Mission Therapeutics Ltd Presents At The Annual Meeting Of AACR The Identification Of Novel Inhibitors Of The UCHL1 Oncogene
Poster exemplifies amenability of wider target family to development of drug-like molecules
Philadelphia, PA, US and Cambridge UK, 20 April 2015 – MISSION Therapeutics, a company focused on the discovery and development of modulators of the deubiquitylating (DUB) enzyme family for the treatment of cancer and other diseases, today presents a poster at AACR entitled “Discovery of highly selective UCHL1 inhibitors with in vivo pre-clinical anti-tumour activity”.
UCHL1 is a prototypical oncogene that selectively drives proliferation in many tumour types including multiple myeloma and lung cancer. UCHL1 depletion leads to the selective killing of a number of tumours whose proliferation is driven by UCHL1. Validation of DUB targets like UCHL1 exemplifies the rationale for developing inhibitors of the ubiquitin pathways to target a broad range of cancers with defined genetic abnormalities, or resistance to standard-of-care modalities.
Using its integrated drug discovery platform combining unique biochemical, cellular, biophysical and structural assays, MISSION has identified and optimised potent and selective small molecule, active site inhibitors of UCHL1. These inhibitors recapitulate UCHL1 target biology and exhibit in vitro target engagement in proprietary cellular assays. Further lead optimisation has generated compounds with drug-like properties that demonstrate efficacy in disease models. Cumulatively, the data support not only the potential further pre-clinical development of UCHL1 compounds but also the tractability of a broader range of DUBs to pharmacologic intervention, with the potential to reach a diversity of cancers comprising different genetic signatures.
Xavier Jacq, Vice President Biology at MISSION, commented: “We are delighted to share our recent progress in the development of first-in-class selective UCHL1 inhibitors targeting difficult to treat cancers. The advances presented, underpin MISSION’s ability to identify small molecule leads of a hitherto difficult enzyme class. Surmounting the key challenges of targeting DUBs, we have paved the way for the timely development of inhibitors of several DUBs and the generation of a wholly new structural class of anti-cancer agents."
Notes To Editors
About MISSION Therapeutics
Founded in 2011, MISSION Therapeutics builds on the research of Professor Steve Jackson FRS, who holds the Frederick James Quick Chair of Biology at the University of Cambridge, by exploiting the new and extensive research emerging on the ubiquitin pathways that control cellular responses to DNA damage.
MISSION has established a broad platform of technologies for the discovery and preclinical development of first-in-class modulators of ubiquitin pathway enzymes involved in cancer and other diseases. The Company is developing drugs to inhibit the proliferation of tumour cells, exploiting certain properties of specific DUBs, such as their oncogene status or association with synthetic lethality, the latter now a clinically-proven mechanism for selectively killing tumour cells.
The Company has received £27 million in venture capital from a blue chip syndicate comprising institutional and corporate investors (Sofinnova Partners, Imperial Innovations, SR One, Roche Venture Fund and Pfizer Venture Investments) and is based at the Babraham Research Campus, south of Cambridge.
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Philadelphia, PA, US and Cambridge UK, 20 April 2015 – MISSION Therapeutics, a company focused on the discovery and development of modulators of the deubiquitylating (DUB) enzyme family for the treatment of cancer and other diseases, today presents a poster at AACR entitled “Discovery of highly selective UCHL1 inhibitors with in vivo pre-clinical anti-tumour activity”.
UCHL1 is a prototypical oncogene that selectively drives proliferation in many tumour types including multiple myeloma and lung cancer. UCHL1 depletion leads to the selective killing of a number of tumours whose proliferation is driven by UCHL1. Validation of DUB targets like UCHL1 exemplifies the rationale for developing inhibitors of the ubiquitin pathways to target a broad range of cancers with defined genetic abnormalities, or resistance to standard-of-care modalities.
Using its integrated drug discovery platform combining unique biochemical, cellular, biophysical and structural assays, MISSION has identified and optimised potent and selective small molecule, active site inhibitors of UCHL1. These inhibitors recapitulate UCHL1 target biology and exhibit in vitro target engagement in proprietary cellular assays. Further lead optimisation has generated compounds with drug-like properties that demonstrate efficacy in disease models. Cumulatively, the data support not only the potential further pre-clinical development of UCHL1 compounds but also the tractability of a broader range of DUBs to pharmacologic intervention, with the potential to reach a diversity of cancers comprising different genetic signatures.
Xavier Jacq, Vice President Biology at MISSION, commented: “We are delighted to share our recent progress in the development of first-in-class selective UCHL1 inhibitors targeting difficult to treat cancers. The advances presented, underpin MISSION’s ability to identify small molecule leads of a hitherto difficult enzyme class. Surmounting the key challenges of targeting DUBs, we have paved the way for the timely development of inhibitors of several DUBs and the generation of a wholly new structural class of anti-cancer agents."
Notes To Editors
About MISSION Therapeutics
Founded in 2011, MISSION Therapeutics builds on the research of Professor Steve Jackson FRS, who holds the Frederick James Quick Chair of Biology at the University of Cambridge, by exploiting the new and extensive research emerging on the ubiquitin pathways that control cellular responses to DNA damage.
MISSION has established a broad platform of technologies for the discovery and preclinical development of first-in-class modulators of ubiquitin pathway enzymes involved in cancer and other diseases. The Company is developing drugs to inhibit the proliferation of tumour cells, exploiting certain properties of specific DUBs, such as their oncogene status or association with synthetic lethality, the latter now a clinically-proven mechanism for selectively killing tumour cells.
The Company has received £27 million in venture capital from a blue chip syndicate comprising institutional and corporate investors (Sofinnova Partners, Imperial Innovations, SR One, Roche Venture Fund and Pfizer Venture Investments) and is based at the Babraham Research Campus, south of Cambridge.
Help employers find you! Check out all the jobs and post your resume.