IDENTIFICATION OF POTENT BH3-MIMETIC COMBINATIONS TARGETING PRO-SURVIVAL PATHWAYS IN HUMAN B-CELL ACUTE LYMPHOBLASTIC LEUKEMIA
Sign Up to like & getrecommendations! Published in 2019 at "Experimental Hematology"
DOI: 10.1016/j.exphem.2019.06.411
Abstract: Precursor-B acute lymphoblastic leukemia (B-ALL) is an aggressive hematological malignancy. Relapsed disease has a poor prognosis despite improved outcomes with tyrosine kinase inhibitors (TKIs) and immunotherapeutic approaches such as CAR-T cells. Targeting cell survival with… read more here.
Keywords: bh3 mimetic; acute lymphoblastic; bh3; lymphoblastic leukemia ... See more keywords
What can we learn from mice lacking pro-survival BCL-2 proteins to advance BH3 mimetic drugs for cancer therapy?
Sign Up to like & getrecommendations! Published in 2022 at "Cell death and differentiation"
DOI: 10.1038/s41418-022-00987-0
Abstract: In many human cancers the control of apoptosis is dysregulated, for instance as a result of the overexpression of pro-survival BCL-2 proteins. This promotes tumorigenesis by protecting nascent neoplastic cells from stress and renders malignant… read more here.
Keywords: bh3 mimetic; survival bcl; bcl; bcl proteins ... See more keywords
Targeting Bfl-1 via acute CDK9 inhibition overcomes intrinsic BH3 mimetic resistance in lymphomas.
Sign Up to like & getrecommendations! Published in 2020 at "Blood"
DOI: 10.1182/blood.2020008528
Abstract: BH3 mimetics like Venetoclax target pro-survival Bcl-2 family proteins and are important therapeutics in the treatment of hematological malignancies. We demonstrate endogenous Bfl-1 expression can render preclinical lymphoma tumor models insensitive to Mcl-1 and Bcl-2-inhibitors.… read more here.
Keywords: bfl; bh3; cdk9; targeting bfl ... See more keywords
BCL-XL inhibition by BH3-mimetic drugs induces apoptosis in models of Epstein-Barr virus-associated T/NK-cell lymphoma.
Sign Up to like & getrecommendations! Published in 2020 at "Blood advances"
DOI: 10.1182/bloodadvances.2020002446
Abstract: Epstein-Barr virus (EBV)-associated T- and natural killer (NK)-cell malignancies, such as extranodal NK-/T-cell lymphoma (ENKTL), exhibit high chemoresistance and, accordingly, such patients have a poor prognosis. The rare nature of such cancers and nonmalignant T/NK… read more here.
Keywords: epstein barr; barr virus; cell; bh3 mimetic ... See more keywords
Targeting intermediary metabolism enhances the efficacy of BH3 mimetic therapy in hematologic malignancies
Sign Up to like & getrecommendations! Published in 2018 at "Haematologica"
DOI: 10.3324/haematol.2018.204701
Abstract: BH3 mimetics are novel targeted drugs with remarkable specificity, potency and enormous potential to improve cancer therapy. However, acquired resistance is an emerging problem. We report the rapid development of resistance in chronic lymphocytic leukemia… read more here.
Keywords: efficacy bh3; intermediary metabolism; mimetic therapy; resistance ... See more keywords
Anti-Leukemic Properties of Aplysinopsin Derivative EE-84 Alone and Combined to BH3 Mimetic A-1210477
Sign Up to like & getrecommendations! Published in 2021 at "Marine Drugs"
DOI: 10.3390/md19060285
Abstract: Aplysinopsins are a class of marine indole alkaloids that exhibit a wide range of biological activities. Although both the indole and N-benzyl moieties of aplysinopsins are known to possess antiproliferative activity against cancer cells, their… read more here.
Keywords: anti leukemic; k562 cells; aplysinopsin derivative; properties aplysinopsin ... See more keywords
The carboxyl-terminal sequence of PUMA binds to both anti-apoptotic proteins and membranes
Sign Up to like & getrecommendations! Published in 2023 at "eLife"
DOI: 10.7554/elife.88329
Abstract: Anti-apoptotic proteins such as BCL-XL promote cell survival by sequestering pro-apoptotic BCL-2 family members, an activity that frequently contributes to tumorigenesis. Thus, the development of small-molecule inhibitors for anti-apoptotic proteins, termed BH3-mimetics, is revolutionizing how… read more here.
Keywords: puma; bh3 mimetic; carboxyl terminal; anti apoptotic ... See more keywords