Details of the Target

General Information of Target

Target ID LDTP01328
Target Name CAAX prenyl protease 1 homolog (ZMPSTE24)
Gene Name ZMPSTE24
Gene ID 10269
Synonyms
FACE1; STE24; CAAX prenyl protease 1 homolog; EC 3.4.24.84; Farnesylated proteins-converting enzyme 1; FACE-1; Prenyl protein-specific endoprotease 1; Zinc metalloproteinase Ste24 homolog
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGMWASLDALWEMPAEKRIFGAVLLFSWTVYLWETFLAQRQRRIYKTTTHVPPELGQIMD
SETFEKSRLYQLDKSTFSFWSGLYSETEGTLILLFGGIPYLWRLSGRFCGYAGFGPEYEI
TQSLVFLLLATLFSALTGLPWSLYNTFVIEEKHGFNQQTLGFFMKDAIKKFVVTQCILLP
VSSLLLYIIKIGGDYFFIYAWLFTLVVSLVLVTIYADYIAPLFDKFTPLPEGKLKEEIEV
MAKSIDFPLTKVYVVEGSKRSSHSNAYFYGFFKNKRIVLFDTLLEEYSVLNKDIQEDSGM
EPRNEEEGNSEEIKAKVKNKKQGCKNEEVLAVLGHELGHWKLGHTVKNIIISQMNSFLCF
FLFAVLIGRKELFAAFGFYDSQPTLIGLLIIFQFIFSPYNEVLSFCLTVLSRRFEFQADA
FAKKLGKAKDLYSALIKLNKDNLGFPVSDWLFSMWHYSHPPLLERLQALKTMKQH
Target Bioclass
Enzyme
Family
Peptidase M48A family
Subcellular location
Endoplasmic reticulum membrane
Function
Transmembrane metalloprotease whose catalytic activity is critical for processing lamin A/LMNA on the inner nuclear membrane and clearing clogged translocons on the endoplasmic reticulum. Proteolytically removes the C-terminal three residues of farnesylated proteins. Plays also an antiviral role independently of its protease activity by restricting enveloped RNA and DNA viruses, including influenza A, Zika, Ebola, Sindbis, vesicular stomatitis, cowpox, and vaccinia. Mechanistically, controls IFITM antiviral pathway to hinder viruses from breaching the endosomal barrier by modulating membrane fluidity.
Uniprot ID
O75844
Ensemble ID
ENST00000372759.4
HGNC ID
HGNC:12877
ChEMBL ID
CHEMBL3739253

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 20 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
HDSF-alk
 Probe Info  		2.56  LDD0197  [1]
CHEMBL5175495
 Probe Info  		9.57  LDD0196  [2]
CY4
 Probe Info  		100.00  LDD0244  [3]
TH211
 Probe Info  		Y253(8.19)  LDD0260  [4]
C-Sul
 Probe Info  		3.93  LDD0066  [5]
TH214
 Probe Info  		Y253(13.54)  LDD0258  [4]
TH216
 Probe Info  		Y253(7.03)  LDD0259  [4]
YN-1
 Probe Info  		100.00  LDD0444  [6]
YN-4
 Probe Info  		100.00  LDD0445  [6]
ONAyne
 Probe Info  		K470(0.68)  LDD0274  [7]
STPyne
 Probe Info  		K251(3.58); K259(7.69); K423(7.14); K429(0.39)  LDD0277  [7]
OPA-S-S-alkyne
 Probe Info  		K259(2.08)  LDD3494  [8]
Probe 1
 Probe Info  		Y253(9.06); Y432(13.10)  LDD3495  [9]
P26
 Probe Info  		4.18  LDD0409  [10]
HPAP
 Probe Info  		5.27  LDD0064  [11]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [12]
NHS
 Probe Info  		K251(0.00); K429(0.00)  LDD0010  [13]
SF
 Probe Info  		Y253(0.00); Y432(0.00)  LDD0028  [14]
Acrolein
 Probe Info  		N.A.  LDD0217  [15]
NAIA_5
 Probe Info  		N.A.  LDD2223  [16]
PAL-AfBPP Probe
Click To Hide/Show 187 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DR-1
 Probe Info  		2.54  LDD0398  [17]
PARPYnD
 Probe Info  		2.34  LDD0374  [18]
IMP2070
 Probe Info  		1.61  LDD0280  [19]
C004
 Probe Info  		15.56  LDD1714  [20]
C007
 Probe Info  		5.31  LDD1716  [20]
C010
 Probe Info  		6.19  LDD1719  [20]
C011
 Probe Info  		5.10  LDD1720  [20]
C022
 Probe Info  		18.90  LDD1728  [20]
