Identification of natural allosteric inhibitor for Akt1 protein through computational approaches and in vitro evaluation.
Sign Up to like & getrecommendations! Published in 2017 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2016.12.025
Abstract: Akt, a serine/threonine protein kinase, is often hyper activated in breast and prostate cancers, but with poor prognosis. Allosteric inhibitors regulate aberrant kinase activity by stabilizing the protein in inactive conformation. Several natural compounds have… read more here.
Keywords: allosteric inhibitor; inactive conformation; natural allosteric; inhibitor akt1 ... See more keywords
Structure of an inactive conformation of GTP-bound RhoA GTPase.
Sign Up to like & getrecommendations! Published in 2021 at "Structure"
DOI: 10.1016/j.str.2020.12.015
Abstract: By using 31P NMR, we present evidence that the Rho family GTPase RhoA, similar to Ras GTPases, exists in an equilibrium of conformations when bound to GTP. High-resolution crystal structures of RhoA bound to the… read more here.
Keywords: bound rhoa; gtp bound; gtp; inactive conformation ... See more keywords
Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro
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DOI: 10.1038/s41467-025-59432-8
Abstract: The essential role of RIPK3 in necroptosis makes its inhibition a promising therapeutic strategy. However, the development of RIPK3 inhibitors has been hampered by on-target apoptosis and limited kinase selectivity. Inspired by the R69H mutation,… read more here.
Keywords: inactive conformation; target apoptosis; target; ripk3 ... See more keywords