DS6: anticandidal, antibiofilm peptide against Candida tropicalis and exhibit synergy with commercial drug
In conclusion, DS6 may have utility as an alternative antifungal therapy for C. tropicalis. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd. DS6 peptide exhibits efficient antifungal activity with no toxic effect on normal cells. DS6 can provide clues to aid the discovery of new drug combinations with investigations regarding modes of action refining clinical utility and conventional drug resistance. (Source: Journal of Peptide Science)
Source: Journal of Peptide Science - January 24, 2017 Category: Biochemistry Authors: Kusum Singh, Shashank Shekhar, Yudhishthir Yadav, Immaculata Xess, Sharmistha Dey Tags: Research Article Source Type: research

The 3 ‐nitro‐2‐pyridinesulfenyl group: synthesis and applications to peptide chemistry
The 3‐nitro‐2‐pyridinesulfenyl chloride, commonly abbreviated as Npys‐Cl, was among the first stable heterocyclic sulfenyl halides to be isolated. After its discovery, the Npys group was widely used as a protecting group for the amines, alcohols and thiols. Herein, we have reviewed some of the aspects of the Npys‐Cl moiety, and its most promising recent uses are summarized, from the stability of the Npys protection of amines, hydroxyls and thiols and removal conditions for potential applications in peptide synthesis, to one of its most successful applications for the formation of mixed disulfides. Indeed, Npys pr...
Source: Journal of Peptide Science - January 24, 2017 Category: Biochemistry Authors: C édric Rentier, Kentarou Fukumoto, Akihiro Taguchi, Yoshio Hayashi Tags: Special Issue Review Source Type: research

Antifungal peptides: a potential new class of antifungals for treating vulvovaginal candidiasis caused by fluconazole ‐resistant Candida albicans
Vulvovaginal candidiasis/candidosis is a common fungal infection afflicting approximately 75% of women globally caused primarily by the yeast Candida albicans. Fluconazole is widely regarded as the antifungal drug of choice since its introduction in 1990 due to its high oral bioavailability, convenient dosing regimen and favourable safety profile. However, its widespread use has led to the emergence of fluconazole‐resistant C. albicans, posing a universal clinical concern. Coupled to the dearth of new antifungal drugs entering the market, it is imperative to introduce new drug classes to counter this threat. Antimicrobia...
Source: Journal of Peptide Science - January 18, 2017 Category: Biochemistry Authors: Siew Mei Samantha Ng, Yi Yong Alvin Yap, Jin Wei Darryl Cheong, Fui Mee Ng, Qiu Ying Lau, Timothy Barkham, Jeanette Woon Pei Teo, Jeffrey Hill, Cheng San Brian Chia Tags: Research Article Source Type: research

Development of poly(lactide ‐co‐glycolide) nanoparticles functionalized with a mitochondria penetrating peptide
The development of mitochondria‐targeting cell permeable vectors represents a promising therapeutic approach for several diseases, such as cancer and oxidative pathologies. Nevertheless, access to mitochondria can be difficult. A new hybrid material composed by poly(lactide‐co‐glycolide) (PLGA) functionalized with a 6‐mer mitochondria penetrating peptide (MPP), consisting in alternating arginine and unnatural cyclohexylalanine, was developed. Circular dichroism, FT‐IR and DSC studies indicated that the conjugation of the peptide with the polymer led to the obtainment of a more rigid material with respect to both ...
Source: Journal of Peptide Science - January 16, 2017 Category: Biochemistry Authors: Francesca Selmin, Giulia Magri, Chiara G.M. Gennari, Silvia Marchian ò, Nicola Ferri, Sara Pellegrino Tags: Special Issue Article Source Type: research

Issue information
(Source: Journal of Peptide Science)
Source: Journal of Peptide Science - January 16, 2017 Category: Biochemistry Tags: Issue Information Source Type: research

