Details of the Target

General Information of Target

Target ID LDTP06211
Target Name Caspase-8 (CASP8)
Gene Name CASP8
Gene ID 841
Synonyms
MCH5; Caspase-8; CASP-8; EC 3.4.22.61; Apoptotic cysteine protease; Apoptotic protease Mch-5; CAP4; FADD-homologous ICE/ced-3-like protease; FADD-like ICE; FLICE; ICE-like apoptotic protease 5; MORT1-associated ced-3 homolog; MACH) [Cleaved into: Caspase-8 subunit p18; Caspase-8 subunit p10]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDFSRNLYDIGEQLDSEDLASLKFLSLDYIPQRKQEPIKDALMLFQRLQEKRMLEESNLS
FLKELLFRINRLDLLITYLNTRKEEMERELQTPGRAQISAYRVMLYQISEEVSRSELRSF
KFLLQEEISKCKLDDDMNLLDIFIEMEKRVILGEGKLDILKRVCAQINKSLLKIINDYEE
FSKERSSSLEGSPDEFSNGEELCGVMTISDSPREQDSESQTLDKVYQMKSKPRGYCLIIN
NHNFAKAREKVPKLHSIRDRNGTHLDAGALTTTFEELHFEIKPHDDCTVEQIYEILKIYQ
LMDHSNMDCFICCILSHGDKGIIYGTDGQEAPIYELTSQFTGLKCPSLAGKPKVFFIQAC
QGDNYQKGIPVETDSEEQPYLEMDLSSPQTRYIPDEADFLLGMATVNNCVSYRNPAEGTW
YIQSLCQSLRERCPRGDDILTILTEVNYEVSNKDDKKNMGKQMPQPTFTLRKKLVFPSD
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Peptidase C14A family
Subcellular location
Cytoplasm
Function
Thiol protease that plays a key role in programmed cell death by acting as a molecular switch for apoptosis, necroptosis and pyroptosis, and is required to prevent tissue damage during embryonic development and adulthood. Initiator protease that induces extrinsic apoptosis by mediating cleavage and activation of effector caspases responsible for FAS/CD95-mediated and TNFRSF1A-induced cell death. Cleaves and activates effector caspases CASP3, CASP4, CASP6, CASP7, CASP9 and CASP10. Binding to the adapter molecule FADD recruits it to either receptor FAS/TNFRSF6 or TNFRSF1A. The resulting aggregate called the death-inducing signaling complex (DISC) performs CASP8 proteolytic activation. The active dimeric enzyme is then liberated from the DISC and free to activate downstream apoptotic proteases. Proteolytic fragments of the N-terminal propeptide (termed CAP3, CAP5 and CAP6) are likely retained in the DISC. In addition to extrinsic apoptosis, also acts as a negative regulator of necroptosis: acts by cleaving RIPK1 at 'Asp-324', which is crucial to inhibit RIPK1 kinase activity, limiting TNF-induced apoptosis, necroptosis and inflammatory response. Also able to initiate pyroptosis by mediating cleavage and activation of gasdermin-C and -D (GSDMC and GSDMD, respectively): gasdermin cleavage promotes release of the N-terminal moiety that binds to membranes and forms pores, triggering pyroptosis. Initiates pyroptosis following inactivation of MAP3K7/TAK1. Also acts as a regulator of innate immunity by mediating cleavage and inactivation of N4BP1 downstream of TLR3 or TLR4, thereby promoting cytokine production. May participate in the Granzyme B (GZMB) cell death pathways. Cleaves PARP1 and PARP2. Independent of its protease activity, promotes cell migration following phosphorylation at Tyr-380.; [Isoform 5]: Lacks the catalytic site and may interfere with the pro-apoptotic activity of the complex.; [Isoform 6]: Lacks the catalytic site and may interfere with the pro-apoptotic activity of the complex.; [Isoform 7]: Lacks the catalytic site and may interfere with the pro-apoptotic activity of the complex (Probable). Acts as an inhibitor of the caspase cascade.; [Isoform 8]: Lacks the catalytic site and may interfere with the pro-apoptotic activity of the complex.
