Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors

JJL Liao - Journal of medicinal chemistry, 2007 - ACS Publications
Protein kinases constitute one of the largest protein families in humans. 1, 2 The kinase
enzymes in this family catalyze phosphorylation of serine, threonine, or tyrosine residues …

Aurora kinase inhibitors: progress towards the clinic

M Kollareddy, D Zheleva, P Dzubak… - Investigational new …, 2012 - Springer
The Aurora kinases (serine/threonine kinases) were discovered in 1995 during studies of
mutant alleles associated with abnormal spindle pole formation in Drosophila melanogaster …

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase

MG Manfredi, JA Ecsedy, KA Meetze… - Proceedings of the …, 2007 - National Acad Sciences
Increased Aurora A expression occurs in a variety of human cancers and induces
chromosomal abnormalities during mitosis associated with tumor initiation and progression …

A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma

G Görgün, E Calabrese, T Hideshima… - Blood, The Journal …, 2010 - ashpublications.org
Aurora-A is a mitotic kinase that regulates mitotic spindle formation and segregation. In
multiple myeloma (MM), high Aurora-A gene expression has been correlated with …

Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase

AA Mortlock, KM Foote, NM Heron… - Journal of medicinal …, 2007 - ACS Publications
The Aurora kinases have been the subject of considerable interest as targets for the
development of new anticancer agents. While evidence suggests inhibition of Aurora B …

PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer

P Carpinelli, R Ceruti, ML Giorgini, P Cappella… - Molecular cancer …, 2007 - AACR
PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against
Aurora kinases and cross-reactivities with some receptor tyrosine kinases relevant for …

Mitotic drug targets and the development of novel anti-mitotic anticancer drugs

M Schmidt, H Bastians - Drug resistance updates, 2007 - Elsevier
Drugs that interfere with the normal progression of mitosis belong to the most successful
chemotherapeutic compounds currently used for anti-cancer treatment. Classically, these …

Recent progress in anticancer agents incorporating pyrazole scaffold

S Mor, M Khatri, R Punia… - Mini Reviews in Medicinal …, 2022 - benthamdirect.com
The search for new anticancer agents is considered a dynamic field of medicinal chemistry.
In recent years, the synthesis of compounds with anticancer potential has increased and a …

MLN8054, a small-molecule inhibitor of Aurora A, causes spindle pole and chromosome congression defects leading to aneuploidy

K Hoar, A Chakravarty, C Rabino… - … and cellular biology, 2007 - Am Soc Microbiol
Aurora A kinase plays an essential role in the proper assembly and function of the mitotic
spindle, as its perturbation causes defects in centrosome separation, spindle pole …

Molecular mechanism of Aurora A kinase autophosphorylation and its allosteric activation by TPX2

A Zorba, V Buosi, S Kutter, N Kern, F Pontiggia, YJ Cho… - Elife, 2014 - elifesciences.org
We elucidate the molecular mechanisms of two distinct activation strategies
(autophosphorylation and TPX2-mediated activation) in human Aurora A kinase. Classic …