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news.FORMA Therapeutics and The Netherlands Cancer Institute (NKI) have announced today a collaborative initiative and exclusive license agreement in which FORMA has acquired a unique covalent chemistry platform developed by NKI Chemical Biology Laboratories principal investigator and FORMA’s deubiquitinase (DUB) investigator network member Dr Huib Ovaa.
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Under this collaborative initiative, FORMA and Dr Ovaa will advance the research, discovery and clinical application of highly-selective, irreversible therapeutics. This represents a distinct and additional agreement between FORMA Therapeutics and Dr Ovaa, with the first agreement announced in the area of DUBs on 9 July 2013.
FORMA Therapeutics chief scientific officer and research and development head Dr Kenneth W Bair noted that the company is extremely excited about exploring the therapeutic potential of covalent drug binders with Dr Huib Ovaa’s discovery laboratory.
"The unique reactivity profile of the propargyl moiety will be examined across a broad variety of cysteine-containing proteins, initially to understand the distinctly different microenvironments of proteins and their potential utility in creating breakthrough drugs.
"Dr Ovaa’s laboratory has solved a number of challenging problems at the interface between chemistry, biology and medicine, and we look forward to a productive partnership to create next-generation covalent inhibitors," Dr Bair added.
Cysteine residues play an important role the catalytic action of many enzymes. Such enzymes implicated in a broad range of diseases include various families of proteases such as cathepsins, caspases and deubiquitinating enzymes, but also many phosphatases.