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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1993 1
1994 6
1995 43
1996 97
1997 148
1998 198
1999 253
2000 291
2001 318
2002 354
2003 352
2004 379
2005 361
2006 349
2007 393
2008 343
2009 352
2010 336
2011 338
2012 345
2013 303
2014 266
2015 266
2016 236
2017 166
2018 158
2019 77
2020 1
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6,112 results
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Page 1
Pathways and mechanisms of venetoclax resistance
Bose P, et al. Leuk Lymphoma 2017 - Review. PMID 28140720 Free PMC article.
The approval of venetoclax, a 'BH3-mimetic' antagonist of the BCL-2 anti-apoptotic protein, for chronic lymphocytic leukemia represents a major milestone in translational apoptosis research. ...Finally, the successful clinical development of potent and selective antagonists of BCL-X(L) and MCL-1 is eagerly awaited....
The approval of venetoclax, a 'BH3-mimetic' antagonist of the BCL-2 anti-apoptotic protein, for chronic lymphocytic leukemia r …
BCL-X(L) overexpression promotes tumor progression-associated properties.
Trisciuoglio D, et al. Cell Death Dis 2017. PMID 29238043 Free PMC article.
By using human melanoma and glioblastoma cell lines and their derivative BCL-X(L) overexpressing clones, we investigated the role of BCL-X(L) in aggressive features of these two tumor histotypes. ...BCL-X(L) expression reduction by siRNA, the exposure to a BCL-X(L)-specific inhibitor and the use of a panel of human melanoma cell lines corroborated the evidence that BCL-X(L) regulates tumor progression-associated properties. ...
By using human melanoma and glioblastoma cell lines and their derivative BCL-X(L) overexpressing clones, we investigated the r …
The Structural Biology of Bcl-x(L).
Lee EF and Fairlie WD. Int J Mol Sci 2019 - Review. PMID 31067648 Free PMC article.
Much of our knowledge of the molecular details of these interactions has come from biochemical and structural studies on the pro-survival protein Bcl-x(L). ...Structural studies involving Bcl-x(L) were also the basis for the discovery of the first small-molecule pro-survival protein inhibitors, leading ultimately to the development of a new class of drugs now successfully used for cancer treatment in the clinic. ...
Much of our knowledge of the molecular details of these interactions has come from biochemical and structural studies on the pro-survival …
A selective BCL-X(L) PROTAC degrader achieves safe and potent antitumor activity.
Khan S, et al. Nat Med 2019. PMID 31792461 Free PMC article.
B-cell lymphoma extra large (BCL-X(L)) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-X(L) inhibitors, such as ABT263, as safe and effective anticancer agents. To reduce the toxicity of ABT263, we converted it into DT2216, a BCL-X(L) proteolysis-targeting chimera (PROTAC), that targets BCL-X(L) to the Von Hippel-Lindau (VHL) E3 ligase for degradation. ...
B-cell lymphoma extra large (BCL-X(L)) is a well-validated cancer target. However, the on-target and dose-limiting thrombocyto …
Bcl-x(L) deamidation is regulated by multiple ion transporters and is intramolecularly catalyzed.
Dho SH, et al. Biochim Biophys Acta Mol Cell Res 2018. PMID 29694915 Free article.
The rate of nonenzymatic deamidation of two asparagines in the anti-apoptotic protein Bcl-x(L) is accelerated by this increase in pH. ...The conservation of such histidines implies that human Bcl-x(L) is in essence "designed" to be deamidated, which provides further evidence that deamidation serves as a bona fide regulatory post-translational modification of Bcl-x(L)....
The rate of nonenzymatic deamidation of two asparagines in the anti-apoptotic protein Bcl-x(L) is accelerated by this i …
New agents that target senescent cells: the flavone, fisetin, and the BCL-X(L) inhibitors, A1331852 and A1155463.
Zhu Y, et al. Aging (Albany NY) 2017. PMID 28273655 Free PMC article.
Here we report that fisetin, a naturally-occurring flavone with low toxicity, and A1331852 and A1155463, selective BCL-X(L) inhibitors that may have less hematological toxicity than the less specific BCL-2 family inhibitor navitoclax, are senolytic. ...
Here we report that fisetin, a naturally-occurring flavone with low toxicity, and A1331852 and A1155463, selective BCL-X(L) in …
BH3-Mimetic Drugs: Blazing the Trail for New Cancer Medicines
Merino D, et al. Cancer Cell 2018 - Review. PMID 30537511 Free article.
Pro-survival BCL-2 proteins prevent apoptosis by keeping the cell death effectors, BAX and BAK, in check. The BH3-only proteins initiate apoptosis by neutralizing the pro-survival BCL-2 proteins. ...The BCL-2 inhibitor venetoclax has been approved for treatment of refractory chronic lymphocytic leukemia and this drug and inhibitors of pro-survival MCL-1 and BCL-XL are being tested in diverse malignancies....
Pro-survival BCL-2 proteins prevent apoptosis by keeping the cell death effectors, BAX and BAK, in check. The BH3-only proteins initi …
Structural and functional analyses of hepatitis B virus X protein BH3-like domain and Bcl-xL interaction.
Zhang TY, et al. Nat Commun 2019. PMID 31324803 Free PMC article.
Hepatitis B virus (HBV) X protein, HBx, interacts with anti-apoptotic Bcl-2 and Bcl-xL proteins through its BH3-like motif to promote HBV replication and cytotoxicity. Here we report the crystal structure of HBx BH3-like motif in complex with Bcl-xL where the BH3-like motif adopts a short α-helix to snuggle into a hydrophobic pocket in Bcl-xL via its noncanonical Trp120 residue and conserved Leu123 residue. ...
Hepatitis B virus (HBV) X protein, HBx, interacts with anti-apoptotic Bcl-2 and Bcl-xL proteins through its BH3- …
Mannose impairs tumour growth and enhances chemotherapy
Gonzalez PS, et al. Nature 2018. PMID 30464341 Free article.
As a result, the administration of mannose in combination with conventional chemotherapy affects levels of anti-apoptotic proteins of the Bcl-2 family, leading to sensitization to cell death. ...
As a result, the administration of mannose in combination with conventional chemotherapy affects levels of anti-apoptotic proteins of the …
Homoharringtonine regulates the alternative splicing of Bcl-x and caspase 9 through a protein phosphatase 1-dependent mechanism.
Sun Q, et al. BMC Complement Altern Med 2018. PMID 29788973 Free PMC article.
Calyculin A, an inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), significantly inhibited the effects of HHT on the alternative splicing of Bcl-x and Caspase 9, in contrast to okadaic acid, a specific inhibitor of PP2A. Overexpression of PP1 resulted in a decrease in the ratio of Bcl-xL/xS and an increase in the ratio of Caspase 9a/9b. Moreover, the effects of HHT on Bcl-x and Caspase 9 splicing were enhanced in response to PP1 overexpression. ...
Calyculin A, an inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), significantly inhibited the effect …
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