General Information of Target

Target ID LDTP02198
Target Name Cathepsin D (CTSD)
Gene Name CTSD
Gene ID 1509
Synonyms
CPSD; Cathepsin D; EC 3.4.23.5) [Cleaved into: Cathepsin D light chain; Cathepsin D heavy chain]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQPSSLLPLALCLLAAPASALVRIPLHKFTSIRRTMSEVGGSVEDLIAKGPVSKYSQAVP
AVTEGPIPEVLKNYMDAQYYGEIGIGTPPQCFTVVFDTGSSNLWVPSIHCKLLDIACWIH
HKYNSDKSSTYVKNGTSFDIHYGSGSLSGYLSQDTVSVPCQSASSASALGGVKVERQVFG
EATKQPGITFIAAKFDGILGMAYPRISVNNVLPVFDNLMQQKLVDQNIFSFYLSRDPDAQ
PGGELMLGGTDSKYYKGSLSYLNVTRKAYWQVHLDQVEVASGLTLCKEGCEAIVDTGTSL
MVGPVDEVRELQKAIGAVPLIQGEYMIPCEKVSTLPAITLKLGGKGYKLSPEDYTLKVSQ
AGKTLCLSGFMGMDIPPPSGPLWILGDVFIGRYYTVFDRDNNRVGFAEAARL
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase A1 family
Subcellular location
Lysosome
Function
Acid protease active in intracellular protein breakdown. Plays a role in APP processing following cleavage and activation by ADAM30 which leads to APP degradation. Involved in the pathogenesis of several diseases such as breast cancer and possibly Alzheimer disease.
TTD ID
T67102
Uniprot ID
P07339
DrugMap ID
TTPT2QI
Ensemble ID
ENST00000236671.7
HGNC ID
HGNC:2529
ChEMBL ID
CHEMBL2581

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 36 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
9.87  LDD0402  [2]
Alkylaryl probe 1
 Probe Info 
13.00  LDD0385  [3]
Alkylaryl probe 2
 Probe Info 
16.00  LDD0391  [3]
ILS-2
 Probe Info 
3.69  LDD0416  [4]
FBPP2
 Probe Info 
131.86  LDD0318  [5]
C-Sul
 Probe Info 
4.31  LDD0066  [6]
YN-1
 Probe Info 
100.00  LDD0444  [7]
YN-4
 Probe Info 
100.00  LDD0445  [7]
ONAyne
 Probe Info 
K345(0.63); K357(0.69)  LDD0274  [8]
STPyne
 Probe Info 
K122(8.68); K127(7.54); K184(6.99); K28(5.57)  LDD0277  [8]
P11
 Probe Info 
20.00  LDD0201  [9]
Alkylaryl probe 3
 Probe Info 
10.30  LDD0282  [10]
DBIA
 Probe Info 
C286(1.53)  LDD3311  [11]
THZ1-DTB
 Probe Info 
C329(1.06)  LDD0460  [12]
BTD
 Probe Info 
C329(1.06)  LDD2089  [13]
AHL-Pu-1
 Probe Info 
C329(2.11)  LDD0171  [14]
EA-probe
 Probe Info 
N.A.  LDD0440  [15]
HHS-482
 Probe Info 
Y269(1.40); Y325(0.87)  LDD0285  [16]
FBP2
 Probe Info 
2.44  LDD0053  [5]
4-Iodoacetamidophenylacetylene
 Probe Info 
C329(0.00); C286(0.00)  LDD0038  [17]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [18]
Lodoacetamide azide
 Probe Info 
C329(0.00); C286(0.00); C290(0.00); C117(0.00)  LDD0037  [17]
ATP probe
 Probe Info 
N.A.  LDD0035  [19]
IPM
 Probe Info 
N.A.  LDD0025  [20]
WYneO
 Probe Info 
N.A.  LDD0022  [21]
NHS
 Probe Info 
K127(0.00); K357(0.00)  LDD0010  [21]
PF-06672131
 Probe Info 
N.A.  LDD0017  [22]
SF
 Probe Info 
N.A.  LDD0028  [23]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [24]
1c-yne
 Probe Info 
N.A.  LDD0228  [25]
Acrolein
 Probe Info 
N.A.  LDD0217  [26]
AOyne
 Probe Info 
15.00  LDD0443  [27]
MPP-AC
 Probe Info 
N.A.  LDD0428  [28]
NAIA_5
 Probe Info 
C329(0.00); C286(0.00); C117(0.00); C366(0.00)  LDD2223  [29]
TER-AC
 Probe Info 
N.A.  LDD0426  [28]
TPP-AC
 Probe Info 
N.A.  LDD0427  [28]
PAL-AfBPP Probe
Click To Hide/Show 25 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
PARPYnD
 Probe Info 
1.38  LDD0374  [30]
ILS-1 PP
 Probe Info 
8.40  LDD0417  [4]
IMP2070
 Probe Info 
11.49  LDD0367  [31]
FFF probe11
 Probe Info 
18.81  LDD0471  [32]
FFF probe12
 Probe Info 
17.41  LDD0473  [32]
FFF probe13
 Probe Info 
20.00  LDD0475  [32]
FFF probe14
 Probe Info 
19.81  LDD0477  [32]
FFF probe15
 Probe Info 
17.62  LDD0478  [32]
FFF probe2
 Probe Info 
18.03  LDD0463  [32]
FFF probe3
 Probe Info 
19.15  LDD0464  [32]
FFF probe4
 Probe Info 
16.31  LDD0466  [32]
FFF probe6
 Probe Info 
6.13  LDD0467  [32]
FFF probe7
 Probe Info 
20.00  LDD0483  [32]
FFF probe9
 Probe Info 
20.00  LDD0470  [32]
JN0003
 Probe Info 
20.00  LDD0469  [32]
VE-P
 Probe Info 
N.A.  LDD0396  [33]
DR-1
 Probe Info 
3.34  LDD0397  [34]
A-DA
 Probe Info 
2.05  LDD0145  [35]
Kambe_31
 Probe Info 
3.56  LDD0128  [36]
BD-F
 Probe Info 
G323(0.00); Y325(0.00); E324(0.00)  LDD0024  [37]
LD-F
 Probe Info 
Q240(0.00); E324(0.00); G323(0.00); P237(0.00)  LDD0015  [37]
Photocelecoxib
 Probe Info 
I321(0.00); G323(0.00)  LDD0019  [38]
Photoindomethacin
 Probe Info 
P319(0.00); G323(0.00); Y325(0.00)  LDD0154  [38]
Photonaproxen
 Probe Info 
N.A.  LDD0156  [38]
OEA-DA
 Probe Info 
20.00  LDD0046  [39]

