Emerging principles in protease-based drug discovery

M Drag, GS Salvesen - Nature reviews Drug discovery, 2010 - nature.com
Proteases have an important role in many signalling pathways, and represent potential drug
targets for diseases ranging from cardiovascular disorders to cancer, as well as for …

Targeting p38 MAPK pathway for the treatment of Alzheimer's disease

L Munoz, AJ Ammit - Neuropharmacology, 2010 - Elsevier
Accumulating evidence indicates that p38 mitogen-activated protein kinase (MAPK) could
play more than one role in Alzheimer's disease (AD) pathophysiology and that patients …

[图书][B] Introduction to proteins: structure, function, and motion

A Kessel, N Ben-Tal - 2018 - taylorfrancis.com
Introduction to Proteins provides a comprehensive and state-of-the-art introduction to the
structure, function, and motion of proteins for students, faculty, and researchers at all levels …

[HTML][HTML] The origin of allosteric functional modulation: multiple pre-existing pathways

A Del Sol, CJ Tsai, B Ma, R Nussinov - Structure, 2009 - cell.com
Although allostery draws increasing attention, not much is known about allosteric
mechanisms. Here we argue that in all proteins, allosteric signals transmit through multiple …

[HTML][HTML] Development of allosteric modulators of GPCRs for treatment of CNS disorders

HH Nickols, PJ Conn - Neurobiology of disease, 2014 - Elsevier
The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a
promising new strategy with potential for developing novel treatments for a variety of central …

Selectively nonselective kinase inhibition: striking the right balance

R Morphy - Journal of medicinal chemistry, 2010 - ACS Publications
Protein kinases have become the second most exploited group of drug targets after G-
protein-coupled receptors (GPCRs), accounting for 30% of drug discovery projects at many …

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

BJ Melancon, CR Hopkins, MR Wood… - Journal of medicinal …, 2012 - ACS Publications
(PAMs), which potentiate GABAA receptor response, and negative allosteric modulators
(NAMs), which decrease channel activity and modulate the ability of these GABAergic …

Flavonoids as protein kinase inhibitors for cancer chemoprevention: direct binding and molecular modeling

DX Hou, T Kumamoto - Antioxidants & redox signaling, 2010 - liebertpub.com
Protein kinases play crucial roles in the regulation of multiple cell signaling pathways and
cellular functions. Deregulation of protein kinase function has been implicated in …

Mechanisms of drug resistance in kinases

R Barouch-Bentov, K Sauer - Expert opinion on investigational …, 2011 - Taylor & Francis
Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

Approaches to discover non-ATP site kinase inhibitors

LK Gavrin, E Saiah - MedChemComm, 2013 - pubs.rsc.org
The catalytic domain of kinases shows a high degree of sequence homology, especially for
kinases that belong to the same family. They share a common ATP binding site with a …