Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47

ACS Medicinal Chemistry Letters

Volumn 3, Issue 10, 2012, Pages 789-792

  Weinstock, Joseph ^a   Wu, Jian ^a   Cao, Ping ^a   Kingsbury, William D ^a   McDermott, Jeffrey L ^a   Kodrasov, Matthew P ^a   McKelvey, Devin M ^a   Suresh Kumar, K G ^a   Goldenberg, Seth J ^a   Mattern, Michael R ^a   Nicholson, Benjamin ^a  

^a Progenra Inc   (United States)

Author keywords

deubiquitylase; p53; Pol ; Ubiquitin isopeptidase

Indexed keywords

ANTINEOPLASTIC AGENT; CYSTEINE PROTEINASE; CYSTEINE PROTEINASE INHIBITOR; PROTEIN P53; UBIQUITIN SPECIFIC PROTEASE 47; UBIQUITIN SPECIFIC PROTEASE 7; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; B CELL LEUKEMIA; CANCER CELL CULTURE; COLORECTAL CANCER; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG METABOLISM; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VIVO STUDY; MOLECULARLY TARGETED THERAPY; MULTIPLE MYELOMA; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

EID: 84867369144     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml200276j     Document Type: Article

References (17)

1. Dye, B.; Schulman, B. A. Structural mechanisms underlying posttranslational modification by ubiquitin-like proteins Annu. Rev. Biophys. Biomol. Struct. 2007, 36, 131-150
2. Hershko, A.; Ciechanover, A. The ubiquitin-proteasome pathway Annu. Rev. Biochem. 1998, 67, 425-479
3. Nijman, S. M.; Luna-Vargas, M. P.; Velds, A.; Brummelkamp, T. R.; Dirac, A. M. A genomic and functional inventory of deubiquitinating enzymes Cell 2005, 123, 773-786
4. Reyes-Turcu, F. E.; Ventii, K. H.; Wilkinson, K. D. Regulation and cellular roles of ubiquitin-specific deubiquitibnating enzymes Annu. Rev. Biochem. 2009, 78, 363-397
5. Nicholson, B.; Suresh Kumar, K. G. The multifaceted roles of USP7: new therapeutic opportunities Cell. Biochem. Biophys. 2011, 60, 61-68
6. Waring, D.; Lebman, J. A.; Batuello, C. N.; Mayo, L. D. Controlling the Mdm2-Mdmx-p53 circuit Pharmaceuticals 2010, 3, 1576-1593
7. Catic, A.; Fiebiger, E.; Korbel, G. A.; Blom, D.; Galardy, P. J. Screen for ISG15-crossreactive deubiquitinases PLoS ONE 2007, 2, e679
8. Parsons, J. L.; Khoronenkova, S. V.; Edelmann, M. J.; Kessler, B. M.; Dianov, G. L. USP47 is a deubiquitylating enzyme that regulates base excision repair by controlling steady-state levels of DNA polymerase b Mol. Cell 2011, 41, 609-615
9. Peschiaroli, A.; Skaar, J. R.; Pagano, M.; Melino, G. The ubiquitin specific protease USP47 is a novel beta-TrCP interactor regulating cell survival Oncogene 2010, 29, 1384-1393
10. Colland, F.; Formstecher, E.; Jacq, X.; Reverdy, C.; Planquette, C. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells Mol. Cancer Ther. 2009, 8, 2286-2295
11. Guedat, P.; Boissy, G.; Borg-Capra, C.; Colland, F.; Daviet, L. Novel cysteine protease inhibitors and their therapeutic applications; Hybrigenics SA: US20070032499, 2007.
12. Nicholson, B.; Leach, C. A.; Goldenberg, S. J.; Francis, D. M.; Kodrasov, M. P. Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities Protein Sci. 2008, 17, 1035-1043
13. Dolman, H.; Kuipers, J. New thio compounds having fungicidal activity. European Patent Application, 1987, 0234622, A1.
14. Basha, A.; Lipton, M.; Weinreb, S. M. A mild, general method for conversion of esters to amides Tetrahedron Lett. 1977, 18, 4171-4174
15. Altun, M.; Kramer, H. B.; Willems, L. I.; McDermott, J. L.; Leach, C. A. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes Chem. Biol. 2011, 18, 1401-1412
16. Jiang, H.; Lin, J.; Su, Z. Z.; Collart, F. R.; Huberman, E. Induction of differentiation in human promyelocytic HL-60 leukemia cells activates p21, WAF1/CIP1, expression in the absence of p53 Oncogene 1994, 9, 3397-3406
17. Ponzio, G.; Loubat, A.; Rochet, N.; Turchi, L.; Rezzonico, R. Early G1 growth arrest of hybridoma B cells by DMSO involves cyclin D2 inhibition and p21[CIP1] induction Oncogene 1998, 17, 1159-1166