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2005 1
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2014 33
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Page 1
Obatoclax mesylate : pharmacology and potential for therapy of hematological neoplasms.
Joudeh J, Claxton D. Joudeh J, et al. Expert Opin Investig Drugs. 2012 Mar;21(3):363-73. doi: 10.1517/13543784.2012.652302. Epub 2012 Feb 11. Expert Opin Investig Drugs. 2012. PMID: 22324354 Review.
AREAS COVERED: The pan Bcl-2 family member BH3 domain mimetic obatoclax (GX15-070) is currently under clinical evaluation in solid tumors and hematological neoplasms. ...Pharmacology, pharmacodynamics, drug resistance and clinical use of this agent in leukemias and lymphom …
AREAS COVERED: The pan Bcl-2 family member BH3 domain mimetic obatoclax (GX15-070) is currently under clinical evaluation in solid tu …
Obatoclax mesylate, a pan-bcl-2 inhibitor, in combination with docetaxel in a phase 1/2 trial in relapsed non-small-cell lung cancer.
Chiappori A, Williams C, Northfelt DW, Adams JW, Malik S, Edelman MJ, Rosen P, Van Echo DA, Berger MS, Haura EB. Chiappori A, et al. J Thorac Oncol. 2014 Jan;9(1):121-5. doi: 10.1097/JTO.0000000000000027. J Thorac Oncol. 2014. PMID: 24346101 Free PMC article. Clinical Trial.
INTRODUCTION: The proapoptotic small-molecule pan-Bcl-2 inhibitor obatoclax mesylate (GX15-070) may enhance the cytotoxicity of chemotherapy in relapsed/refractory non-small-cell lung cancer (NSCLC). ...Neutropenia (31%), febrile neutropenia (16%), and dyspnea (19%) …
INTRODUCTION: The proapoptotic small-molecule pan-Bcl-2 inhibitor obatoclax mesylate (GX15-070) may enhance the cytotoxicity o …
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy.
Castillo Bautista CM, Eismann K, Gentzel M, Pelucchi S, Mertens J, Walters HE, Yun MH, Sterneckert J. Castillo Bautista CM, et al. Cells. 2023 Sep 11;12(18):2247. doi: 10.3390/cells12182247. Cells. 2023. PMID: 37759469 Free PMC article.
We used an induced pluripotent stem cell model of ALS caused by mutant FUS to identify a small molecule BH3 mimetic that disrupts the BECN1-BCL2 interaction. We identified obatoclax as a brain-penetrant drug candidate that rescued neurons at nanomolar concentrations by red …
We used an induced pluripotent stem cell model of ALS caused by mutant FUS to identify a small molecule BH3 mimetic that disrupts the BECN1- …
The BH3 Mimetic Obatoclax Accumulates in Lysosomes and Causes Their Alkalinization.
Stamelos VA, Fisher N, Bamrah H, Voisey C, Price JC, Farrell WE, Redman CW, Richardson A. Stamelos VA, et al. PLoS One. 2016 Mar 7;11(3):e0150696. doi: 10.1371/journal.pone.0150696. eCollection 2016. PLoS One. 2016. PMID: 26950068 Free PMC article.
We have evaluated the mechanism of action of obatoclax in eight ovarian cancer cell lines. Consistent with its function as a BH3 mimetic, obatoclax induced apoptosis in three cell lines. ...These studies explain, for the first time, how obatoclax inhibits lys …
We have evaluated the mechanism of action of obatoclax in eight ovarian cancer cell lines. Consistent with its function as a BH3 mime …
An evidence-based review of obatoclax mesylate in the treatment of hematological malignancies.
Goard CA, Schimmer AD. Goard CA, et al. Core Evid. 2013;8:15-26. doi: 10.2147/CE.S42568. Epub 2013 Mar 14. Core Evid. 2013. PMID: 23515850 Free PMC article.