C026
 Probe Info  		6.77  LDD1732  [20]
C027
 Probe Info  		6.54  LDD1733  [20]
C039
 Probe Info  		6.11  LDD1739  [20]
C040
 Probe Info  		27.10  LDD1740  [20]
C041
 Probe Info  		12.13  LDD1741  [20]
C049
 Probe Info  		7.36  LDD1747  [20]
C053
 Probe Info  		6.87  LDD1751  [20]
C055
 Probe Info  		19.29  LDD1752  [20]
C056
 Probe Info  		29.24  LDD1753  [20]
C063
 Probe Info  		27.86  LDD1760  [20]
C064
 Probe Info  		9.65  LDD1761  [20]
C067
 Probe Info  		5.43  LDD1763  [20]
C070
 Probe Info  		15.45  LDD1766  [20]
C072
 Probe Info  		10.34  LDD1768  [20]
C082
 Probe Info  		9.00  LDD1774  [20]
C087
 Probe Info  		27.67  LDD1779  [20]
C091
 Probe Info  		30.06  LDD1782  [20]
C092
 Probe Info  		56.49  LDD1783  [20]
C094
 Probe Info  		64.00  LDD1785  [20]
C095
 Probe Info  		6.19  LDD1786  [20]
C100
 Probe Info  		8.82  LDD1789  [20]
C106
 Probe Info  		37.27  LDD1793  [20]
C107
 Probe Info  		10.06  LDD1794  [20]
C108
 Probe Info  		17.51  LDD1795  [20]
C112
 Probe Info  		53.82  LDD1799  [20]
C117
 Probe Info  		10.20  LDD1804  [20]
C129
 Probe Info  		9.65  LDD1811  [20]
C130
 Probe Info  		12.38  LDD1812  [20]
C134
 Probe Info  		44.63  LDD1816  [20]
C135
 Probe Info  		25.81  LDD1817  [20]
C139
 Probe Info  		16.80  LDD1821  [20]
C140
 Probe Info  		10.41  LDD1822  [20]
C141
 Probe Info  		20.97  LDD1823  [20]
C143
 Probe Info  		23.10  LDD1825  [20]
C147
 Probe Info  		8.82  LDD1829  [20]
C152
 Probe Info  		21.11  LDD1833  [20]
C153
 Probe Info  		31.56  LDD1834  [20]
C159
 Probe Info  		24.76  LDD1839  [20]
C160
 Probe Info  		27.10  LDD1840  [20]
C161
 Probe Info  		37.53  LDD1841  [20]
C163
 Probe Info  		11.47  LDD1843  [20]
C164
 Probe Info  		15.35  LDD1844  [20]
C165
 Probe Info  		16.68  LDD1845  [20]
C166
 Probe Info  		8.28  LDD1846  [20]
C169
 Probe Info  		93.70  LDD1849  [20]
C170
 Probe Info  		8.82  LDD1850  [20]
C172
 Probe Info  		5.31  LDD1852  [20]
C173
 Probe Info  		6.68  LDD1853  [20]
C177
 Probe Info  		10.20  LDD1856  [20]
C178
 Probe Info  		22.32  LDD1857  [20]
C183
 Probe Info  		5.10  LDD1861  [20]
C186
 Probe Info  		13.09  LDD1864  [20]
C187
 Probe Info  		25.81  LDD1865  [20]
C191
 Probe Info  		23.59  LDD1868  [20]
C193
 Probe Info  		19.16  LDD1869  [20]
C194
 Probe Info  		22.16  LDD1870  [20]
C196
 Probe Info  		20.82  LDD1872  [20]
C197
 Probe Info  		9.85  LDD1873  [20]
C198
 Probe Info  		19.97  LDD1874  [20]
C199
 Probe Info  		7.16  LDD1875  [20]
C201
 Probe Info  		79.34  LDD1877  [20]
C204
 Probe Info  		4.96  LDD1879  [20]
C205
 Probe Info  		4.99  LDD1880  [20]
C206
 Probe Info  		38.85  LDD1881  [20]
C208
 Probe Info  		5.06  LDD1883  [20]
C210
 Probe Info  		58.89  LDD1884  [20]
C211
 Probe Info  		12.82  LDD1885  [20]
C213
 Probe Info  		18.90  LDD1887  [20]
C216
 Probe Info  		7.41  LDD1890  [20]
C218
 Probe Info  		34.30  LDD1892  [20]
C219
 Probe Info  		8.69  LDD1893  [20]
C220
 Probe Info  		36.25  LDD1894  [20]
C222
 Probe Info  		8.69  LDD1896  [20]
C225
 Probe Info  		11.31  LDD1898  [20]
C226
 Probe Info  		14.83  LDD1899  [20]
C228
 Probe Info  		40.22  LDD1901  [20]
C229
 Probe Info  		8.57  LDD1902  [20]
C231
 Probe Info  		33.13  LDD1904  [20]
C232
