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Select item 66144461.

Apogossypol-mediated reorganisation of the endoplasmic reticulum antagonises mitochondrial fission and apoptosis

Govindaraju Yedida, Mateus Milani, Gerald M Cohen, Shankar Varadarajan

Cell Death Dis. 2019 Jul; 10(7): 521. Published online 2019 Jul 8. doi: 10.1038/s41419-019-1759-y

PMCID:: PMC6614446

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Select item 26530562.

Synthesis and evaluation of Apogossypol Atropisomers as Potential Bcl-x_L Antagonists

Jun Wei, Michele F. Rega, Shinichi Kitada, Hongbin Yuan, Dayong Zhai, Prabhakar Risbood, Herbert H. Seltzman, Charles E. Twine, John C. Reed, Maurizio Pellecchia

Cancer Lett. Author manuscript; available in PMC 2010 Jan 8.

Published in final edited form as: Cancer Lett. 2009 Jan 8; 273(1): 107–113. Published online 2008 Sep 7. doi: 10.1016/j.canlet.2008.07.031

PMCID:: PMC2653056

Article PDF–1.6M

Select item 43949643.

Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo

WENHUA ZHAN, XINGBIN HU, JING YI, QUNXING AN, XIAOFENG HUANG

Mol Med Rep. 2015 Jun; 11(6): 4142–4148. Published online 2015 Feb 10. doi: 10.3892/mmr.2015.3326

Correction in:: Mol Med Rep. 2018 Jun; 17(6): 8010.

PMCID:: PMC4394964

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Select item 22654584.

Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2–transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048)

Shinichi Kitada, Christina L. Kress, Maryla Krajewska, Lee Jia, Maurizio Pellecchia, John C. Reed

Blood. 2008 Mar 15; 111(6): 3211–3219. Prepublished online 2008 Jan 17. doi: 10.1182/blood-2007-09-113647

PMCID:: PMC2265458

Article

Select item 27508235.

Apogossypol Derivatives as Antagonists of Anti-apoptotic Bcl-2 Family Proteins

Jun Wei, Shinichi Kitada, Michele F. Rega, Aras Emdadi, Hongbin Yuan, Jason Cellitti, John L. Stebbins, Dayong Zhai, Jiazhi Sun, Li Yang, Russell Dahl, Ziming Zhang, Bainan Wu, Si Wang, Tyler A. Reed, Hong-Gang Wang, Nicholas Lawrence, Said Sebti, John C. Reed, Maurizio Pellecchia

Mol Cancer Ther. Author manuscript; available in PMC 2010 Apr 1.

Published in final edited form as: Mol Cancer Ther. 2009 Apr; 8(4): 904–913. doi: 10.1158/1535-7163.MCT-08-1050

Correction in:: volume 8 on page 2076

PMCID:: PMC2750823

Article PDF–1.9M

Select item 32288806.

Enhanced delivery of mda-7/IL-24 using a serotype chimeric adenovirus (Ad.5/3) in combination with the Apogossypol derivative BI-97C1 (Sabutoclax) improves therapeutic efficacy in low CAR colorectal cancer cells

Belal Azab, Rupesh Dash, Swadesh K. Das, Sujit K. Bhutia, Xue-Ning Shen, Bridget A. Quinn, Siddik Sarkar, Xiang-Yang Wang, Michael Hedvat, Igor P. Dmitriev, David T. Curiel, Steven Grant, Paul Dent, John C. Reed, Maurizio Pellecchia, Devanand Sarkar, Paul B. Fisher

J Cell Physiol. Author manuscript; available in PMC 2013 May 1.

Published in final edited form as: J Cell Physiol. 2012 May; 227(5): 2145–2153. doi: 10.1002/jcp.22947

PMCID:: PMC3228880

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Select item 28808507.

BI-97C1, an Optically Pure Apogossypol Derivative as Pan-Active Inhibitor of Anti-apoptotic B-cell lymphoma/leukemia-2 (Bcl-2) Family Proteins

Jun Wei, John L. Stebbins, Shinichi Kitada, Rupesh Dash, William Placzek, Michele F. Rega, Bainan Wu, Jason Cellitti, Dayong Zhai, Li Yang, Russell Dahl, Paul B. Fisher, John C. Reed, Maurizio Pellecchia

J Med Chem. Author manuscript; available in PMC 2011 May 27.

Published in final edited form as: J Med Chem. 2010 May 27; 53(10): 4166–4176. doi: 10.1021/jm1001265

PMCID:: PMC2880850

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Select item 31024018.