Obatoclax mesylate is an intravenously-administered drug under investigation in Phase I and II clinical trials as a novel anticancer therapeutic for hematological malignancies and solid tumors. ...By understanding the molecular underpinnings of obatoclax resp …
Obatoclax mesylate is an intravenously-administered drug under investigation in Phase I and II clinical trials as a novel anti …
Obatoclax induces G1/G0-phase arrest via p38/p21(waf1/Cip1) signaling pathway in human esophageal cancer cells.
Zhong D, Gu C, Shi L, Xun T, Li X, Liu S, Yu L. Zhong D, et al. J Cell Biochem. 2014 Sep;115(9):1624-35. doi: 10.1002/jcb.24829. J Cell Biochem. 2014. PMID: 24788582
The cell cycle arresting effect of obatoclax was associated with up-regulation of p21(waf1/Cip1). Knockdown of p21(waf1/Cip1) significantly attenuated obatoclax-induced G1/G0-phase arrest. Although obatoclax stimulated phosphorylation of Erk, p38, and JNK, ph …
The cell cycle arresting effect of obatoclax was associated with up-regulation of p21(waf1/Cip1). Knockdown of p21(waf1/Cip1) signifi …
Biomimetic nanoparticle loading obatoclax mesylate for the treatment of non-small-cell lung cancer (NSCLC) through suppressing Bcl-2 signaling.
Chen S, Ren Y, Duan P. Chen S, et al. Biomed Pharmacother. 2020 Sep;129:110371. doi: 10.1016/j.biopha.2020.110371. Epub 2020 Jun 18. Biomed Pharmacother. 2020. PMID: 32563984 Free article.
Lung cancer still remains a leading cause of cancer mortality in the world. Obatoclax mesylate (OM), a B cell chronic lymphocytic leukemia/lymphoma 2 (Bcl-2) family antagonist, is a potential antitumor drug. ...
Lung cancer still remains a leading cause of cancer mortality in the world. Obatoclax mesylate (OM), a B cell chronic lymphocy …
Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-kappaB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells.
Zhou C, Li T, Xia M, Wu Z, Zhong X, Li A, Rashid HK, Ma C, Zhou R, Duan H, Zhang X, Peng J, Li L. Zhou C, et al. ACS Infect Dis. 2023 Nov 10;9(11):2105-2118. doi: 10.1021/acsinfecdis.3c00218. Epub 2023 Oct 5. ACS Infect Dis. 2023. PMID: 37796279
Obatoclax promotes HIV-1 transcriptional initiation and elongation by regulating the NF-kappaB pathway. Obatoclax activates caspase 8 and does not induce the phosphorylation of the antiapoptotic protein Bcl-2 in latent HIV-1 infected cell lines. ...
Obatoclax promotes HIV-1 transcriptional initiation and elongation by regulating the NF-kappaB pathway. Obatoclax activates ca …
Obatoclax inhibits SARS-CoV-2 entry by altered endosomal acidification and impaired cathepsin and furin activity in vitro.
Mao B, Le-Trilling VTK, Wang K, Mennerich D, Hu J, Zhao Z, Zheng J, Deng Y, Katschinski B, Xu S, Zhang G, Cai X, Hu Y, Wang J, Lu M, Huang A, Tang N, Trilling M, Lin Y. Mao B, et al. Emerg Microbes Infect. 2022 Dec;11(1):483-497. doi: 10.1080/22221751.2022.2026739. Emerg Microbes Infect. 2022. PMID: 34989664 Free PMC article.
Additionally, obatoclax impaired the SARS-CoV-2 S-mediated membrane fusion by targeting the MCL-1 protein and reducing furin protease activity. ...Our data suggested that obatoclax should be further explored as a clinical drug for the treatment of COVID-19....
Additionally, obatoclax impaired the SARS-CoV-2 S-mediated membrane fusion by targeting the MCL-1 protein and reducing furin protease …
279 results