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Special Issue "Peptide Drug Discovery and Development"

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

Deadline for manuscript submissions: closed (20 September 2013)

Special Issue Editors

Guest Editor
Assoc. Professor Pankaj Karande (Website)

Department of Chemical and Biological Engineering, Rensselaer Polytechnic Institute, 3217 CBIS, 110 8th St., Troy, NY 12180, USA
Interests: drug discovery; drug delivery; peptide engineering; high throughput screening; vaccine design; biomaterials and diagnostics
Guest Editor
Prof. Dr. Bernd Groner (Website)

Georg Speyer Haus, Institute for Tumor Biology and Experimental Therapy, Paul Ehrlich Str. 42, D-60596 Frankfurt am Main, Germany
Fax: +49 69 63395185
Interests: cytokine signal transduction; peptide inhibitors of oncoproteins; breast cancer research; experimental tumor therapy

Special Issue Information

Dear Colleagues,

The journal “Pharmaceuticals” is planning to publish a special issue covering the topic “Peptide drug discovery and development” and we are inviting you to contribute an article to this volume.

Peptides represent an attractive class of molecules for the design of new drugs, lead structures, drug carriers and excepients. Recent developments in peptide synthesis techniques and high-throughput screening platforms have created enthusiasm and interest in the design and discovery of novel peptides for a broad range of biological and pharmacological applications. Advances in peptide engineering have helped to overcome traditional limitations in peptide drug development such as poor systemic stability, rapid clearance and low binding affinities to biological targets. Currently there are nearly one hundred peptide based drug candidates in clinical trials, a dramatic increase compared to a decade ago. These developments signal a ‘second wave’ in peptide drug development.

The past two decades have also witnessed the derivation of chemically modified peptide constructs. They make use of non-natural amino acids, sugars and peptide bonds to provide  natural peptide backbones with desirable structural and functional properties. These ‘peptidomimetics’ have created exciting opportunities to engineer unique and complementary physical, chemical, structural and biological activities within the peptide sequence. The ability of peptides to recognize structural domains which are not limited to conventional drug binding pockets, makes them exciting leads for drug discovery. Peptide based drugs will therefore have a significant impact in the near future for the treatment of a broad range of indications including cancer, infectious diseases, neurodegenerative diseases and inflammation.

We would like you to share your contributions to the advances and opportunities in this burgeoning field of peptide drug discovery and development for this special issue. Areas of interest include:

  • Discovery of peptide drugs, prodrugs, formulations and drug carriers
  • Peptide drugs in oncology, neurology, inflammation and other physiological disorders
  • Peptide based vaccines and immunomodulating agents
  • In vitro and in vivo validation of peptide drugs
  • Advances in synthetic peptide design and screening techniques
  • Design and engineering of peptidomimetics and other novel hybrid peptide constructs
  • Approaches for improving peptide stability and target recognition
  • Peptide Theranostics

Dr. Pankaj Karande
Prof. Dr. Bernd Groner
Guest Editors

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 quarterly 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).

Published Papers (2 papers)

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Review

Open AccessReview Antimicrobial Peptides
Pharmaceuticals 2013, 6(12), 1543-1575; doi:10.3390/ph6121543
Received: 22 October 2013 / Revised: 21 November 2013 / Accepted: 25 November 2013 / Published: 28 November 2013
Cited by 69 | PDF Full-text (575 KB) | HTML Full-text | XML Full-text
Abstract
The rapid increase in drug-resistant infections has presented a serious challenge to antimicrobial therapies. The failure of the most potent antibiotics to kill “superbugs” emphasizes the urgent need to develop other control agents. Here we review the history and new development of [...] Read more.
The rapid increase in drug-resistant infections has presented a serious challenge to antimicrobial therapies. The failure of the most potent antibiotics to kill “superbugs” emphasizes the urgent need to develop other control agents. Here we review the history and new development of antimicrobial peptides (AMPs), a growing class of natural and synthetic peptides with a wide spectrum of targets including viruses, bacteria, fungi, and parasites. We summarize the major types of AMPs, their modes of action, and the common mechanisms of AMP resistance. In addition, we discuss the principles for designing effective AMPs and the potential of using AMPs to control biofilms (multicellular structures of bacteria embedded in extracellular matrixes) and persister cells (dormant phenotypic variants of bacterial cells that are highly tolerant to antibiotics). Full article
(This article belongs to the Special Issue Peptide Drug Discovery and Development)
Open AccessReview Database-Guided Discovery of Potent Peptides to Combat HIV-1 or Superbugs
Pharmaceuticals 2013, 6(6), 728-758; doi:10.3390/ph6060728
Received: 2 April 2013 / Revised: 2 May 2013 / Accepted: 13 May 2013 / Published: 27 May 2013
Cited by 15 | PDF Full-text (636 KB) | HTML Full-text | XML Full-text
Abstract
Antimicrobial peptides (AMPs), small host defense proteins, are indispensable for the protection of multicellular organisms such as plants and animals from infection. The number of AMPs discovered per year increased steadily since the 1980s. Over 2,000 natural AMPs from bacteria, protozoa, fungi, [...] Read more.
Antimicrobial peptides (AMPs), small host defense proteins, are indispensable for the protection of multicellular organisms such as plants and animals from infection. The number of AMPs discovered per year increased steadily since the 1980s. Over 2,000 natural AMPs from bacteria, protozoa, fungi, plants, and animals have been registered into the antimicrobial peptide database (APD). The majority of these AMPs (>86%) possess 11–50 amino acids with a net charge from 0 to +7 and hydrophobic percentages between 31–70%. This article summarizes peptide discovery on the basis of the APD. The major methods are the linguistic model, database screening, de novo design, and template-based design. Using these methods, we identified various potent peptides against human immunodeficiency virus type 1 (HIV-1) or methicillin-resistant Staphylococcus aureus (MRSA). While the stepwise designed anti-HIV peptide is disulfide-linked and rich in arginines, the ab initio designed anti-MRSA peptide is linear and rich in leucines. Thus, there are different requirements for antiviral and antibacterial peptides, which could kill pathogens via different molecular targets. The biased amino acid composition in the database-designed peptides, or natural peptides such as θ-defensins, requires the use of the improved two-dimensional NMR method for structural determination to avoid the publication of misleading structure and dynamics. In the case of human cathelicidin LL-37, structural determination requires 3D NMR techniques. The high-quality structure of LL-37 provides a solid basis for understanding its interactions with membranes of bacteria and other pathogens. In conclusion, the APD database is a comprehensive platform for storing, classifying, searching, predicting, and designing potent peptides against pathogenic bacteria, viruses, fungi, parasites, and cancer cells. Full article
(This article belongs to the Special Issue Peptide Drug Discovery and Development)
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