Chemical optimization of a novel class of USP7 inhibitor for cancer treatment

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: 1R43CA174037-01A1
Agency Tracking Number: R43CA174037
Amount: $224,974.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: NCI
Solicitation Number: PA13-234
Timeline
Solicitation Year: 2014
Award Year: 2014
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
271A GREAT VALLEY PKWY, 271A GREAT VALLEY PKWY, MALVERN, PA, 19355-
DUNS: 190641816
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 JOSEPH WEINSTOCK
 (610) 644-6974
 weinstock@progenra.com
Business Contact
 MICHAEL MATTERN
Phone: (610) 644-6974
Email: mattern@progenra.com
Research Institution
 Stub
Abstract
DESCRIPTION (provided by applicant): Many regulatory proteins are themselves tightly controlled by ubiquitin conjugating and deconjugating enzymes, whose dysfunctional forms are implicated in numerous diseases, including cancers. USP7, a deubiquitylating enzyme, regulates ubiquitylation and, thereby, stability of the E3 ligase HDM2, which in cells effects ubiquitylation and promotes proteasomal degradation of the tumor suppressor p53 as well as a number of other proteins such as FOXO4, PTEN and claspin. Thus, inhibiting USP7 can impact both p53 wild type and mutant tumors. In addition, by de-ubiquitylating and preserving the transcription factor Foxp3, USP7 increases T regulatory cell (Treg) mediated suppression of tumor-infiltrating T effector cells, the latter being associated with improved clinical outcome for many solid tumors, including lung cancers. Thus, USP7 functions to limit immune cell-mediated antitumor defenses. The observation that the accumulation of Foxp3+ Treg cells at the tumor or in d

* Information listed above is at the time of submission. *

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