Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma.
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DOI: 10.1021/acs.jmedchem.2c00324
Abstract: Bruton's tyrosine kinase proteolysis-targeting chimeras (BTK-PROTACs) have emerged as a promising approach to address the limitations of BTK inhibitors. However, conducting the rational discovery of orally bioavailable BTK-PROTACs presents significant challenges. In this study, dimensionality… read more here.
Keywords: btk protacs; discovery orally; bruton tyrosine; orally bioavailable ... See more keywords
Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00552
Abstract: PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification. To… read more here.
Keywords: pkmyt1 inhibitor; pkmyt1; discovery orally; orally bioavailable ... See more keywords
Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.
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DOI: 10.1021/acsmedchemlett.7b00116
Abstract: We have discovered a novel series of tetrahydrobenzimidazoles 3 as TGR5 agonists. Initial structure-activity relationship studies with an assay that measured cAMP levels in murine enteroendocrine cells (STC-1 cells) led to the discovery of potent… read more here.
Keywords: tetrahydrobenzimidazoles tgr5; agonists type; efficacious tetrahydrobenzimidazoles; discovery orally ... See more keywords
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
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DOI: 10.1021/acsmedchemlett.8b00220
Abstract: The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were identified… read more here.
Keywords: 8353 discovery; dual mechanism; oncology; discovery orally ... See more keywords