Apogossypol derivative BI-97C1 (Sabutoclax) targeting Mcl-1 sensitizes prostate cancer cells to mda-7/IL-24–mediated toxicity

Rupesh Dash, Belal Azab, Bridget A. Quinn, Xuening Shen, Xiang-Yang Wang, Swadesh K. Das, Mohamed Rahmani, Jun Wei, Michael Hedvat, Paul Dent, Igor P. Dmitriev, David T. Curiel, Steven Grant, Bainan Wu, John L. Stebbins, Maurizio Pellecchia, John C. Reed, Devanand Sarkar, Paul B. Fisher

Proc Natl Acad Sci U S A. 2011 May 24; 108(21): 8785–8790. Published online 2011 May 9. doi: 10.1073/pnas.1100769108

Correction in:: Proc Natl Acad Sci U S A. 2017 May 30; 114(22): E4522–E4523.

PMCID:: PMC3102401

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Select item 27474809.

Apogossypol Derivatives as Pan-active Inhibitors of Anti-apoptotic B-cell lymphoma/leukemia-2 (Bcl-2) Family Proteins

Jun Wei, Shinichi Kitada, Michele F. Rega, John L. Stebbins, Dayong Zhai, Jason Cellitti, Hongbin Yuan, Aras Emdadi, Russell Dahl, Ziming Zhang, Li Yang, John C. Reed, Maurizio Pellecchia

J Med Chem. Author manuscript; available in PMC 2010 Jul 23.

Published in final edited form as: J Med Chem. 2009 Jul 23; 52(14): 4511–4523. doi: 10.1021/jm900472s

PMCID:: PMC2747480

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Select item 357407010.

Endoplasmic Reticulum Membrane Reorganization Is Regulated by Ionic Homeostasis

Shankar Varadarajan, Kayoko Tanaka, Joshua L. Smalley, Edward T. W. Bampton, Maurizio Pellecchia, David Dinsdale, Gary B. Willars, Gerald M. Cohen

PLoS One. 2013; 8(2): e56603. Published online 2013 Feb 15. doi: 10.1371/journal.pone.0056603

PMCID:: PMC3574070

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Select item 350470111.

A novel cellular stress response characterised by a rapid reorganisation of membranes of the endoplasmic reticulum

S Varadarajan, E T W Bampton, J L Smalley, K Tanaka, R E Caves, M Butterworth, J Wei, M Pellecchia, J Mitcheson, T W Gant, D Dinsdale, G M Cohen

Cell Death Differ. 2012 Dec; 19(12): 1896–1907. Published online 2012 Sep 7. doi: 10.1038/cdd.2012.108

PMCID:: PMC3504701

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Select item 448441412.

Therapy of prostate cancer using a novel cancer terminator virus and a small molecule BH-3 mimetic

Siddik Sarkar, Bridget A. Quinn, Xue-Ning Shen, Rupesh Dash, Swadesh K. Das, Luni Emdad, Alexander L. Klibanov, Xiang-Yang Wang, Maurizio Pellecchia, Devanand Sarkar, Paul B. Fisher

Oncotarget. 2015 May 10; 6(13): 10712–10727. Published online 2015 Mar 12. doi: 10.18632/oncotarget.3544

PMCID:: PMC4484414

Article PDF–7.3M

Select item 410602413.

Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo

Yuan Sun, Jack Wu, Amro Aboukameel, Sanjeev Banerjee, Alan A. Arnold, Jianyong Chen, Zaneta Nikolovska-Coleska, Yanqiong Lin, Xiaolan Ling, Dajun Yang, Shaomeng Wang, Ayad Al-Katib, Ramzi M. Mohammad

Cancer Biol Ther. Author manuscript; available in PMC 2014 Jul 22.

Published in final edited form as: Cancer Biol Ther. 2008 Sep; 7(9): 1418–1426. Published online 2008 Sep 4. doi: 10.4161/cbt.7.9.6430

PMCID:: PMC4106024

Article PDF–752K

Select item 926093314.

Practical Strategy to 1,1′-Dideoxygossypol Derivatives from Gossypol and Its Antitumor Activities

Wei Wang, Yuzhi Lu, Juncheng Ge, Niya Liu

ACS Omega. 2022 Jul 5; 7(26): 22938–22943. Published online 2022 Jun 22. doi: 10.1021/acsomega.2c02955

PMCID:: PMC9260933

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Select item 379244115.

Evaluation and critical assessment of putative MCL-1 inhibitors

S Varadarajan, M Vogler, M Butterworth, D Dinsdale, L D Walensky, G M Cohen

Cell Death Differ. 2013 Nov; 20(11): 1475–1484. Published online 2013 Jul 5. doi: 10.1038/cdd.2013.79

PMCID:: PMC3792441

Article PDF–3.6M

Select item 376398616.

