Targeting aberrant RAS/RAF/MEK/ERK signaling for cancer therapy
U Degirmenci, M Wang, J Hu - Cells, 2020 - mdpi.com
The RAS/RAF/MEK/ERK (MAPK) signaling cascade is essential for cell inter-and intra-
cellular communication, which regulates fundamental cell functions such as growth, survival …
cellular communication, which regulates fundamental cell functions such as growth, survival …
Targeting ERK1/2 protein-serine/threonine kinases in human cancers
R Roskoski Jr - Pharmacological research, 2019 - Elsevier
ERK1 and ERK2 are key protein kinases that contribute to the Ras-Raf-MEK-ERK MAP
kinase signalling module. This pathway participates in the control of numerous processes …
kinase signalling module. This pathway participates in the control of numerous processes …
Conformational states dynamically populated by a kinase determine its function
INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …
physiological function is the regulation of their binding and enzymatic activities, which is …
Ligand binding remodels protein side-chain conformational heterogeneity
SA Wankowicz, SH de Oliveira, DW Hogan… - Elife, 2022 - elifesciences.org
While protein conformational heterogeneity plays an important role in many aspects of
biological function, including ligand binding, its impact has been difficult to quantify …
biological function, including ligand binding, its impact has been difficult to quantify …
A molecular switch modulates assembly and host factor binding of the HIV-1 capsid
RT Schirra, NFB Dos Santos, KK Zadrozny… - Nature structural & …, 2023 - nature.com
The HIV-1 capsid is a fullerene cone made of quasi-equivalent hexamers and pentamers of
the viral CA protein. Typically, quasi-equivalent assembly of viral capsid subunits is …
the viral CA protein. Typically, quasi-equivalent assembly of viral capsid subunits is …
An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering
Allostery is an inherent feature of proteins, but it remains challenging to reveal the
mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic …
mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic …
From structure to the dynamic regulation of a molecular switch: A journey over 3 decades
SS Taylor, J Wu, JGH Bruystens, JC Del Rio… - Journal of Biological …, 2021 - ASBMB
It is difficult to imagine where the signaling community would be today without the Protein
Data Bank. This visionary resource, established in the 1970s, has been an essential partner …
Data Bank. This visionary resource, established in the 1970s, has been an essential partner …
Structure, activation and dysregulation of fibroblast growth factor receptor kinases: perspectives for clinical targeting
The receptor tyrosine kinase family of fibroblast growth factor receptors (FGFRs) play crucial
roles in embryonic development, metabolism, tissue homeostasis and wound repair via …
roles in embryonic development, metabolism, tissue homeostasis and wound repair via …
[HTML][HTML] The mechanism of activation of monomeric B-Raf V600E
RC Maloney, M Zhang, H Jang, R Nussinov - Computational and Structural …, 2021 - Elsevier
Oncogenic mutations in the serine/threonine kinase B-Raf, particularly the V600E mutation,
are frequent in cancer, making it a major drug target. Although much is known about B-Raf's …
are frequent in cancer, making it a major drug target. Although much is known about B-Raf's …
ATP-competitive inhibitors modulate the substrate binding cooperativity of a kinase by altering its conformational entropy
ATP-competitive inhibitors are currently the largest class of clinically approved drugs for
protein kinases. By targeting the ATP-binding pocket, these compounds block the catalytic …
protein kinases. By targeting the ATP-binding pocket, these compounds block the catalytic …