Structure-Guided Discovery of Selective Polo-Like Kinase 3 Inhibitors.

Jeremy L Yap¹, Gabrielle Lovett², Jeremy W Mason², Joseph Tucker¹, David Boe¹, Andy Chen¹, Karen J Coffman², Jamie DaSilva³, Theresa Dickinson², Veronique Frattini², Yanfei Guan², Michel Farchi Guiraldelli², Xinjun J Hou², Jayasankar Jasti², Nathaniel T Kenton¹, Roger Machin-Rivera², Lisa Marroquin³, Christopher L McClendon², Mikayla McLaughlin², Amanda Pecora², Matthew C Robinson¹, Ingrid A Stock², George S Tria², Jamison Tuttle², Jennifer A Young², Lei Zhang², Alpha A Lee¹

¹Drug Discovery, PostEra, Cambridge, Massachusetts 02142-1187, United States.

²Pfizer Research and Development, Cambridge, Massachusetts 02139, United States.

³Pfizer Research and Development, Groton, Connecticut 06340, United States.

PubMed PMC DOI PDF

Abstract

Polo-like kinases (PLKs) are a family of closely related serine/threonine kinases responsible for regulating cell cycle processes and proliferation. While PLK1 inhibitors have led to clinical candidates for oncology, the biological function of other PLKs is relatively unknown, in part, because there is a dearth of selective tool compounds. Herein we report the parallel medicinal chemistry (PMC) an…

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