1173462-16-2Relevant articles and documents
Discovery of Novel Small-Molecule FAK Activators Promoting Mucosal Healing
Basson, Marc D.,Elsayed, Ahmed Adham Raafat,Gallardo-Macias, Ricardo,Golovko, Mikhail Y.,Gurvich, Vadim J.,More, Shyam K.,Oncel, Sema,Rashmi,Wang, Qinggang
supporting information, p. 356 - 364 (2021/03/17)
Gastrointestinal mucosal wounds are common to patients injured by factors as diverse as drugs, inflammatory bowel disease, peptic ulcers, and necrotizing enterocolitis. However, although many drugs are used to ameliorate injurious factors, there is no drug available to actually stimulate mucosal wound healing. Focal adhesion kinase (FAK), a nonreceptor tyrosine kinase, induces epithelial sheet migration and wound healing, making FAK a potential pharmacological target in this regard. In our previous research, we found a lead compound with drug-like properties, ZINC40099027, which promotes FAK phosphorylation, inducing mucosal healing in murine models. Herein we describe the design and optimization of a small library of novel FAK activators based on ZINC40099027 and their applications toward human intestinal epithelial wound closure and mouse ulcer healing.
3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 67, (2009/08/16)
The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
