Enzymes are widely studied as drug targets, and enzyme modulators are therapeutic options for various diseases. Up to 29% of drug targets are reportedly enzymes belonging to various classes. The most popular enzyme targets include kinases, proteases, and phosphatases. Enzymes have historically been considered attractive targets for therapeutics because of their specificity and druggability primarily due to the presence of a binding pocket and catalytic site. About 250 genes coding for enzymes have been identified as FDA-approved drug targets, further highlighting the continued importance of investigating enzyme targets. Enzymes have been identified as disease drivers across various disease areas, including cancer, neurological disease, autoimmune diseases, cardiovascular disease, and metabolic disorders. Enzyme replacement therapies are currently used in metabolic diseases where the deficiency of a specific enzyme is the primary cause.

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The cross-functional discovery teams at Charles River work with a wide range of enzyme targets, including kinases, phosphatases, extra- and intra-cellular proteases, histone, and DNA-modifying enzymes, including gyrases and phosphodiesterases.

  • Selection and Early Clinical Evaluation of the Brain-penetrant 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor UE2343 (Xanamem™)​. British Journal of Pharmacology. 2017, 174(5): 396-408. Full Text​.
  • Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate. Journal of Medicinal Chemistry. 2016, 59(20), 9457-9472. Abstract.
  • Discovery of a Non-Covalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. Journal of Medicinal Chemistry. 2016, 59(19), 9080-9093. Abstract.
  • Neutrophil Maturation Rate Determines the Impact of Dipeptidyl Peptidase 1 Inhibition on Neutrophil Serine Protease Activity. British Journal of Pharmacology. 2016, 173(15): 2390-401. Abstract.
  • Application of Virtual Screening to the Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Potential for the Treatment of Cancer and Axonopathies. BioOrg. Med. Chem. Lett. 2016, 26, 2920-2926. Abstract.
  • Phosphoproteomic Profiling of Tumor Tissues Identifies HSP27 Ser82 Phosphorylation as a Robust Marker of Early Ischemia. Scientific Reports. 2015, 13660. Full Text.

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