TTD ID
T15700
Uniprot ID
Q14790
DrugMap ID
TTEVCT0
Ensemble ID
ENST00000264275.9
HGNC ID
HGNC:1509
ChEMBL ID
CHEMBL3776

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A431 Deletion: p.L62del .
C4II SNV: p.S99F DBIA    Probe Info 
CAL27 Deletion: p.I175TfsTer30 DBIA    Probe Info 
HCT15 SNV: p.P232H .
HEC1 SNV: p.R68Ter; p.K121E DBIA    Probe Info 
HEC1B SNV: p.R68Ter; p.K121E .
HT115 SNV: p.R68Q .
ICC9 SNV: p.R233Q .
JURKAT SNV: p.L48R Compound 10    Probe Info 
KYM1 SNV: p.R68P DBIA    Probe Info 
KYSE150 SNV: p.Q125Ter DBIA    Probe Info 
MINO SNV: p.F3C .
RKO Deletion: p.F120del DBIA    Probe Info 
SKMEL2 SNV: p.Q215H DBIA    Probe Info 
SUPT1 SNV: p.R233Q DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 19 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		13.11  LDD0402  [1]
STPyne
 Probe Info  		K130(1.69)  LDD0277  [2]
DBIA
 Probe Info  		C419(1.43)  LDD3310  [3]
BTD
 Probe Info  		C164(1.97)  LDD1700  [4]
Johansson_61
 Probe Info  		_(17.88)  LDD1485  [5]
AHL-Pu-1
 Probe Info  		C426(2.75)  LDD0168  [6]
HHS-475
 Probe Info  		Y365(1.06)  LDD0265  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		C345(0.00); C236(0.00); C426(0.00); C360(0.00)  LDD0038  [8]
IA-alkyne
 Probe Info  		C131(0.00); C345(0.00); C236(0.00); C426(0.00)  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		C131(0.00); C236(0.00); C426(0.00); C164(0.00)  LDD0037  [8]
NAIA_4
 Probe Info  		N.A.  LDD2226  [9]
WYneO
 Probe Info  		N.A.  LDD0022  [10]
Compound 10
 Probe Info  		N.A.  LDD2216  [11]
Compound 11
 Probe Info  		N.A.  LDD2213  [11]
IPM
 Probe Info  		N.A.  LDD0005  [10]
TFBX
 Probe Info  		N.A.  LDD0148  [12]
Acrolein
 Probe Info  		N.A.  LDD0217  [13]
AOyne
 Probe Info  		8.10  LDD0443  [14]
NAIA_5
 Probe Info  		N.A.  LDD2223  [9]

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 C164(0.51)  LDD2142  [4]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C164(0.68)  LDD2130  [4]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C164(0.96)  LDD2117  [4]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C164(1.28)  LDD2152  [4]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C164(0.93)  LDD2131  [4]
 LDCM0025  4SU-RNA HEK-293T C426(2.75)  LDD0168  [6]
 LDCM0026  4SU-RNA+native RNA HEK-293T C426(2.08); C360(3.64)  LDD0169  [6]
 LDCM0545  Acetamide MDA-MB-231 C164(0.37)  LDD2138  [4]
 LDCM0520  AKOS000195272 MDA-MB-231 C164(0.71)  LDD2113  [4]
 LDCM0156  Aniline NCI-H1299 9.12  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C164(0.37)  LDD2091  [4]
 LDCM0630  CCW28-3 231MFP C360(0.71)  LDD2214  [15]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [13]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C360(1.25)  LDD1702  [4]
 LDCM0202  EV-93 T cell C360(13.65)  LDD0514  [16]
 LDCM0625  F8 Ramos C164(0.51); C360(0.98)  LDD2187  [17]
 LDCM0572  Fragment10 MDA-MB-231 C360(2.81)  LDD1389  [5]
 LDCM0573  Fragment11 MDA-MB-231 C360(20.00)  LDD1391  [5]
 LDCM0574  Fragment12 Ramos C164(0.74); C360(1.01)  LDD2191  [17]
 LDCM0575  Fragment13 MDA-MB-231 C360(1.20)  LDD1469  [5]
 LDCM0576  Fragment14 MDA-MB-231 C360(1.42)  LDD1397  [5]
 LDCM0579  Fragment20 MDA-MB-231 C360(1.88)  LDD1402  [5]
 LDCM0580  Fragment21 MDA-MB-231 C360(1.87)  LDD1404  [5]
 LDCM0582  Fragment23 MDA-MB-231 C360(1.39)  LDD1408  [5]
 LDCM0583  Fragment24 Ramos C360(1.35)  LDD1410  [5]
 LDCM0584  Fragment25 MDA-MB-231 C360(0.98)  LDD1411  [5]
 LDCM0578  Fragment27 MDA-MB-231 C360(0.83)  LDD1401  [5]
 LDCM0586  Fragment28 MDA-MB-231 C360(1.11)  LDD1415  [5]
 LDCM0587  Fragment29 Ramos C360(1.60)  LDD1476  [5]
 LDCM0588  Fragment30 MDA-MB-231 C360(1.96)  LDD1419  [5]
 LDCM0589  Fragment31 MDA-MB-231 C360(0.54)  LDD1477  [5]
 LDCM0590  Fragment32 Ramos C164(0.63); C360(1.60)  LDD2201  [17]
 LDCM0468  Fragment33 MDA-MB-231 C360(3.05)  LDD1425  [5]
 LDCM0593  Fragment35 Ramos C360(1.31)  LDD1430  [5]
