The multifaceted roles of USP7: new therapeutic opportunitiesBenjamin Nicholson
Progenra Inc, 277 Great Valley Parkway, Malvern, PA 19355, USA
Cell Biochem Biophys 60:61-8. 2011
..Taken together, USP7 inhibitors hold promise as a new strategy for the treatment of disease...
- Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities
Benjamin Nicholson
Division of Research and Development, Progenra, Inc, Malvern, Pennsylvania 19355, USA
Protein Sci 17:1035-43. 2008
..Taken together, these studies illustrate the utility of the reporter-based approach to measuring isopeptidase activity...
- Deubiquitinating enzymes as novel anticancer targets
Benjamin Nicholson
Progenra, Inc, 271A Great Valley Parkway, Malvern, PA 19355, USA
Future Oncol 3:191-9. 2007
..In the following review, this fascinating class of regulatory enzymes will be described, and specific examples of DUBs that are viable targets for anticancer therapy will be considered...
- Targeting the ubiquitin E3 ligase MuRF1 to inhibit muscle atrophy
Michael J Eddins
Progenra, Inc, 277 Great Valley Parkway, Malvern, PA 19355, USA
Cell Biochem Biophys 60:113-8. 2011
..Thus MuRF1 can be targeted in a specific manner and produce positive results in cellular atrophy models...
- Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format
Xufan Tian
Division of Research and Development, Progenra, Inc, Malvern, Pennsylvania 19355, USA
Assay Drug Dev Technol 9:165-73. 2011
..Specifically, we have used this assay format to characterize P022077, a selective ubiquitin-specific protease 7 inhibitor discovered at Progenra...
- Strategies for the identification of ubiquitin ligase inhibitors
Seth J Goldenberg
Progenra Inc, 271A Great Valley Parkway, Malvern, PA 19355, USA
Biochem Soc Trans 38:132-6. 2010
..In this paper, we will discuss current platforms that report on E3 ligase activity and can detect E3 inhibitors, and underline the advantages and disadvantages of each approach...
- Strategies for the identification of novel inhibitors of deubiquitinating enzymes
Seth J Goldenberg
Progenra Inc, 271A Great Valley Parkway, Malvern, PA 19355, USA
Biochem Soc Trans 36:828-32. 2008
..In this review, current platforms for detecting DUB inhibitors are discussed and the advantages and disadvantages of the approaches are underlined...
- Detection and characterization of SUMO protease activity using a sensitive enzyme-based reporter assay
Craig A Leach
Progenra Inc, Malvern, PA, USA
Methods Mol Biol 497:269-81. 2009
..The utility of this SUMO-CHOP-Reporter assay platform is demonstrated by its ability to determine K(m) values and to characterize inhibitors of SUMO proteases...
- Novel approach for characterizing ubiquitin E3 ligase function
Jeffrey G Marblestone
Progenra, Inc, Malvern, Pennsylvania, USA
J Biomol Screen 15:1220-8. 2010
..As the number of E3 ligases associated with various disease states increases, the ability to quantitate the activity of these enzymes in an expeditious manner becomes imperative in drug discovery...
- Glaciapyrroles A, B, and C, pyrrolosesquiterpenes from a Streptomyces sp. isolated from an Alaskan marine sediment
Venkat R Macherla
Nereus Pharmaceuticals, Inc, 10480 Wateridge Circle, San Diego, California 92121, USA
J Nat Prod 68:780-3. 2005
..The structures of 1, 2, and 3 were established using spectroscopic methods...
- Structure-activity relationship studies of salinosporamide A (NPI-0052), a novel marine derived proteasome inhibitor
Venkat R Macherla
Nereus Pharmaceuticals, Inc, 10480 Wateridge Circle, San Diego, California 92121, USA
J Med Chem 48:3684-7. 2005
..These findings provide insights into structure-activity relationships within this novel series...
- Aureoverticillactam, a novel 22-atom macrocyclic lactam from the marine actinomycete Streptomyces aureoverticillatus
Scott S Mitchell
Nereus Pharmaceuticals, Inc, 10480 Wateridge Circle, San Diego, California 92121, USA
J Nat Prod 67:1400-2. 2004
..Using extensive MS, UV, and NMR spectral analyses, the structure has been established as compound 1, aureoverticillactam, a 22-atom macrocyclic lactam incorporating both triene and tetraene conjugated olefins...
- A novel orally active proteasome inhibitor induces apoptosis in multiple myeloma cells with mechanisms distinct from Bortezomib
Dharminder Chauhan
The Jerome Lipper Multiple Myeloma Center, Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts 02115, USA
Cancer Cell 8:407-19. 2005
..Combining NPI-0052 and Bortezomib induces synergistic anti-MM activity. Our study therefore provides the rationale for clinical protocols evaluating NPI-0052, alone and together with Bortezomib, to improve patient outcome in MM...
- Lajollamycin, a nitro-tetraene spiro-beta-lactone-gamma-lactam antibiotic from the marine actinomycete Streptomyces nodosus
Rama Rao Manam
Nereus Pharmaceuticals Inc, 10480 Wateridge Circle, San Diego, CA 92121, USA
J Nat Prod 68:240-3. 2005
..Lajollamycin (1) showed antimicrobial activity against both drug-sensitive and -resistant Gram-positive bacteria and inhibited the growth of B16-F10 tumor cells in vitro...
- NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent
Benjamin Nicholson
Nereus Pharmaceuticals, San Diego, California 92121, USA
Anticancer Drugs 17:25-31. 2006
..These data warrant further evaluation of NPI-2358 as a vascular-disrupting agent in vivo. Currently, NPI-2358 is in preclinical development for the treatment of cancer...
