[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

R Roskoski Jr - Pharmacological research, 2020 - Elsevier
Because genetic alterations including mutations, overexpression, translocations, and
dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this …

Properties of FDA-approved small molecule protein kinase inhibitors

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …

[HTML][HTML] Structural mechanism of a drug-binding process involving a large conformational change of the protein target

P Ayaz, A Lyczek, YT Paung, VR Mingione… - Nature …, 2023 - nature.com
Proteins often undergo large conformational changes when binding small molecules, but
atomic-level descriptions of such events have been elusive. Here, we report unguided …

Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update

R Roskoski Jr - Pharmacological research, 2021 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, the
protein kinase enzyme family has become one of the most important drug targets in the 21st …

[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update

R Roskoski Jr - Pharmacological research, 2024 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

[HTML][HTML] Structural analysis of the full-length human LRRK2

A Myasnikov, H Zhu, P Hixson, B Xie, K Yu, A Pitre… - Cell, 2021 - cell.com
Mutations in leucine-rich repeat kinase 2 (LRRK2) are commonly implicated in the
pathogenesis of both familial and sporadic Parkinson's disease (PD). LRRK2 regulates …

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 …

ERK1/2 MAP kinases: structure, function, and regulation

R Roskoski Jr - Pharmacological research, 2012 - Elsevier
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-
MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large …

[HTML][HTML] The role of the ALK receptor in cancer biology

B Hallberg, RH Palmer - Annals of Oncology, 2016 - Elsevier
ABSTRACT A vast array of oncogenic variants has been identified for anaplastic lymphoma
kinase (ALK). Therefore, there is a need to better understand the role of ALK in cancer …