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 C329(0.76)  LDD2142  [13]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C329(0.96)  LDD2130  [13]
 LDCM0026  4SU-RNA+native RNA DM93 C329(2.11)  LDD0171  [14]
 LDCM0088  C45 HEK-293T 20.00  LDD0201  [9]
 LDCM0108  Chloroacetamide HeLa C290(0.00); C329(0.00)  LDD0222  [26]
 LDCM0632  CL-Sc Hep-G2 C329(1.63); C117(0.75); C117(0.67)  LDD2227  [29]
 LDCM0189  Compound 16 HEK-293T 24.10  LDD0492  [32]
 LDCM0185  Compound 17 HEK-293T 8.89  LDD0504  [32]
 LDCM0182  Compound 18 HEK-293T 11.90  LDD0501  [32]
 LDCM0184  Compound 20 HEK-293T 17.24  LDD0503  [32]
 LDCM0191  Compound 21 HEK-293T 15.38  LDD0493  [32]
 LDCM0186  Compound 31 HEK-293T 13.99  LDD0506  [32]
 LDCM0187  Compound 32 HEK-293T 25.64  LDD0507  [32]
 LDCM0188  Compound 33 HEK-293T 10.20  LDD0505  [32]
 LDCM0190  Compound 34 HEK-293T 18.52  LDD0497  [32]
 LDCM0192  Compound 35 HEK-293T 15.87  LDD0491  [32]
 LDCM0193  Compound 36 HEK-293T 12.90  LDD0494  [32]
 LDCM0194  Compound 37 HEK-293T 18.87  LDD0498  [32]
 LDCM0195  Compound 38 HEK-293T 28.17  LDD0499  [32]
 LDCM0196  Compound 39 HEK-293T 11.30  LDD0496  [32]
 LDCM0197  Compound 40 HEK-293T 16.53  LDD0495  [32]
 LDCM0181  Compound 41 HEK-293T 10.64  LDD0502  [32]
 LDCM0183  Compound 42 HEK-293T 4.78  LDD0500  [32]
 LDCM0152  DR NCI-H1299 3.34  LDD0397  [34]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C329(1.26)  LDD1702  [13]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [15]
 LDCM0573  Fragment11 MDA-MB-231 C117(6.60)  LDD1391  [40]
 LDCM0576  Fragment14 MDA-MB-231 C117(0.66)  LDD1397  [40]
 LDCM0577  Fragment15 MDA-MB-231 C117(1.21)  LDD1399  [40]
 LDCM0579  Fragment20 MDA-MB-231 C117(12.51)  LDD1402  [40]
 LDCM0582  Fragment23 MDA-MB-231 C117(3.10)  LDD1408  [40]
 LDCM0584  Fragment25 MDA-MB-231 C117(0.97)  LDD1411  [40]
 LDCM0578  Fragment27 MDA-MB-231 C117(0.57)  LDD1401  [40]
 LDCM0587  Fragment29 MDA-MB-231 C117(1.42)  LDD1417  [40]
 LDCM0589  Fragment31 MDA-MB-231 C117(1.32)  LDD1421  [40]
 LDCM0590  Fragment32 MDA-MB-231 C117(2.87)  LDD1423  [40]
 LDCM0596  Fragment38 MDA-MB-231 C117(1.23)  LDD1433  [40]
 LDCM0597  Fragment39 MDA-MB-231 C117(1.29)  LDD1435  [40]
 LDCM0566  Fragment4 Ramos C117(1.54)  LDD2184  [41]
 LDCM0598  Fragment40 MDA-MB-231 C117(1.02)  LDD1436  [40]
 LDCM0599  Fragment41 MDA-MB-231 C117(1.32)  LDD1438  [40]
 LDCM0601  Fragment43 MDA-MB-231 C117(3.12)  LDD1441  [40]
 LDCM0603  Fragment45 MDA-MB-231 C117(20.00)  LDD1444  [40]
 LDCM0604  Fragment46 MDA-MB-231 C117(1.21)  LDD1445  [40]
 LDCM0605  Fragment47 MDA-MB-231 C117(1.92)  LDD1446  [40]
 LDCM0608  Fragment50 MDA-MB-231 C117(6.19)  LDD1449  [40]
 LDCM0610  Fragment52 MDA-MB-231 C117(1.10)  LDD1452  [40]
 LDCM0614  Fragment56 MDA-MB-231 C117(1.63)  LDD1458  [40]
 LDCM0568  Fragment6 MDA-MB-231 C117(1.35)  LDD1382  [40]
 LDCM0569  Fragment7 MDA-MB-231 C117(3.54)  LDD1383  [40]
 LDCM0570  Fragment8 MDA-MB-231 C117(6.19)  LDD1385  [40]
 LDCM0571  Fragment9 MDA-MB-231 C117(2.13)  LDD1387  [40]
 LDCM0123  JWB131 DM93 Y269(1.40); Y325(0.87)  LDD0285  [16]
 LDCM0124  JWB142 DM93 Y269(1.30); Y325(1.26)  LDD0286  [16]
 LDCM0125  JWB146 DM93 Y269(1.37); Y325(1.17)  LDD0287  [16]
 LDCM0126  JWB150 DM93 Y269(2.14); Y325(3.17)  LDD0288  [16]
 LDCM0127  JWB152 DM93 Y269(1.56); Y325(1.67)  LDD0289  [16]
 LDCM0128  JWB198 DM93 Y269(0.57)  LDD0290  [16]
 LDCM0129  JWB202 DM93 Y269(0.74); Y325(0.92)  LDD0291  [16]
 LDCM0130  JWB211 DM93 Y269(1.11); Y325(1.12)  LDD0292  [16]
 LDCM0073  Kambe_cp3 PC-3 3.56  LDD0128  [36]
 LDCM0079  kambe_cp64 PC-3 2.30  LDD0135  [36]
 LDCM0022  KB02 MDA-MB-231 C117(20.00)  LDD1374  [40]
 LDCM0023  KB03 MDA-MB-231 C117(20.00)  LDD1376  [40]
 LDCM0024  KB05 G361 C286(1.53)  LDD3311  [11]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C329(1.06)  LDD2089  [13]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C329(0.83)  LDD2106  [13]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C329(0.76)  LDD2125  [13]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C329(1.30)  LDD2136  [13]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C329(0.77)  LDD2150  [13]
 LDCM0099  Phenelzine HEK-293T 10.30  LDD0282  [10]
 LDCM0084  Ro 48-8071 A-549 2.05  LDD0145  [35]
 LDCM0021  THZ1 HeLa S3 C329(1.06)  LDD0460  [12]
 LDCM0008  Tranylcypromine SH-SY5Y 2.44  LDD0053  [5]

