Science
Myofibroblasts
◆ Myofibroblasts, a differentiated cell type expressing α-smooth muscle actin (α-SMA), are essential for wound healing and tissue repair following insult (viral, environmental, drug, etc.);
◆ Myofibroblasts can be derived from resting fibroblasts and other precursor cells, such as epithelial cells, endothelial cells, and mononuclear cells;
◆ Aberrant regulation of myofibroblast activation (dysregulated repair), leading to excessive production of ECM, contributes to a number of pathologies, such as organ fibrotic processes and tumor invasiveness
Key steps in tissue fibrogenesis
★ Targeting key molecular targets/signaling pathways central for myofibroblast activation leads to innovative therapies with the potential to slow down, stop and/or reverse fibrogenic process
Integrated discovery engine
◆ High resolution of inhibitor-bound protein complexes affords precise analysis of binding modes and chemical spaces;
◆ In-depth analysis of inter-molecular interactions expands horizons for SAR exploration and IP creation;
◆ Design and virtual screening of compounds from different chemotypes allows alignment of key pharmacophores;
◆ Target-based evaluation along with off-target counter screens enhances drug-like property optimization;
◆ Iteration of target selectivity and potency results in treatment-changing medicines with superior safety and efficacy
