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Description: Smurf1-IN-A01 is a novel, potent, high affinity and selective inhibitor of E3 ubiquitin-protein ligase Smurf1 (Smad ubiquitination regulatory factor-1) with Kd value of 3.7 nM. It disturbs Smurf1-Smad1/5 interaction and blocks Smurf1 mediated Smad1/5 ubiquitination. Smurf1-IN-A01 increases responsiveness to BMP-2 in myoblasts and osteoblasts. The ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) negatively regulates bone morphogenetic protein (BMP) pathway by ubiquitinating certain signal components for degradation. Thus, it can be an eligible pharmacological target for increasing BMP signal responsiveness.
References: Sci Rep. 2014 May 14; 4:4965.
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