 LDCM0595  Fragment37 Ramos C360(1.02)  LDD1432  [5]
 LDCM0596  Fragment38 MDA-MB-231 C360(0.96)  LDD1433  [5]
 LDCM0566  Fragment4 MDA-MB-231 C360(12.31)  LDD1378  [5]
 LDCM0599  Fragment41 MDA-MB-231 C360(0.96)  LDD1438  [5]
 LDCM0603  Fragment45 MDA-MB-231 C360(20.00)  LDD1482  [5]
 LDCM0610  Fragment52 Ramos C164(0.98); C360(0.86)  LDD2204  [17]
 LDCM0612  Fragment54 MDA-MB-231 C360(1.16)  LDD1456  [5]
 LDCM0614  Fragment56 MDA-MB-231 C360(1.03)  LDD1458  [5]
 LDCM0615  Fragment63-R Jurkat _(15.23)  LDD1487  [5]
 LDCM0617  Fragment63-S Jurkat _(11.95)  LDD1490  [5]
 LDCM0569  Fragment7 Jurkat _(17.88)  LDD1485  [5]
 LDCM0570  Fragment8 Ramos C360(1.39)  LDD1386  [5]
 LDCM0571  Fragment9 Ramos C360(3.18)  LDD1464  [5]
 LDCM0117  HHS-0201 DM93 Y365(1.06)  LDD0265  [7]
 LDCM0119  HHS-0401 DM93 Y365(0.98)  LDD0267  [7]
 LDCM0015  HNE MDA-MB-231 C360(0.99)  LDD0346  [17]
 LDCM0022  KB02 Ramos 19.28  LDD0431  [18]
 LDCM0023  KB03 MDA-MB-231 C360(3.30)  LDD1376  [5]
 LDCM0024  KB05 COLO792 C419(1.43)  LDD3310  [3]
 LDCM0169  KB63 Ramos 20.00  LDD0432  [18]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C164(0.47)  LDD2121  [4]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C164(0.45)  LDD2089  [4]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C164(0.85)  LDD2092  [4]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C164(1.10)  LDD2094  [4]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C164(0.22)  LDD2096  [4]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C164(0.86)  LDD2097  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C164(0.95)  LDD2099  [4]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C164(0.69)  LDD2101  [4]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C164(0.44)  LDD2104  [4]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C164(0.95)  LDD2105  [4]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C164(1.00)  LDD2107  [4]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C164(0.37)  LDD2108  [4]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C164(0.62)  LDD2109  [4]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C164(0.93)  LDD2111  [4]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C164(0.42)  LDD2115  [4]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C164(0.53)  LDD2116  [4]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C164(0.60)  LDD2118  [4]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C164(2.19)  LDD2119  [4]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C164(0.48)  LDD2120  [4]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C164(0.60)  LDD2122  [4]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C164(0.58)  LDD2123  [4]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C164(0.35)  LDD2124  [4]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C164(0.64)  LDD2125  [4]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C164(0.41)  LDD2126  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C164(0.86)  LDD2127  [4]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C164(0.56)  LDD2128  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C164(0.91)  LDD2129  [4]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C164(0.53)  LDD2133  [4]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C164(0.40)  LDD2134  [4]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C164(1.11)  LDD2135  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C164(1.09)  LDD2136  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C164(1.12)  LDD2137  [4]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C164(1.97)  LDD1700  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C164(0.78)  LDD2140  [4]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C164(0.54)  LDD2143  [4]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C164(1.92)  LDD2144  [4]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C164(0.70)  LDD2146  [4]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C164(0.46)  LDD2148  [4]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C164(0.33)  LDD2149  [4]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C164(0.32)  LDD2150  [4]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C164(0.59)  LDD2151  [4]
