Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model.
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DOI: 10.1021/acs.jmedchem.1c01006
Abstract: Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven… read more here.
Keywords: selective csf1r; murine colon; csf1r; orally active ... See more keywords
Active and Selective Ensembles in Oxide-Derived Copper Catalysts for CO2 Reduction
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DOI: 10.1021/acsenergylett.0c01777
Abstract: Copper catalysts are unique in CO2 reduction as they allow the formation of C2+ products. Depending on the catalysts’ synthesis, product distribution varies significantly: while Cu nanoparticles pr... read more here.
Keywords: co2 reduction; selective ensembles; copper catalysts; active selective ... See more keywords
Discovery of 3-Quinazolin-4(3H)-on-3-yl-2,N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors.
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DOI: 10.1021/acsmedchemlett.0c00239
Abstract: Phosphoinositide 3-kinases (PI3Ks) mediate a series of events related to cell growth, proliferation, survival, and differentiation. Overexpression of PI3Ks can lead to the dysregulation of cell homeostasis and cause tumorigenesis. In this study, rationally designed… read more here.
Keywords: pi3k; discovery quinazolin; orally active; active selective ... See more keywords