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 …
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
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 …
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …
Trends in kinase drug discovery: targets, indications and inhibitor design
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 …
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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
myeloid leukemia as well as other selected cancers has greatly increased optimism for the …