Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor
Sign Up to like & getrecommendations! Published in 2020 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.9b00568
Abstract: Herein we describe the discovery of A-1331852, a first-in-class orally active BCL-XL inhibitor that selectively and potently induces apoptosis in BCL-XL-dependent tumor cells. This molecule was generated by re-engineering our previously reported BCL-XL inhibitor A-1155463… read more here.
Keywords: bcl inhibitor; discovery 1331852; 1331852 first; bcl ... See more keywords
Abstract 1621: L105, a next generation of Bcl-2 inhibitor, overcomes Bcl-2 mutation and exhibits superior antitumor activity
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1621
Abstract: Background: The Bcl-2 inhibitor venetoclax is approved for the treatment of chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL) and acute myeloid leukemia (AML). However, disease progression occurs when Ventoclax long-term treatment as a single… read more here.
Keywords: l105; bcl inhibitor; venetoclax; next generation ... See more keywords
Abstract 1631: Combination of olverembatinib (HQP1351) with BCL-2 inhibitor lisaftoclax (APG-2575) overcomes resistance in gastrointestinal stromal tumors (GISTs)
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DOI: 10.1158/1538-7445.am2023-1631
Abstract: GISTs are common malignant mesenchymal tumors that occur in the GI tract, with an estimated incidence rate of 1% to 2%. About 75% to 80% of patients with GIST have mutations in the KIT gene,… read more here.
Keywords: gist; lisaftoclax; inhibitor lisaftoclax; bcl inhibitor ... See more keywords
Rapid Complete Response to Single-Agent Bcl-2 Inhibitor Venetoclax in a Heart-Transplanted Patient with Triple Refractory Immunoglobulin Light-Chain Amyloidosis
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DOI: 10.1159/000504355
Abstract: Immunoglobulin light-chain amyloidosis (AL) is a disease with limited treatment options due to the frailty of patients caused by organ damage. Since the clonal plasma cells often contain the cytogenetic aberration t(11;14), the Bcl-2 inhibitor… read more here.
Keywords: inhibitor venetoclax; chain amyloidosis; bcl inhibitor; immunoglobulin light ... See more keywords