| CLINICAL STUDY | It showed strong potency in an in vitro assay & significant bone resorption inhibition (antiosteoporosis activity) in an in vivo animal model of the disease |
| STATUS | In development |
| TECHNOLOGY |
In a combinatorial study involving protein-protein interaction, the author found a novel series of SH2 binders with anti-osteo porosis activity by using a strategy that combined structure- based design with combinatorial synthesis SH2 domains are protein units that mediate intracellular protein-protein interactions in signal transduction pathways & the SH2 domain of Src protein is a potential antiosteoporosis target. The author et al used solid-phase paralell synthesis to generate a series of libraries whose compds were based in part on a nonpeptide that has been shown to bind Src SH2 with high affinity. They screened the libraries for SH2 binding activity, identified some good prospects, & used rational drug design methods to create analogs One of these was designed to mimic the mechanism of SH2 binding activity observed in a crystal structure of Src SH2 that is bound to citrate. |
| UPDATE | 05.00 |
| AUTHOR | This data is not available for free |
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