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Protein & Peptide Letters , 23 Issue 12

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Protein & Peptide Letter Article 23, Issue 12

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Protein & Peptide Letters

Highlighted Artcile: Exploration of the Medicinal Peptide Space

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Exploration of the Medicinal Peptide Space

Author(s):

Bert Gevaert, Sofie Stalmans, Evelien Wynendaele, Lien Taevernier, Nathalie Bracke, Matthias D'Hondt and Bart De Spiegeleer Pages 324 - 335 ( 12 )

Abstract:

The chemical properties of peptide medicines, known as the ‘medicinal peptide space’ is considered a multi-dimensional subset of the global peptide space, where each dimension represents a chemical descriptor. These descriptors can be linked to biofunctional, medicinal properties to varying degrees. Knowledge of this space can increase the efficiency of the peptide-drug discovery and development process, as well as advance our understanding and classification of peptide medicines.

For 245 peptide drugs, already available on the market or in clinical development, multivariate dataexploration was performed using peptide relevant physicochemical descriptors, their specific peptidedrug target and their clinical use. Our retrospective analysis indicates that clusters in the medicinal peptide space are located in a relatively narrow range of the physicochemical space: dense and empty regions were found, which can be explored for the discovery of novel peptide drugs.

Keywords:

Chemical space, drug discovery, drug market, peptide therapeutics, PCA.

Affiliation:

Drug Quality and Registration (DruQuaR) group, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium

Graphical Abstract:

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Most Cited Article: Novel Antimicrobial Peptides Isolated from Skin Secretions of the Mexican Frog Hyla eximia

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Novel Antimicrobial Peptides Isolated from Skin Secretions of the Mexican Frog Hyla eximia

Author(s):

Oscar Villa-Hernandez, Lorena Hernandez-Orihuela, Maria del Carmen Rodriguez, Fernando Zamudio-Zuniga, Ruben Castro-Franco, Victoria Pando and Cesar V.F. Batista Pages 1371 - 1378 ( 8 )

Abstract:

In this work, we describe the original characterization of peptides and proteins present in the skin secretions of the Mexican amphibian Hyla eximia. To this purpose, a novel water/dark extraction method, as well as the classic electrical stimulation procedure, was applied in order to extract the skin secretion. Two novel antimicrobial peptides He-1 and He-2 were sequenced. In addition, a molecular mass fingerprint revealed more than one hundred different molecules. Eight peptides in homogeneous form were assayed against five species of bacteria. Thereafter, the peptide He-2 demonstrated high antiparasitic activity against ookinete forms of malaria parasites at low concentration.

Keywords:

Hyla eximia, antimicrobial peptides, mass spectrometry

Affiliation:

Unidad de Proteomica, Instituto de Biotecnologia-UNAM, Av. Universidad, 2001, Col. Chamilpa, CP 62210, Cuernavaca, Mor, Mexico.

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