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
Peptidoglycan recognition protein 3 (PGLYRP3) N-acetylmuramoyl-L-alanine amidase 2 family Q96LB9
Inactive C-alpha-formylglycine-generating enzyme 2 (SUMF2) Sulfatase-modifying factor family Q8NBJ7
Kinesin-like protein KIF1A (KIF1A) Kinesin family Q12756
NEDD4-like E3 ubiquitin-protein ligase WWP2 (WWP2) . O00308
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
Voltage-dependent anion-selective channel protein 2 (VDAC2) Eukaryotic mitochondrial porin family P45880
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 497 (ZNF497) Krueppel C2H2-type zinc-finger protein family Q6ZNH5
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Probable G-protein coupled receptor 141 (GPR141) G-protein coupled receptor 1 family Q7Z602
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Epidermal growth factor receptor kinase substrate 8-like protein 2 (EPS8L2) EPS8 family Q9H6S3
Progranulin (GRN) Granulin family P28799
Histone H3.1 (H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3C10; H3C11; H3C12) Histone H3 family P68431
Late cornified envelope protein 2A (LCE2A) LCE family Q5TA79
Protein sprouty homolog 4 (SPRY4) Sprouty family Q9C004
Synaptotagmin-3 (SYT3) Synaptotagmin family Q9BQG1
Putative insulin-like growth factor 2-associated protein . P09565

