FKBP12 ligands such as FK506 have been shown to activate the BMP signaling pathway and facilitate tissue regeneration. However, the immunosuppressive activity of FK506 limits its clinical application. Using Heck reaction, we generated nonimmunosuppressive
Wang, Yuefan,Peiffer, Brandon J.,Su, Qi,Liu, Jun O.
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF
The present invention provides a new class of non-immunosupressive FK506 analogs which are FKBP-selective, small-molecule BMP agonists with modest potency therepeutics for tissue repair and regeneration. Also disclosed herein are methods for making and use of these compounds.
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Paragraph 0099; 0194; 0195
(2020/08/13)
Synthesis of orthogonally reactive FK506 derivatives via olefin cross metathesis
Chemical inducers of dimerization (CIDs) are employed in a wide range of biological applications to control protein localization, modulate protein-protein interactions and improve drug lifetimes. These bifunctional chemical probes are assembled from two s
Marinec, Paul S.,Evans, Christopher G.,Gibbons, Garrett S.,Tarnowski, Malloree A.,Overbeek, Daniel L.,Gestwicki, Jason E.
experimental part
p. 5763 - 5768
(2009/12/09)
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