Y
Yelena Zherebina
Publications - 3
Citations - 62
Yelena Zherebina is an academic researcher. The author has contributed to research in topics: Selectivity & Axial chirality. The author has an hindex of 2, co-authored 3 publications receiving 39 citations.
Papers
More filters
Journal ArticleDOI
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor
Jayaraman Chandrasekhar,Ryan Dick,Joshua Van Veldhuizen,David Koditek,Eve-Irene Lepist,Mary E. McGrath,Leena Patel,Gary Phillips,Sedillo Kassandra F,John R. Somoza,Joseph Therrien,Nicholas Alexander Till,Jennifer Treiberg,Armando G. Villaseñor,Yelena Zherebina,Stephane Perreault +15 more
TL;DR: A case in which torsional scan studies guided the thoughtful creation of a restricted axis of rotation between two heteroaromatic systems of a phosphoinositide 3-kinase (PI3K) β inhibitor, generating a pair of atropisomeric compounds with significantly different pharmacological and pharmacokinetic profiles.
Journal ArticleDOI
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency
Julie Farand,Nicholas Mai,Jayaraman Chandrasekhar,Zachary Newby,Josh Van Veldhuizen,Jennifer A. Loyer-Drew,Chandrasekar Venkataramani,Guerrero Juan A,Amy Kwok,Ning Li,Yelena Zherebina,Sibylle Wilbert,Jeff Zablocki,Gary Phillips,William J. Watkins,Robert J. Mourey,Notte Gregory +16 more
TL;DR: In many cases, macrocyclization improved Pyk2 potency while weakening FAK potency, thereby improving thePyk2/FAK selectivity ratio for this structural class of inhibitors.
Journal ArticleDOI
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif
Stephane Perreault,Fatima Arjmand,Jayaraman Chandrasekhar,Jia Hao,Kathleen S. Keegan,David Koditek,Eve-Irene Lepist,Clinton K. Matson,Mary E. McGrath,Leena Patel,Sedillo Kassandra F,Joseph Therrien,Nicholas Alexander Till,Adrian Tomkinson,Jennifer Treiberg,Yelena Zherebina,Gary Phillips +16 more
TL;DR: This work led to the discovery of (P)-14, a highly selective and orally bioavailable PI3Kβ inhibitor displaying an excellent pharmacokinetic profile in addition to great cellular potency in various PTEN-deficient tumor cell lines.