The Drug(s) Related To This Target

Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid10498202c1 Small molecular drug D0FE7H
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1h-benoximidazole-2-carboxylic Acid Small molecular drug D0W5NB
2-morpholinoethylamine Small molecular drug DB03096
Alpha-d-mannose Small molecular drug D07LUR
Carbocyclic Peptidomimetic Small molecular drug D0H3EJ
Grassystatin A Small molecular drug D0Y5IQ
Grl-7234 Small molecular drug D02LCH
Kni-10006 Small molecular drug D0S3BO
N-aminoethylmorpholine Small molecular drug D07DYJ
Pmid8410973c3 Small molecular drug D0P6RT
S-methylcysteine Small molecular drug D0CU4Q
5-amino-6-cyclohexyl-4-hydroxy-2-isobutyl-hexanoic Acid . DB07542
Cyclohexylmethyl-23-dihydroxy-5-methyl-hexylamide . DB08740
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ci-992 Small molecular drug D04TSV

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
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 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
4 A Chemical Proteomic Analysis of Illudin-Interacting Proteins. Chemistry. 2019 Sep 25;25(54):12644-12651. doi: 10.1002/chem.201902919. Epub 2019 Sep 3.
Mass spectrometry data entry: PXD014175
5 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
6 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.
7 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.
8 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
9 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.
10 Activity-Based Hydrazine Probes for Protein Profiling of Electrophilic Functionality in Therapeutic Targets. ACS Cent Sci. 2021 Sep 22;7(9):1524-1534. doi: 10.1021/acscentsci.1c00616. Epub 2021 Aug 19.
11 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
12 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.
13 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
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 Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
16 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.
17 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
18 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
19 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
20 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
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 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
23 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
24 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
25 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.
26 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.
27 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.
28 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.
29 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
30 Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333. doi: 10.1021/acschembio.9b00963. Epub 2020 Feb 10.
31 A Probe for NLRP3 Inflammasome Inhibitor MCC950 Identifies Carbonic Anhydrase 2 as a Novel Target. ACS Chem Biol. 2021 Jun 18;16(6):982-990. doi: 10.1021/acschembio.1c00218. Epub 2021 May 18.
Mass spectrometry data entry: PXD024915 , PXD024913
32 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.
33 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.
34 Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor. ACS Med Chem Lett. 2020 Feb 5;11(4):535-540. doi: 10.1021/acsmedchemlett.9b00658. eCollection 2020 Apr 9.
35 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.
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37 Evaluation of fully-functionalized diazirine tags for chemical proteomic applications. Chem Sci. 2021 May 7;12(22):7839-7847. doi: 10.1039/d1sc01360b.
Mass spectrometry data entry: PXD025652
38 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094
39 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
40 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.
41 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