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Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
Shukla MR, Patra S, Verma M, Sadasivam G, Jana N, Mahangare SJ, Vidhate P, Lagad D, Tarage A, Cheemala M, Kulkarni C, Bhagwat S, Chaudhari VD, Sayyed M, Pachpute V, Phadtare R, Gole G, Phukan S, Sunkara B, Samant C, Shingare M, Naik A, Trivedi S, Marisetti AK, Reddy M, Gholve M, Mahajan N, Sabde S, Patil V, Modi D, Mehta M, Nigade P, Tamane K, Tota S, Goyal H, Volam H, Pawar S, Ahirrao P, Dinchhana L, Mallurwar S, Akarte A, Bokare A, Kanhere R, Reddy N, Koul S, Dandekar M, Singh M, Bernstein PR, Narasimham L, Bhonde M, Gundu J, Goel R, Kulkarni S, Sharma S, Kamboj RK, Palle VP. Shukla MR, et al. Among authors: shingare m. J Med Chem. 2020 Dec 10;63(23):14700-14723. doi: 10.1021/acs.jmedchem.0c01264. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33297683
Dual PI3Kδγ inhibition demonstrates potent anticancer effects in diffuse large B-cell lymphoma models: Discovery and preclinical characterization of LL-00084282.
Verma MK, Samant C, Kale R, Patra S, Mahajan N, Gholve MK, Marisetti A, Sunkara B, Naik A, Shingare M, Reddy M, Bokare AM, Akarte A, Koul S, Nigade PB, Patil VB, Modi D, Ahirrao P, Pawar S, Kuldharan S, Dinchhana L, Mehta M, Gundu J, Jana N, Vidhate P, Mahangare SJ, Shukla MR, Goel RN, Bhonde M, Kamboj RK, Palle VP. Verma MK, et al. Among authors: shingare m. Biochem Biophys Res Commun. 2022 Dec 31;637:267-275. doi: 10.1016/j.bbrc.2022.11.038. Epub 2022 Nov 15. Biochem Biophys Res Commun. 2022. PMID: 36410276
HDAC activity is dispensable for repression of cell-cycle genes by DREAM and E2F:RB complexes.
Barrett A, Shingare MR, Rechtsteiner A, Wijeratne TU, Rodriguez KM, Rubin SM, Müller GA. Barrett A, et al. Among authors: shingare mr. bioRxiv [Preprint]. 2023 Oct 28:2023.10.28.564489. doi: 10.1101/2023.10.28.564489. bioRxiv. 2023. Update in: Nat Commun. 2024 May 24;15(1):4450. doi: 10.1038/s41467-024-48724-0. PMID: 37961464 Free PMC article. Updated. Preprint.
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