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Drug discoveryExploring the kinome to unlock new possibilitiesWith our sights set on discovery, Aclaris is currently exploring the kinome, a subset of the human genome that consists of a collection of approximately 518 protein kinases, one of the largest of all human gene families, and a key control point in cell behavior. Classified into eight major groups based on their structural similarity to each other, kinases are key regulators of cell function for many cell processes. By transferring phosphates to other molecules, kinases can induce a cellular response to environmental cues. Dysregulation and/or mutations in kinases can disrupt normal cell signaling and lead to diseases ranging from diabetes to cancer, making them important targets for drug development.
Currently, there are a number of approved kinase inhibitors on the market, such as Xeljanz® (tofacitinib citrate), Gleevec® (imatinib mesylate), and Tarceva® (erlotinib). However, these drugs only target a small fraction of the kinome, with many clinically relevant kinases lacking validated inhibitors.
Were focused on the design and development of kinase inhibitors that target key enzymes involved in chronic inflammation, autoimmune disease, or the regulation of cancer growth, survival and metastasis.
https://www.aclaristx.com/drugdiscovery/
Kinase inhibitors in focus after Merck bid for ArQuleDec. 9, 2019 10:40 AM ET|About: Pfizer Inc. (PFE)|By: Douglas W. House, SA News Editor Merck's $2.7B bid for ArQule is yet another example of Big Biopharma's high regard for oral kinase inhibitors for treating cancer. ArQule's lead drug is ARQ 531, an oral inhibitor of Bruton's tyrosine kinase (BTK).
https://seekingalpha.com/news/3524810-kinase-inhibitors-in-focus-after-merck-bid-for-arqule
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