Special Issue "GPCR Based Drug Discovery"

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A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 March 2013)

Special Issue Editor

Guest Editor
Dr. Sandra Siehler
Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, WSJ-88.2.05, 4002 Basel, Switzerland
E-Mail: sandra.siehler@novartis.com
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

Special Issue Information

Dear Colleagues,

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
Guest Editor

Submission

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.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 800 CHF (Swiss Francs).

Keywords

  • 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

Published Papers (16 papers)

Pharmaceuticals 2013, 6(8), 915-928; doi:10.3390/ph6080915
Received: 6 May 2013; in revised form: 18 July 2013 / Accepted: 26 July 2013 / Published: 2 August 2013
Show/Hide Abstract | PDF Full-text (249 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2013, 6(4), 500-509; doi:10.3390/ph6040500
Received: 6 March 2013; in revised form: 20 March 2013 / Accepted: 1 April 2013 / Published: 8 April 2013
Show/Hide Abstract | Cited by 2 | PDF Full-text (939 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2012, 5(5), 417-446; doi:10.3390/ph5050417
Received: 3 February 2012; in revised form: 18 April 2012 / Accepted: 19 April 2012 / Published: 27 April 2012
Show/Hide Abstract | Cited by 2 | PDF Full-text (533 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(4), 652-664; doi:10.3390/ph4040652
Received: 17 February 2011; in revised form: 2 April 2011 / Accepted: 6 April 2011 / Published: 13 April 2011
Show/Hide Abstract | Cited by 6 | PDF Full-text (948 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(4), 567-589; doi:10.3390/ph4040567
Received: 11 March 2011; in revised form: 22 March 2011 / Accepted: 22 March 2011 / Published: 25 March 2011
Show/Hide Abstract | Cited by 3 | PDF Full-text (454 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(3), 524-550; doi:10.3390/ph4030524
Received: 17 December 2010; in revised form: 7 March 2011 / Accepted: 7 March 2011 / Published: 14 March 2011
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Pharmaceuticals 2011, 4(3), 509-523; doi:10.3390/ph4030509
Received: 3 February 2011; in revised form: 9 March 2011 / Accepted: 9 March 2011 / Published: 14 March 2011
Show/Hide Abstract | Cited by 1 | PDF Full-text (690 KB) | HTML Full-text | XML Full-text
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Pharmaceuticals 2011, 4(3), 485-493; doi:10.3390/ph4030485
Received: 3 February 2011; in revised form: 4 March 2011 / Accepted: 7 March 2011 / Published: 9 March 2011
Show/Hide Abstract | Cited by 1 | PDF Full-text (236 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(3), 457-469; doi:10.3390/ph4030457
Received: 13 December 2010; in revised form: 17 February 2011 / Accepted: 18 February 2011 / Published: 25 February 2011
Show/Hide Abstract | Cited by 3 | PDF Full-text (1028 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(2), 273-284; doi:10.3390/ph4020273
Received: 6 December 2010; in revised form: 7 January 2011 / Accepted: 14 January 2011 / Published: 25 January 2011
Show/Hide Abstract | Cited by 3 | PDF Full-text (289 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(2), 244-272; doi:10.3390/ph4020244
Received: 6 December 2010; in revised form: 22 December 2010 / Accepted: 18 January 2011 / Published: 25 January 2011
Show/Hide Abstract | Cited by 4 | PDF Full-text (216 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(1), 202-214; doi:10.3390/ph4010202
Received: 1 December 2010; in revised form: 23 December 2010 / Accepted: 24 December 2010 / Published: 18 January 2011
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Pharmaceuticals 2011, 4(1), 117-137; doi:10.3390/ph4010117
Received: 30 November 2010; in revised form: 25 December 2010 / Accepted: 4 January 2011 / Published: 4 January 2011
Show/Hide Abstract | Cited by 1 | PDF Full-text (251 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2011, 4(1), 7-43; doi:10.3390/ph4010007
Received: 24 November 2010; in revised form: 20 December 2010 / Accepted: 21 December 2010 / Published: 23 December 2010
Show/Hide Abstract | Cited by 6 | PDF Full-text (1717 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2010, 3(11), 3478-3493; doi:10.3390/ph3113478
Received: 21 September 2010; in revised form: 27 October 2010 / Accepted: 8 November 2010 / Published: 9 November 2010
Show/Hide Abstract | Cited by 2 | PDF Full-text (307 KB) | HTML Full-text | XML Full-text

Pharmaceuticals 2010, 3(9), 2821-2837; doi:10.3390/ph3092821
Received: 2 July 2010; in revised form: 18 August 2010 / Accepted: 20 August 2010 / Published: 26 August 2010
Show/Hide Abstract | PDF Full-text (213 KB) | HTML Full-text | XML Full-text

Last update: 1 November 2012

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