From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement
Yelena Mostinski, Guus J.J.E. Heynen, María P. López‐Alberca, Jérôme Paul, Sandra Miksche, Silke Radetzki, David Schaller, Elena Shanina, Carola Seyffarth, Yuliya Kolomeets, Nandor Ziebart, Judith de Schryver, Sylvia Oestreich, Martin Neuenschwander, Yvette Roske, Udo Heinemann, Christoph Rademacher, Andrea Volkamer, Jens Peter von Kries, Walter Birchmeier, Marc Nazaré
Abstract
inhibited proliferation of two cancer cell lines that are resistant to cancer drugs and diminished ERK signaling.
Topics & Concepts
ChemistryMAPK/ERK pathwayPyrazolonesProtein kinase BCell growthCancer researchPI3K/AKT/mTOR pathwayDrug discoverySignal transductionPharmacologyBiochemistryBiologyMedicinal chemistryProtein Tyrosine PhosphatasesCytokine Signaling Pathways and InteractionsGalectins and Cancer Biology