Special Issue "GPCR Based Drug Discovery"
A special issue of Pharmaceuticals (ISSN 1424-8247).
Deadline for manuscript submissions: closed (31 March 2013)
Dr. Sandra Siehler
Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, WSJ-88.2.05, 4002 Basel, Switzerland
Interests: G protein-coupled receptors (GPCRs); G proteins; RhoGEF-Rho signaling; adenylyl cyclases; cellular signaling pathways; cell-based/ biochemical/ -physical assays for membrane proteins; cardiovascular pharmacology; drug discovery
Multiple G protein-coupled receptors (GPCRs) are present on the cell surface of every cell type, form complexes with other receptors and proteins, and transmit signals into the intracellular lumen to regulate key physiological events. Dysregulated GPCR signaling is causative for pathophysiological conditions, and targeting of GPCRs is hence widely utilized for therapeutic intervention. The recent advancements towards purification, in vitro reconstitution, and structural determination of GPCRs open up new avenues for biochemical –and physical strategies to complement classical cellular drug discovery approaches. Emerging cellular signaling aspects of GPCRs include new temporal and spatial insights, and emerging concepts on G12/13 and MAPK pathways, adenylyl cyclase isoform-specific signaling, and ligand pharmacology. Physiological cell systems containing native GPCRs and signaling environments become more important in early drug discovery to identify GPCR ligands with activities projectable to in vivo disease models and related pharmacodynamic readouts. The purpose of this special issue is to capture these novel facets of GPCR drug discovery.
Dr. Sandra Siehler
Manuscript Submission Information
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. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short 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.
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- GPCR structures
- biochemical/-physical approaches for GPCRs
- kinetic analyses of GPCRs signaling
- spatial signaling of GPCRs
- cellular assays for GPCRs in recombinant versus primary cells/ differentiated stem cells
- G12/13 signaling of GPCRs
- GPCR-linked MAPK signaling pathways (ERK, p38MAPK, JNK)
- adenylyl cyclases as mediators of GPCR signaling
- pharmacology/ functional selectivity of GPCR ligands
- pathophysiological signaling of GPCRs
- in vivo pharmacodynamic assays for GPCRs