 LDCM0627  NUDT7-COV-1 HEK-293T C360(0.33)  LDD2206  [19]
 LDCM0628  OTUB2-COV-1 HEK-293T C360(0.90)  LDD2207  [19]
 LDCM0131  RA190 MM1.R C203(1.49); C360(1.33)  LDD0304  [20]
 LDCM0170  Structure8 Ramos 13.90  LDD0433  [18]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cullin-3 (CUL3) Cullin family Q13618
CASP8 and FADD-like apoptosis regulator (CFLAR) Peptidase C14A family O15519
Caspase-10 (CASP10) Peptidase C14A family Q92851
Caspase-8 (CASP8) Peptidase C14A family Q14790
Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) Peptidase C14B family Q9UDY8
Tumor necrosis factor alpha-induced protein 3 (TNFAIP3) Peptidase C64 family P21580
Serine/threonine-protein kinase PLK1 (PLK1) Ser/Thr protein kinase family P53350
Integrin-linked protein kinase (ILK) TKL Ser/Thr protein kinase family Q13418
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) TKL Ser/Thr protein kinase family Q13546
RAF proto-oncogene serine/threonine-protein kinase (RAF1) TKL Ser/Thr protein kinase family P04049
Tyrosine-protein phosphatase non-receptor type 6 (PTPN6) Protein-tyrosine phosphatase family P29350
E3 ubiquitin-protein ligase RNF34 (RNF34) . Q969K3
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
B-cell receptor-associated protein 31 (BCAP31) BCAP29/BCAP31 family P51572
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Androgen receptor (AR) Nuclear hormone receptor family P10275
Cytokine and receptor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor ligand superfamily member 6 (FASLG) Tumor necrosis factor family P48023
Tumor necrosis factor receptor superfamily member 10A (TNFRSF10A) . O00220
Tumor necrosis factor receptor superfamily member 6 (FAS) . P25445
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Vacuolar protein sorting-associated protein 33A (VPS33A) STXBP/unc-18/SEC1 family Q96AX1
CASP8-associated protein 2 (CASP8AP2) . Q9UKL3
FAS-associated death domain protein (FADD) . Q13158
Nucleolar protein 3 (NOL3) . O60936

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetyl-ile-glu-thr-asp-aldehyde Small molecular drug D0N8TA
An-9 Small molecular drug DB05103
Bardoxolone Small molecular drug DB12651
Glionitrin A Small molecular drug D0Y2TI
Trichostatin A Small molecular drug DB04297
Amooranin . D08LIU
Bryostatin 1 . DB11752
Oleandrin . DB12843

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 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
3 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
4 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
5 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
6 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
7 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.
8 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
9 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
10 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
11 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
12 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
13 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.
14 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.
15 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.
16 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
17 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
18 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.
19 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
20 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.