Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112186
Abstract: Anti-apoptotic protein BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance, rendering it an attractive target for cancer treatment. However, BCL-XL inhibitors such as ABT-263 cannot be safely used in the clinic because… read more here.
Keywords: abt 263; protac; bcl degraders; target ... See more keywords
ABT-263 induces G1/G0-phase arrest, apoptosis and autophagy in human esophageal cancer cells in vitro.
Sign Up to like & getrecommendations! Published in 2017 at "Acta pharmacologica Sinica"
DOI: 10.1038/aps.2017.78
Abstract: Both the anti- and pro-apoptotic members of the Bcl-2 family are regulated by a conserved Bcl-2 homology (BH3) domain. ABT-263 (Navitoclax), a novel BH3 mimetic and orally bioavailable Bcl-2 family inhibitor with high affinity for… read more here.
Keywords: esophageal cancer; abt 263; human esophageal; cancer cells ... See more keywords
Navitoclax (ABT-263) rejuvenates human skin by eliminating senescent dermal fibroblasts in a mouse/human chimeric model.
Sign Up to like & getrecommendations! Published in 2022 at "Rejuvenation research"
DOI: 10.1089/rej.2022.0048
Abstract: Chronic senescence, such as aging, contributes to age-related tissue dysfunction and disease development. The accumulation of senescent fibroblasts and the senescence-associated secretory phenotype are particularly implicated in this process. Removal of senescent cells has been… read more here.
Keywords: dermal fibroblasts; abt 263; skin; human skin ... See more keywords
Modulation of Navitoclax Sensitivity by Dihydroartemisinin-Mediated MCL-1 Repression in BCR-ABL+ B-Lineage Acute Lymphoblastic Leukemia
Sign Up to like & getrecommendations! Published in 2017 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-17-1231
Abstract: Purpose: BCR-ABL+ B-ALL leukemic cells are highly dependent on the expression of endogenous antiapoptotic MCL-1 to promote viability and are resistant to BH3-mimetic agents such as navitoclax (ABT-263) that target BCL-2, BCL-XL, and BCL-W. However,… read more here.
Keywords: mcl; leukemic cells; abt 263; bcr abl ... See more keywords
NOTCH1 Represses MCL-1 Levels in GSI-resistant T-ALL, Making them Susceptible to ABT-263
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-18-0867
Abstract: Purpose: Effective targeted therapies are lacking for refractory and relapsed T-cell acute lymphoblastic leukemia (T-ALL). Suppression of the NOTCH pathway using gamma-secretase inhibitors (GSI) is toxic and clinically not effective. The goal of this study… read more here.
Keywords: abt 263; mcl levels; represses mcl; notch1 represses ... See more keywords
Abstract 2518: Heterogeneity of cytokine secretion in single senescent fibroblasts is impacted by ONC201 and ABT-263
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-2518
Abstract: Cellular senescence and the associated secretory phenotype (SASP) promote cancer. During the process of aging, cellular and molecular changes that occur in non-cancerous cells can alter responses to cancer therapy and immune response in the… read more here.
Keywords: abt 263; senescent; senescent fibroblasts; cancer ... See more keywords
Abstract 5840: Normal fibroblasts, cancer-associated fibroblasts, and their senescent counterparts exert varying effects on tumorigenic potential and ABT-263 sensitivity of gastric cancer cells
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-5840
Abstract: It has become increasingly apparent that cancer is not a tumor cell-centric disease. Elements of the tumor microenvironment (TME), including fibroblasts and senescent cells, have been shown to contribute to tumor cell proliferation, metastasis, and… read more here.
Keywords: abt 263; sensitivity; ags cells; fibroblasts senescent ... See more keywords
Inhibition of antiapoptotic BCL-2 proteins with ABT-263 induces fibroblast apoptosis, reversing persistent pulmonary fibrosis
Sign Up to like & getrecommendations! Published in 2023 at "JCI Insight"
DOI: 10.1172/jci.insight.163762
Abstract: Patients with progressive fibrosing interstitial lung diseases (PF-ILDs) carry a poor prognosis and have limited therapeutic options. A hallmark feature is fibroblast resistance to apoptosis, leading to their persistence, accumulation, and excessive deposition of extracellular… read more here.
Keywords: antiapoptotic bcl; abt 263; apoptosis; inhibition antiapoptotic ... See more keywords
Hydroxychloroquine Promotes Bcl-xL Inhibition-induced Apoptosis in BxPC-3 Human Pancreatic Cancer Cells
Sign Up to like & getrecommendations! Published in 2022 at "AntiCancer Research"
DOI: 10.21873/anticanres.15836
Abstract: Background/Aim: Anti-apoptotic proteins, including Bcl-2 and Bcl-xL, hinder cancer treatment, and several drugs targeting these molecules have been developed. One is ABT-263 (navitoclax), which targets Bcl-2, Bcl-xL, and Bcl-w. On the other hand, hydroxychloroquine (HCQ)… read more here.
Keywords: abt 263; bxpc; hcq abt; hcq ... See more keywords
Taking Advantage of the Senescence-Promoting Effect of Olaparib after X-ray and Proton Irradiation Using the Senolytic Drug, ABT-263
Sign Up to like & getrecommendations! Published in 2022 at "Cancers"
DOI: 10.3390/cancers14061460
Abstract: Simple Summary Radiotherapy is one of the most common treatments for cancer. Overcoming the failure and side effects of radiotherapy are current challenges. It has been recently demonstrated that senescence contributes to radioresistance. Cellular senescence… read more here.
Keywords: cell; abt 263; olaparib; senolytic drug ... See more keywords
Developing 3D Organoid Raft Cultures from Patient-Derived Xenografts as Rapid Models to Screen Efficacy of Experimental Therapeutics
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms232214392
Abstract: Reliable preclinical models are needed for screening new cancer drugs. Thus, we developed an improved 3D tumor organoid model termed “organoid raft cultures” (ORCs). Development of ORCs involved culturing tumors ex vivo on collagen beds… read more here.
Keywords: abt 263; derived xenografts; patient derived; organoid raft ... See more keywords