Development of withaferin A analogs as probes of angiogenesis

Bioorganic & Medicinal Chemistry Letters
Yasuno YokotaRoyce Mohan

Abstract

The natural product withaferin A (WFA) is a potent angiogenesis inhibitor and it targets the ubiquitin-proteasome pathway in vascular endothelial cells. We generated a biotinylated affinity analog WFA-LC(2)B for use as a probe to study angiogenesis. WFA-LC(2)B inhibits angiogenic sprouting in vitro and it causes levels of ubiquitinated proteins to increase in tumor necrosis factor-alpha-treated human umbilical vein endothelial cells, confirming the retention of WFA's biological activity. We show that WFA-LC(2)B forms protein adducts in endothelial cells which are competed by free WFA in vivo. This WFA-LC(2)B analog will be useful to isolate the biological target of WFA.

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Citations

Jan 6, 2010·The Journal of Biological Chemistry·Paola Bargagna-MohanRoyce Mohan
Mar 15, 2014·Journal of Medicinal Chemistry·E M Kithsiri WijeratneA A Leslie Gunatilaka
Sep 23, 2009·Biochemical Pharmacology·Yanke YuDuxin Sun
Sep 18, 2012·Biochemical Pharmacology·Wim Vanden BergheKaren Heyninck
May 18, 2016·Acta Biomaterialia·David G BelairWilliam L Murphy
Jan 26, 2008·Organic & Biomolecular Chemistry·Mathieu Pucheault
Sep 15, 2011·Magnetic Resonance in Chemistry : MRC·S K BhartiRaja Roy
Apr 17, 2012·Natural Product Reports·Malte GerschStephan A Sieber
May 29, 2010·Journal of Basic and Clinical Physiology and Pharmacology·Thangavel Jeyanthi, Perumal Subramanian
Nov 12, 2016·Journal of Neuro-oncology·Jasdeep DhamiSanjiv S Gambhir
Nov 26, 2011·The Journal of Biological Chemistry·Paola Bargagna-MohanRoyce Mohan
Aug 14, 2019·Biochemical Pharmacology·Behrouz HassanniaWim Vanden Berghe
Apr 4, 2021·Chemistry : a European Journal·Elisa BonandiDaniele Passarella

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