(0.57)  LDD2184  [37]
 LDCM0610  Fragment52 Ramos C327(1.05); C464(0.68); C453(0.95)  LDD2204  [37]
 LDCM0614  Fragment56 Ramos C327(0.50); C464(0.64); C453(1.01); C237(0.85)  LDD2205  [37]
 LDCM0569  Fragment7 Ramos C327(0.28); C464(0.53); C453(0.39); C237(0.48)  LDD2186  [37]
 LDCM0571  Fragment9 Ramos C327(0.27); C464(0.49); C453(0.70); C237(0.29)  LDD2188  [37]
 LDCM0116  HHS-0101 DM93 Y96(0.85); Y146(1.48)  LDD0264  [16]
 LDCM0117  HHS-0201 DM93 Y96(0.70); Y146(1.36)  LDD0265  [16]
 LDCM0118  HHS-0301 DM93 Y96(0.77); Y146(0.89)  LDD0266  [16]
 LDCM0119  HHS-0401 DM93 Y96(0.82); Y146(1.74)  LDD0267  [16]
 LDCM0120  HHS-0701 DM93 Y96(0.72); Y146(1.10)  LDD0268  [16]
 LDCM0107  IAA HeLa H402(0.00); C327(0.00); H388(0.00)  LDD0221  [29]
 LDCM0123  JWB131 DM93 Y146(0.86)  LDD0285  [15]
 LDCM0124  JWB142 DM93 Y146(2.27)  LDD0286  [15]
 LDCM0125  JWB146 DM93 Y146(1.04)  LDD0287  [15]
 LDCM0126  JWB150 DM93 Y146(3.83)  LDD0288  [15]
 LDCM0127  JWB152 DM93 Y146(2.65)  LDD0289  [15]
 LDCM0128  JWB198 DM93 Y146(0.58)  LDD0290  [15]
 LDCM0129  JWB202 DM93 Y146(1.33)  LDD0291  [15]
 LDCM0130  JWB211 DM93 Y146(0.98)  LDD0292  [15]
 LDCM0022  KB02 HEK-293T C453(0.95); C327(1.05); C261(1.00); C464(1.03)  LDD1492  [38]
 LDCM0023  KB03 HEK-293T C453(0.98); C327(1.06); C261(1.00); C464(1.08)  LDD1497  [38]
 LDCM0024  KB05 HMCB C465(1.62)  LDD3312  [9]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C327(1.01); C261(0.85)  LDD2102  [7]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C327(0.54); C464(1.05); C237(0.64)  LDD2121  [7]
 LDCM0109  NEM HeLa N.A.  LDD0223  [29]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C327(0.58); C464(1.08); C237(0.57)  LDD2089  [7]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C327(1.35); C261(1.42); C237(1.19)  LDD2090  [7]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C327(0.97); C261(1.08); C237(0.67)  LDD2092  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C327(1.01); C464(1.07); C237(0.67)  LDD2093  [7]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C261(0.89); C237(1.57)  LDD2094  [7]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C237(0.76)  LDD2096  [7]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C327(0.60); C453(0.96); C261(0.65)  LDD2097  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C327(0.87); C261(0.89); C237(0.97)  LDD2098  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C327(0.75); C261(0.84); C237(1.46)  LDD2099  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C327(1.01)  LDD2100  [7]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C327(0.71); C464(0.45)  LDD2101  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C327(0.73); C261(0.89)  LDD2104  [7]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C327(1.56); C237(1.08)  LDD2105  [7]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C327(0.80)  LDD2106  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C327(0.83); C464(1.16); C261(0.94); C237(1.08)  LDD2107  [7]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C327(0.80); C237(0.65)  LDD2108  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C327(0.78); C453(0.40); C464(0.48); C261(1.15)  LDD2109  [7]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C327(1.03)  LDD2110  [7]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C327(0.87); C453(0.85); C464(1.01); C237(1.29)  LDD2111  [7]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C327(0.66); C261(0.79)  LDD2114  [7]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C327(0.44); C261(1.09)  LDD2115  [7]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C327(0.16); C237(0.64)  LDD2118  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C453(1.44); C464(1.08); C261(1.06); C237(2.65)  LDD2119  [7]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C327(1.04); C453(0.98)  LDD2120  [7]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C327(0.13); C237(0.49)  LDD2122  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C327(0.73); C464(0.91); C261(1.08); C237(0.85)  LDD2123  [7]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C327(0.08); C237(0.43)  LDD2124  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C327(0.70); C464(1.01); C261(1.32); C237(0.74)  LDD2125  [7]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C237(0.65)  LDD2126  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C327(1.00); C464(0.97); C261(1.29); C237(0.77)  LDD2127  [7]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C327(1.35); C261(1.14)  LDD2128  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C327(0.85); C261(1.15); C237(0.93)  LDD2129  [7]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C327(0.61); C464(0.48); C261(0.60)  LDD2134  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C327(0.91); C464(1.80); C261(1.18); C237(0.61)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C327(0.98); C453(1.15); C237(1.23)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C327(0.80); C261(0.98); C237(0.96)  LDD2137  [7]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C237(3.14); C261(1.41); C327(1.15)  LDD1700  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C464(1.10); C261(0.82); C237(0.94)  LDD2140  [7]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C327(0.78); C261(0.52); C237(0.97)  LDD2141  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C327(0.99); C261(0.91)  LDD2143  [7]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C327(2.97); C453(2.09); C464(1.36)  LDD2144  [7]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C327(0.66)  LDD2145  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C327(0.79); C261(1.00)  LDD2146  [7]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C261(1.32)  LDD2147  [7]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C327(0.53); C453(0.35)  LDD2148  [7]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C327(0.11); C237(0.81)  LDD2149  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C327(0.44); C453(0.47); C261(0.96); C237(0.45)  LDD2150  [7]
 LDCM0032  Oleacein HEK-293T 11.32  LDD0184  [13]
 LDCM0029  Quercetin HEK-293T 12.19  LDD0181  [13]
 LDCM0131  RA190 MM1.R C327(1.25)  LDD0304  [39]
 LDCM0003  Sulforaphane MCF-7 2.34  LDD0042  [12]
 LDCM0021  THZ1 HeLa S3 C276(1.08); C237(1.04)  LDD0460  [11]

