منابع مشابه
Mitochondrial apoptosis and BH3 mimetics
The BCL2-selective BH3 mimetic venetoclax was recently approved for the treatment of relapsed, chromosome 17p-deleted chronic lymphocytic leukemia (CLL) and is undergoing extensive testing, alone and in combination, in lymphomas, acute leukemias, and solid tumors. Here we summarize recent advances in understanding of the biology of BCL2 family members that shed light on the action of BH3 mimeti...
متن کاملIntegrity of the CBL gene in mature B-cell malignancies.
Identification of biomarkers for response to novel therapeutic agents is an essential step for the success of tailored treatments in cancer. Preliminary data from clinical trials indicate that inhibitors of the spleen tyrosine kinase (SYK) may be efficacious in subsets of diffuse large B-cell lymphomas (DLBCL) and chronic lymphocytic leukemias (CLL).1 SYK is a component of the signaling cascade...
متن کاملTargeting BCL2 With BH3 Mimetics: Basic Science and Clinical Application of Venetoclax in Chronic Lymphocytic Leukemia and Related B Cell Malignancies
The intracellular protein B-cell-lymphoma-2 (BCL2) has been considered an attractive target for cancer therapy since the discovery of its function as a major promoter of cell survival (an anti-apoptotic) in the late 1980s. However, the challenges of targeting a protein-protein interaction delayed the discovery of fit-for-purpose molecules until the mid-2000s. Since then, a series of high affini...
متن کاملDefining specificity and on-target activity of BH3-mimetics using engineered B-ALL cell lines
One of the hallmarks of cancer is a resistance to the induction of programmed cell death that is mediated by selection of cells with elevated expression of anti-apoptotic members of the BCL-2 family. To counter this resistance, new therapeutic agents known as BH3-mimetic small molecules are in development with the goal of antagonizing the function of anti-apoptotic molecules and promoting the i...
متن کاملOn BH3 Mimetics and Ca2+ Signaling
Preclinical Research BH3 mimetics are anticancer agents that reproduce the spatial arrangement of the BH3 domain of Bcl-2 family proteins. Just like the BH3-only proteins, these compounds bind to the hydrophobic cleft of the pro-survival Bcl-2 members such as Bcl-2 or Bcl-xL, and disrupt their heterodimerization with pro-apoptotic Bax or Bak, sensitizing cells to chemotherapy. In recent years, ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Cells
سال: 2020
ISSN: 2073-4409
DOI: 10.3390/cells9030717