Protein kinase inhibitors: contributions from structure to clinical compounds
LN Johnson - Quarterly reviews of biophysics, 2009 - cambridge.org
Protein kinases catalyse key phosphorylation reactions in signalling cascades that affect
every aspect of cell growth, differentiation and metabolism. The kinases have become prime …
every aspect of cell growth, differentiation and metabolism. The kinases have become prime …
Small molecule kinase inhibitors as anti-cancer therapeutics
O Chahrour, D Cairns, Z Omran - Mini reviews in medicinal …, 2012 - ingentaconnect.com
Protein kinases have emerged as the most important class of targets in oncology drug
discovery because of their major roles in regulating cellular growth and survival. At least, 11 …
discovery because of their major roles in regulating cellular growth and survival. At least, 11 …
Protein kinase inhibitors: emerging pharmacophores 1997-2000
J Dumas - Expert Opinion on Therapeutic Patents, 2001 - Taylor & Francis
Kinase inhibition is a major area for therapeutic intervention against a variety of diseases
including cancer, inflammatory disorders and diabetes. While this mode of action remains …
including cancer, inflammatory disorders and diabetes. While this mode of action remains …
Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition
AC Backes, B Zech, B Felber, B Klebl… - Expert opinion on drug …, 2008 - Taylor & Francis
Background: Protein kinases are essential enzymes propagating cellular signal transduction
processes and consequently emerged as central targets for drug discovery against a wide …
processes and consequently emerged as central targets for drug discovery against a wide …
Non-ATP competitive protein kinase inhibitors
L Garuti, M Roberti, G Bottegoni - Current medicinal chemistry, 2010 - ingentaconnect.com
Protein kinases represent an attractive target in oncology drug discovery. Most of kinase
inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is …
inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is …
Through the “gatekeeper door”: exploiting the active kinase conformation
F Zuccotto, E Ardini, E Casale… - Journal of medicinal …, 2010 - ACS Publications
The human genome comprises more than 500 protein kinases including serine/threonine,
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …
Protein kinase inhibitors: structural insights into selectivity
R Thaimattam, R Banerjee, R Miglani… - Current pharmaceutical …, 2007 - ingentaconnect.com
Protein kinases are involved in many diseases like cancer, inflammation, cardiovascular
disease, and diabetes. They have become attractive target classes for drug development …
disease, and diabetes. They have become attractive target classes for drug development …
Small-molecule inhibitors binding to protein kinases. Part I: exceptions from the traditional pharmacophore approach of type I inhibition
AC Backes, B Zech, B Felber, B Klebl… - Expert Opinion on Drug …, 2008 - Taylor & Francis
Background: Protein kinases are essential enzymes propagating cellular signal transduction
processes and consequently have emerged as central targets for drug discovery against a …
processes and consequently have emerged as central targets for drug discovery against a …
New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors
V Lamba, I Ghosh - Current pharmaceutical design, 2012 - ingentaconnect.com
Over the past decade, therapeutics that target subsets of the 518 human protein kinases
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …
Recent kinase and kinase inhibitor X-ray structures: mechanisms of inhibition and selectivity insights
M Cherry, DH Williams - Current medicinal chemistry, 2004 - ingentaconnect.com
Recent years have seen an explosion in the number of publicly available x-ray crystal
structures of protein kinases. These structures have provided a wealth of information on the …
structures of protein kinases. These structures have provided a wealth of information on the …