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
Regulator of nonsense transcripts 1 (UPF1) DNA2/NAM7 helicase family Q92900
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Eukaryotic peptide chain release factor subunit 1 (ETF1) Eukaryotic release factor 1 family P62495
Polyadenylate-binding protein 1 (PABPC1) Polyadenylate-binding protein type-1 family P11940

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

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 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.
3 Proteome-Wide Profiling of Cellular Targets Modified by Dopamine Metabolites Using a Bio-Orthogonally Functionalized Catecholamine. ACS Chem Biol. 2021 Nov 19;16(11):2581-2594. doi: 10.1021/acschembio.1c00629. Epub 2021 Nov 2.
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
5 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.
6 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.
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 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.
9 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
10 Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors. J Am Chem Soc. 2022 Mar 30;144(12):5377-5388. doi: 10.1021/jacs.1c12748. Epub 2022 Mar 2.
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12 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
13 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
14 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
15 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.
16 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.
17 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.
18 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
19 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.
20 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
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Mass spectrometry data entry: PXD028853
22 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
23 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
24 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
25 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
26 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
27 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
28 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
29 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.
30 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.
31 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.
32 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
33 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.
34 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.
35 A photoaffinity labeling strategy identified EF1A1 as a binding protein of cyclic dinucleotide 2'3'-cGAMP. Cell Chem Biol. 2022 Jan 20;29(1):133-144.e20. doi: 10.1016/j.chembiol.2021.08.006. Epub 2021 Sep 2.
36 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.
37 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
38 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
39 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.