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In Silico Characterization of Novel PTEN Activators
EP27264
Poster Title: In Silico Characterization of Novel PTEN Activators
Submitted on 12 Feb 2018
Author(s): Jacob Wilson1, Emily Palumbo2, Fiona Kearns3, Peng Teng1, Prerna Malaney2, Vladimir Uversky1,5, , Jianfeng Cai3, H. Lee Woodcock3, Vrushank Davé2,6
Affiliations: 1) Depts. of Molecular Medicine, 2) Depts. of Pathology and Cell Biology, 3) USF Depts. of Chemistry, College of Arts and Sciences, 4) USF College of Pharmacy, 5) USF Health Byrd Alzheimer’s Research Institute, 6) H. Lee Moffitt Cancer Center, University of South Florida, Tampa, FL 33612
This poster was presented at USF Health Research Day
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Poster Information
Abstract: PTEN is a crucial tumor suppressor that is commonly mutated or down-regulated in several diseases, which aberrantly activates oncogenic PI3K/AKT signaling. Chemotherapeutic agents and kinase inhibitors (KIs) have met with off-target effects and chemoresistance. We hypothesize that direct activation of endogenous PTEN will reduce aberrant PI3K signaling and minimize the dose of chemotherapeutic or KIs. We have identified and characterized novel small molecules (γ-AAPeptides), which are the first to directly activate PTEN function. Herein, we have utilized in silico methods to elucidate the interaction between these small molecules and PTEN. Furthermore, we will employ in vitro mutational analysis to corroborate our results of proposed integral residues.Summary: The frequent inactivation of PTEN in vivo is linked to the oncogenic activation of the P13K pathway. In this poster, we suggest a positive allosteric modulation of PTEN.Report abuse »
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