Selected Approaches for Rational Drug Design and High Throughput Screening to Identify Anti-Cancer Molecules

Michael Hedvat, Luni Emdad, Swadesh K. Das, Keetae Kim, Santanu Dasgupta, Shibu Thomas, Bin Hu, Shan Zhu, Rupesh Dash, Bridget A. Quinn, Regina A. Oyesanya, Timothy P. Kegelman, Upneet K. Sokhi, Siddik Sarkar, Eda Erdogan, Mitchell E. Menezes, Praveen Bhoopathi, Xiang-Yang Wang, Martin G. Pomper, Jun Wei, Bainan Wu, John L. Stebbins, Paul W. Diaz, John C. Reed, Maurizio Pellecchia, Devanand Sarkar, Paul B. Fisher

Anticancer Agents Med Chem. Author manuscript; available in PMC 2013 Sep 5.

Published in final edited form as: Anticancer Agents Med Chem. 2012 Nov; 12(9): 1143–1155. doi: 10.2174/187152012803529709

PMCID:: PMC3763986

Article PDF–3.1M

Select item 978767517.

Gossypol and Its Natural Derivatives: Multitargeted Phytochemicals as Potential Drug Candidates for Oncologic Diseases

Dilipkumar Pal, Pooja Sahu, Gautam Sethi, Carly E. Wallace, Anupam Bishayee

Pharmaceutics. 2022 Dec; 14(12): 2624. Published online 2022 Nov 28. doi: 10.3390/pharmaceutics14122624

PMCID:: PMC9787675

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Select item 280568018.

New targets for the treatment of follicular lymphoma

Nishant Tageja, Subhash Padheye, Prasad Dandawate, Ayad Al-Katib, Ramzi M Mohammad

J Hematol Oncol. 2009; 2: 50. Published online 2009 Dec 23. doi: 10.1186/1756-8722-2-50

PMCID:: PMC2805680

Article PDF–792K

Select item 598396919.

Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo

Wenhua Zhan, Xingbin Hu, Jing Yi, Qunxing An, Xiaofeng Huang

Mol Med Rep. 2018 Jun; 17(6): 8010. Published online 2018 Feb 13. doi: 10.3892/mmr.2018.8571

Corrects:: Mol Med Rep. 2015 Jun; 11(6): 4142–4148.

PMCID:: PMC5983969

Correction PDF–849K

Select item 415222820.

Bcl-2 Antagonists: A Proof of Concept for CLL Therapy

Kumudha Balakrishnan, Varsha Gandhi

Invest New Drugs. Author manuscript; available in PMC 2014 Sep 2.

Published in final edited form as: Invest New Drugs. 2013 Oct; 31(5): 1384–1394. Published online 2013 Aug 2. doi: 10.1007/s10637-013-0002-4

PMCID:: PMC4152228

Article PDF–282K

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Figure 6

Cell-based assays. (A) Effects of (−) Apogossypol (black squares), (+) Apogossypol (red diamonds), and racemic Apogossypol (green circles) on cell viability of the RS11846 lymphoma cell line. (B) Effects of (−) Apogossypol (black squares), (+) Apogossypol (red diamonds), and racemic Apogossypol (green circles) on cell viability of the DOHH2 lymphoma cell line.

Synthesis and evaluation of Apogossypol Atropisomers as Potential Bcl-xL Antagonists

Cancer Lett. ;273(1):107-113.
Figure 2

Normal phase chiral HPLC of Apogossypol isomers (A) HPLC of racemic Apogossypol (B) HPLC of the (−) Apogossypol (C) HPLC of the (+) Apogossypol.

Synthesis and evaluation of Apogossypol Atropisomers as Potential Bcl-xL Antagonists

Cancer Lett. ;273(1):107-113.
Figure 4

NMR binding studies. (A) Aliphatic region of the ¹H-NMR spectrum of Bcl-x_L (in red) and Bcl-x_L (50 μM) in presence of (−) Apogossypol (200 μM, green), (+) Apogossypol (200 μM, blue) and racemic Apogossypol (200 μM, black). (B) Superposition of [¹⁵N, ¹H]-TROSY spectra of free Bcl-x_L (125 μM, red) after addition of (−) Apogossypol (green, 500 μM) and (+) Apogossypol (blue,500 μM).

Synthesis and evaluation of Apogossypol Atropisomers as Potential Bcl-xL Antagonists

Cancer Lett. ;273(1):107-113.
Figure 1

Apogossypol inhibits the survival and the proliferation of LNCaP cells. (A) Chemical structures of gossypol and apogossypol. (B) An MTT assay was used to evaluate the in vitro anti-survival effects of apogossypol and gossypol. (C) A colony formation assay was performed to assess the anti-proliferation effects of apogossypol and gossypol. ^*P<0.05, compared with the gossypol treated group.

Inhibitory activity of apogossypol in human prostate cancer in vitro and in vivo

Mol Med Rep. 2015 Jun;11(6):4142-4148.