 Probe Info  		62.68  LDD1905  [20]
C233
 Probe Info  		11.63  LDD1906  [20]
C234
 Probe Info  		33.82  LDD1907  [20]
C235
 Probe Info  		27.67  LDD1908  [20]
C238
 Probe Info  		25.81  LDD1911  [20]
C240
 Probe Info  		12.73  LDD1913  [20]
C243
 Probe Info  		35.02  LDD1916  [20]
C244
 Probe Info  		15.24  LDD1917  [20]
C246
 Probe Info  		39.95  LDD1919  [20]
C249
 Probe Info  		14.32  LDD1922  [20]
C252
 Probe Info  		22.32  LDD1925  [20]
C264
 Probe Info  		32.45  LDD1935  [20]
C265
 Probe Info  		23.26  LDD1936  [20]
C266
 Probe Info  		18.13  LDD1937  [20]
C270
 Probe Info  		10.48  LDD1940  [20]
C273
 Probe Info  		10.85  LDD1943  [20]
C277
 Probe Info  		15.78  LDD1947  [20]
C278
 Probe Info  		62.68  LDD1948  [20]
C280
 Probe Info  		13.64  LDD1950  [20]
C282
 Probe Info  		34.78  LDD1952  [20]
C284
 Probe Info  		44.02  LDD1954  [20]
C285
 Probe Info  		41.07  LDD1955  [20]
C287
 Probe Info  		21.71  LDD1957  [20]
C288
 Probe Info  		18.00  LDD1958  [20]
C289
 Probe Info  		53.82  LDD1959  [20]
C290
 Probe Info  		9.19  LDD1960  [20]
C293
 Probe Info  		41.93  LDD1963  [20]
C296
 Probe Info  		25.99  LDD1966  [20]
C297
 Probe Info  		5.86  LDD1967  [20]
C299
 Probe Info  		23.75  LDD1968  [20]
C301
 Probe Info  		5.03  LDD1970  [20]
C303
 Probe Info  		5.21  LDD1972  [20]
C305
 Probe Info  		16.00  LDD1974  [20]
C307
 Probe Info  		6.54  LDD1975  [20]
C310
 Probe Info  		17.51  LDD1977  [20]
C313
 Probe Info  		13.83  LDD1980  [20]
C314
 Probe Info  		22.01  LDD1981  [20]
C320
 Probe Info  		6.87  LDD1986  [20]
C322
 Probe Info  		10.41  LDD1988  [20]
C326
 Probe Info  		14.32  LDD1990  [20]
C327
 Probe Info  		7.84  LDD1991  [20]
C338
 Probe Info  		56.89  LDD2001  [20]
C339
 Probe Info  		8.28  LDD2002  [20]
C343
 Probe Info  		20.68  LDD2005  [20]
C348
 Probe Info  		17.75  LDD2009  [20]
C349
 Probe Info  		41.64  LDD2010  [20]
C350
 Probe Info  		65.80  LDD2011  [20]
C353
 Probe Info  		7.89  LDD2014  [20]
C354
 Probe Info  		7.52  LDD2015  [20]
C355
 Probe Info  		34.30  LDD2016  [20]
C356
 Probe Info  		14.72  LDD2017  [20]
C357
 Probe Info  		8.82  LDD2018  [20]
C361
 Probe Info  		19.70  LDD2022  [20]
C362
 Probe Info  		99.73  LDD2023  [20]
C363
 Probe Info  		24.42  LDD2024  [20]
C364
 Probe Info  		31.78  LDD2025  [20]
C366
 Probe Info  		22.32  LDD2027  [20]
C367
 Probe Info  		9.45  LDD2028  [20]
C373
 Probe Info  		11.79  LDD2033  [20]
C376
 Probe Info  		8.75  LDD2036  [20]
C378
 Probe Info  		8.28  LDD2037  [20]
C380
 Probe Info  		8.69  LDD2039  [20]
C382
 Probe Info  		20.68  LDD2041  [20]
C383
 Probe Info  		18.64  LDD2042  [20]
C386
 Probe Info  		7.41  LDD2045  [20]
C388
 Probe Info  		82.71  LDD2047  [20]
C390
 Probe Info  		57.28  LDD2049  [20]
C392
 Probe Info  		5.06  LDD2051  [20]
C396
 Probe Info  		9.65  LDD2055  [20]
C399
 Probe Info  		12.21  LDD2058  [20]
C403
 Probe Info  		31.12  LDD2061  [20]
C407
 Probe Info  		22.78  LDD2064  [20]
C408
 Probe Info  		5.43  LDD2065  [20]
C409
 Probe Info  		9.71  LDD2066  [20]
C413
 Probe Info  		18.00  LDD2069  [20]
C416
 Probe Info  		5.50  LDD2071  [20]
C419
 Probe Info  		17.63  LDD2074  [20]
C420
 Probe Info  		13.83  LDD2075  [20]
C423
 Probe Info  		10.20  LDD2078  [20]
