Cell active and functionally-relevant small-molecule agonists of calcitonin receptor.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103596
Abstract: The natural calcitonin (CT) receptor and its peptide agonists are considered validated targets for drug discovery. A small molecule agonist, SUN-B8155, has previously been shown to efficiently activate cellular CTR. Herein, we report the synthesis… read more here.
Keywords: receptor; small molecule; cell active; calcitonin receptor ... See more keywords
Discovery of an Irreversible and Cell-Active BCL6 Inhibitor Selectively Targeting Cys53 Located at the Protein-Protein Interaction Interface.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b00732
Abstract: B-cell lymphoma 6 (BCL6) is the most frequently involved oncogene in diffuse large B-cell lymphomas (DLBCLs). BCL6 shows potent transcriptional repressor activity through interactions with its corepressors, such as BCL6 corepressor (BCOR). The inhibition of… read more here.
Keywords: protein; inhibitor; inhibition; bcl6 ... See more keywords
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00864
Abstract: PBRM1 is a subunit of the PBAF chromatin remodeling complex that uniquely contains six bromodomains. PBRM1 can operate as a tumor suppressor or tumor promoter. PBRM1 is a tumor promoter in prostate cancer, contributing to… read more here.
Keywords: pbrm1 bromodomain; cell active; selective cell; pbrm1 ... See more keywords
Repurposing the Kinase Inhibitor Mavelertinib for Giardiasis Therapy
Sign Up to like & getrecommendations! Published in 2022 at "Antimicrobial Agents and Chemotherapy"
DOI: 10.1128/aac.00017-22
Abstract: A phenotypic screen of the ReFRAME compound library was performed to identify cell-active inhibitors that could be developed as therapeutics for giardiasis. A primary screen against Giardia lamblia GS clone H7 identified 85 cell-active compounds… read more here.
Keywords: kinase inhibitor; cell active; kinase; screen ... See more keywords
A facile consensus ranking approach enhances virtual screening robustness and identifies a cell-active DYRK1α inhibitor.
Sign Up to like & getrecommendations! Published in 2018 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2018-0198
Abstract: BACKGROUND Virtual screening is vital for contemporary drug discovery but striking performance fluctuations are commonly encountered, thus hampering error-free use. Results and Methodology: A conceptual framework is suggested for combining screening algorithms characterized by orthogonality… read more here.
Keywords: virtual screening; active dyrk1; consensus ranking; consensus ... See more keywords