Discovery and development of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as Bcl-2/Mcl-1 inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.102938
Abstract: Bcl-2 family proteins play a vital role for cancer cell in escaping apoptosis, and small-molecule anti-apoptotic Bcl-2 protein inhibitors have been developed as new anticancer therapies. In current study, a series of substituted 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid… read more here.
Keywords: bcl protein; carboxylic acid; tetrahydroisoquinoline carboxylic; acid derivatives ... See more keywords
Abstract 1921: The sensitivity of ovarian cancer cells to the HDAC inhibitor belinostat is improved by inhibiting Bcl-xL or Mcl-1 anti-apoptotic proteins
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1921
Abstract: The identification of novel therapeutic strategies is an important urgent requirement for the clinical management of ovarian cancers, which remain the leading cause of death from gynecologic cancer. Our previous studies have shown that the… read more here.
Keywords: cancer; ovarian cancer; bcl mcl; cancer cells ... See more keywords
Individualized Mitochondrial Functional Approach to Combination of BCL-2 and MCL-1 Antagonism in Acute Myeloid Leukemia
Sign Up to like & getrecommendations! Published in 2019 at "Blood"
DOI: 10.1182/blood-2019-131101
Abstract: BCL-2 antagonist venetoclax combined with hypomethylating agents or low-dose cytarabine is a new standard of care for treatment-naive elderly or unfit AML patients. Despite the striking overall response of 70%, only 30% achieved MRD negative… read more here.
Keywords: combination; venetoclax; bh3 profiling; research funding ... See more keywords
Potential mechanisms of resistance to venetoclax and strategies to circumvent it
Sign Up to like & getrecommendations! Published in 2017 at "BMC Cancer"
DOI: 10.1186/s12885-017-3383-5
Abstract: BackgroundVenetoclax (ABT-199), a first-in-class orally bioavailable BCL-2-selective inhibitor, was recently approved by the FDA for use in patients with 17p-deleted chronic lymphocytic leukemia who have received prior therapy. It is also being evaluated in numerous… read more here.
Keywords: venetoclax; mechanisms resistance; potential mechanisms; resistance ... See more keywords
Evaluation of combined BCL-2/MCL-1 inhibition as a therapeutic approach for synovial sarcoma.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2020.38.15_suppl.e23561
Abstract: e23561Background: While Synovial Sarcoma (SS) only accounts for about 10% of soft tissue sarcomas (STS), or ~10,000 cases/year, ~4,000 of these will be fatal. Little benefit has been seen with newe... read more here.
Keywords: sarcoma; evaluation combined; mcl inhibition; combined bcl ... See more keywords
Genetic biomarkers predict response to dual BCL-2 and MCL-1 targeting in acute myeloid leukaemia cells
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.18632/oncotarget.26540
Abstract: Acute myeloid leukaemia (AML) cells often up-regulate pro-survival members of the BCL-2 protein family, such as BCL-2 and MCL-1, to avoid apoptosis. Venetoclax (ABT-199) targets BCL-2 and has shown promising efficacy in AML but over-expression… read more here.
Keywords: mcl; mcl targeting; response; leukaemia ... See more keywords