[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 …

Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

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 …

The molecular details of cytokine signaling via the JAK/STAT pathway

R Morris, NJ Kershaw, JJ Babon - Protein Science, 2018 - Wiley Online Library
More than 50 cytokines signal via the JAK/STAT pathway to orchestrate hematopoiesis,
induce inflammation and control the immune response. Cytokines are secreted …

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 …

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 …

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

Conformational states dynamically populated by a kinase determine its function

T Xie, T Saleh, P Rossi, CG Kalodimos - Science, 2020 - science.org
INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …

[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 …

Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Cyclins and cyclin-dependent protein kinases (CDKs) are important proteins that are
required for the regulation and expression of the large number of components necessary for …