There has been huge progress in the discovery of targeted cancer therapies in recent years.
However, even for the most successful and impactful cancer drugs which have been …

Abstract The RAF-MEK-ERK signaling cascade is a well-characterized MAPK pathway
involved in cell proliferation and survival. The three-layered MAPK signaling cascade is …

Abstract RAS mutations (HRAS, NRAS, and KRAS) are among the most common
oncogenes, and around 19% of patients with cancer harbor RAS mutations. Cells harboring …

An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Right-sided (proximal) colorectal cancer (CRC) has a poor prognosis and a distinct
mutational profile, characterized by oncogenic BRAF mutations and aberrations in mismatch …

Extracellular signal-regulated protein kinase 1/2 (ERK1/2), the only known substrate of
MEK1/2, is located downstream of the RAS-RAF-MEK-ERK (MAPK) pathway and is …

The RAS-ERK pathway is a fundamental signaling cascade crucial for many biological
processes including proliferation, cell cycle control, growth, and survival; common across all …

The mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase 1/2
(ERK1/2) signaling pathway is widely activated by a variety of extracellular stimuli, and its …

Activation of the extracellular signal-regulated kinase-2 (ERK2) by phosphorylation has
been shown to involve changes in protein dynamics, as determined by hydrogen-deuterium …

In this work, pyrrole-2-carboxamides were designed with a structure-guided strategy based
on the crystal structure of MmpL3 and a pharmacophore model. The structure–activity …