C424
 Probe Info  		9.25  LDD2079  [20]
C426
 Probe Info  		24.59  LDD2081  [20]
C428
 Probe Info  		5.21  LDD2083  [20]
C429
 Probe Info  		27.86  LDD2084  [20]
C431
 Probe Info  		46.21  LDD2086  [20]
FFF probe11
 Probe Info  		13.67  LDD0471  [21]
FFF probe13
 Probe Info  		20.00  LDD0475  [21]
FFF probe14
 Probe Info  		20.00  LDD0477  [21]
FFF probe15
 Probe Info  		9.60  LDD0478  [21]
FFF probe2
 Probe Info  		12.96  LDD0463  [21]
FFF probe3
 Probe Info  		20.00  LDD0464  [21]
FFF probe4
 Probe Info  		12.13  LDD0466  [21]
FFF probe6
 Probe Info  		7.45  LDD0467  [21]
FFF probe9
 Probe Info  		6.04  LDD0485  [21]
JN0003
 Probe Info  		20.00  LDD0469  [21]
STS-1
 Probe Info  		N.A.  LDD0136  [22]
STS-2
 Probe Info  		N.A.  LDD0138  [22]
VE-P
 Probe Info  		N.A.  LDD0396  [23]
Alk-rapa
 Probe Info  		7.09  LDD0213  [24]
Staurosporine capture compound
 Probe Info  		N.A.  LDD0083  [25]
KIRA6 AfBP
 Probe Info  		N.A.  LDD0378  [26]
OEA-DA
 Probe Info  		11.91  LDD0046  [27]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa H50(0.00); H335(0.00)  LDD0222  [15]
 LDCM0107  IAA HeLa H339(0.00); H50(0.00); H335(0.00)  LDD0221  [15]
 LDCM0109  NEM HeLa H50(0.00); H339(0.00)  LDD0223  [15]
 LDCM0159  P28 BxPC-3 4.18  LDD0409  [10]
 LDCM0014  Panhematin hPBMC 5.27  LDD0064  [11]
 LDCM0090  Rapamycin JHH-7 7.09  LDD0213  [24]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [25]

References

1 Fatty Acyl Sulfonyl Fluoride as an Activity-Based Probe for Profiling Fatty Acid-Associated Proteins in Living Cells. Chembiochem. 2022 Feb 16;23(4):e202100628. doi: 10.1002/cbic.202100628. Epub 2021 Dec 30.
2 Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20. ACS Med Chem Lett. 2022 Sep 26;13(10):1648-1654. doi: 10.1021/acsmedchemlett.2c00336. eCollection 2022 Oct 13.
3 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.
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 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.
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 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
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 Integrated phenotypic screening and activity-based protein profiling to reveal potential therapy targets of pancreatic cancer. Chem Commun (Camb). 2019 Jan 31;55(11):1596-1599. doi: 10.1039/c8cc08753a.
11 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
12 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
13 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
14 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
15 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.
16 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
17 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.
18 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.
19 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
20 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
21 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.
22 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
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Mass spectrometry data entry: PXD022628
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Mass spectrometry data entry: PXD007570