A historical overview of protein kinases and their targeted small molecule inhibitors

R Roskoski Jr - Pharmacological research, 2015 - Elsevier
Protein kinases play a predominant regulatory role in nearly every aspect of cell biology and
they can modify the function of a protein in almost every conceivable way. Protein …

Kinase drug discovery 20 years after imatinib: progress and future directions

P Cohen, D Cross, PA Jänne - Nature reviews drug discovery, 2021 - nature.com
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

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 …

Protein kinase biochemistry and drug discovery

PA Schwartz, BW Murray - Bioorganic chemistry, 2011 - Elsevier
Protein kinases are fascinating biological catalysts with a rapidly expanding knowledge
base, a growing appreciation in cell regulatory control, and an ascendant role in successful …

How many kinases are druggable? A review of our current understanding

B Anderson, P Rosston, HW Ong… - Biochemical …, 2023 - portlandpress.com
There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …

Imatinib: a selective tyrosine kinase inhibitor

PW Manley, SW Cowan-Jacob, E Buchdunger… - European journal of …, 2002 - Elsevier
The understanding of the pathophysiology of a large number of cancer types provides a
strategy to target cancer cells with minimal effect on normal cells. Protein phosphorylation …

Approved and experimental small‐molecule oncology kinase inhibitor drugs: a mid‐2016 overview

PM Fischer - Medicinal research reviews, 2017 - Wiley Online Library
Kinase inhibitor research is a comparatively recent branch of medicinal chemistry and
pharmacology and the first small‐molecule kinase inhibitor, imatinib, was approved for …

The development and therapeutic potential of protein kinase inhibitors

P Cohen - Current Opinion in Chemical Biology, 1999 - Elsevier
The development and therapeutic potential of protein kinase inhibitors r Page 1 459 The
development and therapeutic potential of protein kinase inhibitors Philip Cohen A number of …

The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling

AC Dar, KM Shokat - Annual review of biochemistry, 2011 - annualreviews.org
Kinases are highly regulated enzymes with diverse mechanisms controlling their catalytic
output. Over time, chemical discovery efforts for kinases have produced ATP-competitive …

Opportunities and challenges in the development of kinase inhibitor therapy for cancer

CL Sawyers - Genes & development, 2003 - genesdev.cshlp.org
The success of the tyrosine kinase imatinib inhibitor (Gleevec, STI571) in treating chronic
myeloid leukemia as well as other selected cancers has greatly increased optimism for the …