Special Issue "Allosteric Modulators"
A special issue of Pharmaceuticals (ISSN 1424-8247).
Deadline for manuscript submissions: closed (15 April 2014)
Dr. Marlene A. Jacobson
Moulder Center for Drug Discovery Research, Temple University School Of Pharmacy, 3307 North Broad Street, Philadelphia, PA 19140, USA
Interests: allosteric modulators of G-protein coupled receptors including muscarinic and metabotropic glutamate receptors
Recent advancements in the discovery of allosteric modulators for G protein-coupled receptors (GPCRs) and kinases have revolutionized drug discovery and development. While most currently marketed drugs bind to the orthosteric site for the endogenous ligand, allosteric modulators bind to topographically distinct sites. Orthosteric sites are in general highly conserved across protein superfamilies and identification of highly selective ligands is challenging. Targeting allosteric sites on GPCRs and kinases has emerged as a successful strategy for identification of highly selective ligands with therapeutic utility for the treatment of disease states which previously could not be addressed due to inability to identify subtype selective ligands. In recent years, the discovery of GPCR allosteric modulators as treatments for CNS disorders including schizophrenia, Fragile X and Alzheimer’s disease and allosteric inhibitors for kinases have advanced into clinical development. This special issue invites original research including review articles on the pharmacology, chemical biology and medicinal chemistry of allosteric modulators including assay development and screening technologies, mechanism of action, structural features of binding sites and clinical research and development.
Dr. Marlene A. Jacobson
Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.
Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are refereed through a peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed Open Access monthly journal published by MDPI.
- allosteric modulation
- drug discovery
- G protein coupled receptors
- positive allosteric modulator
- negative allosteric modulator
- allosteric inhibitor
- bitopic ligand