Understanding the Species Selectivity of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.8b00626
Abstract: To test for on target toxicity of a new chemical entity, it is important to have comparable binding affinities of the compound in the target proteins from humans and the test species. To evaluate our… read more here.
Keywords: mcl; affinity; mcl inhibitors; myeloid cell ... See more keywords
Structure-Based Optimization of 3-Phenyl-N-(2-(3-phenylureido)ethyl)thiophene-2-sulfonamide Derivatives as Selective Mcl-1 Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00690
Abstract: Selective Mcl-1 inhibitors may overcome the drug resistance caused by current anti-apoptotic Bcl-2 protein inhibitors in tumors with Mcl-1 overexpression. Based on previously discovered compounds with a 3-phenylthiophene-2-sulfonamide core moiety, in this work, we have… read more here.
Keywords: optimization phenyl; mcl inhibitors; selective mcl; based optimization ... See more keywords
BAX-BAK heterodimer as a pharmacodynamic biomarker of on-target drug action of Mcl-1 inhibitors to evaluate in-vivo effectiveness.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2018.36.15_suppl.2582
Abstract: 2582Background: Clinical development of promising small molecule Mcl-1 inhibitors is underway. The Mcl-1 inhibitors act by disrupting complexes of Mcl-1 with pro-apoptotic proteins such as BAK/BIM/... read more here.
Keywords: mcl; pharmacodynamic biomarker; mcl inhibitors; bak heterodimer ... See more keywords
Recent Advances in Cancer Drug Development: Targeting Induced Myeloid Cell Leukemia-1 (Mcl-1) Differentiation Protein.
Sign Up to like & getrecommendations! Published in 2017 at "Current medicinal chemistry"
DOI: 10.2174/0929867324666170912092659
Abstract: BACKGROUND Anti-apoptotic members of the Bcl-2 family of proteins are upregulated in a majority of cancers and are potential therapeutic targets. Fragment-based design led to the development of clinical candidates that target Bcl-xL/Bcl-2. Although these… read more here.
Keywords: mcl; mcl inhibitors; cancer drug; development ... See more keywords