Bivalent 14 ‐mer peptide ligands of CXCR4 with polyproline linkers with anti‐chemotactic activity against Jurkat cells
Interaction of CXCR4 with its endogenous ligand, stromal‐cell derived factor‐1 (SDF‐1)/CXCL12, induces various physiological functions involving chemotaxis. Bivalent ligands with a polyproline helix bearing a cyclic pentapeptide, FC131, were previously shown to have higher binding affinities for CXCR4 than the corresponding monovalent ligands. Bivalent ligands based on a 14‐mer peptide T140 derivative with polyproline linkers have been designed and synthesized. The activity of these peptides as well as the effect of bivalency of the ligand on CXCR4 binding has been assessed. The binding affinity of these series of ...
Source: Journal of Peptide Science - January 11, 2017 Category: Biochemistry Authors: Tomohiro Tanaka, Toru Aoki, Wataru Nomura, Hirokazu Tamamura Tags: Special Issue Article Source Type: research

Histidine ‐rich designer peptides of the LAH4 family promote cell delivery of a multitude of cargo
The histidine‐rich designer peptides of the LAH4 family exhibit potent antimicrobial, transfection, transduction and cell‐penetrating properties. They form non‐covalent complexes with their cargo, which often carry a negative overall charge at pH 7.4 and include a large range of molecules and structures such as oligonucleotides, including siRNA and DNA, peptides, proteins, nanodots and adeno‐associated viruses. These complexes are thought to enter the cells through an endosomal pathway where the acidification of the organelle is essential for efficient endosomal escape. Biophysical measurements indicate that, upon ...
Source: Journal of Peptide Science - January 8, 2017 Category: Biochemistry Authors: Gilles Moulay, Christian Leborgne, A. James Mason, Christopher Aisenbrey, Antoine Kichler, Burkhard Bechinger Tags: Special Issue Article Source Type: research

Comparison of patient ‐derived high and low phosphatidylserine‐exposing colorectal carcinoma cells in their interaction with anti‐cancer peptides
Current cancer treatment is frequently compromised by severe adverse effects on healthy cells and tissues as well as by the increasing burden of (multi‐)drug resistances. Some representatives of small, amphipathic peptides known as host defense peptides possess the potential to overcome these limitations and to evolve as future anti‐cancer therapeutics. Peptide NK‐2, derived from porcine NK‐lysin, was originally discovered due to its broad‐spectrum antimicrobial activities. Today, also potent anti‐cancer activity is proven and accompanied by low toxicity towards normal human cells. The molecular basis underlyin...
Source: Journal of Peptide Science - January 7, 2017 Category: Biochemistry Authors: Dominik Wilms, J örg Andrä Tags: Research Article Source Type: research

An unexpected cell ‐penetrating peptide from Bothrops jararaca venom identified through a novel size exclusion chromatography screening
Efficient drug delivery systems are currently one of the greatest challenges in pharmacokinetics, and the transposition of the gap between in vitro candidate molecule and in vivo test drug is, sometimes, poles apart. In this sense, the cell‐penetrating peptides (CPP) may be the bridge uniting these worlds. Here, we describe a technique to rapidly identify unlabeled CPPs after incubation with liposomes, based on commercial desalting (size exclusion) columns and liquid chromatography‐MS/MS, for peptide de novo sequencing. Using this approach, we found it possible to identify one new CPP – interestingly, a classical bra...
Source: Journal of Peptide Science - January 4, 2017 Category: Biochemistry Authors: Juliana Mozer Sciani, Hugo Vigerelli, Andr é Santos Costa, Diana Aparecida Dias Câmara, Paulo Luiz‐de‐Sá Junior, Daniel Carvalho Pimenta Tags: Research Article Source Type: research

The importance of being Aib. Aggregation and self ‐assembly studies on conformationally constrained oligopeptides
The role of the conformationally constrained α‐aminoisobutyric acid (Aib) residue in the aggregation and self‐assembly properties of oligopeptides is discussed, critically reviewing our recent work in the field. In this connection, three significant case studies are presented: (i) aggregation propensity of Aib homo‐oligopeptides of different length; (ii) perturbation of the conformational and aggregation properties of Ala‐based pentapeptides by a single Aib versus Ala substitution; and (iii) build up of self‐assembled monolayers formed by Aib homo‐hexapeptide building blocks. The peptides investigated were all...
Source: Journal of Peptide Science - January 4, 2017 Category: Biochemistry Authors: Mariano Venanzi, Emanuela Gatto, Fernando Formaggio, Claudio Toniolo Tags: Special Issue Review Source Type: research

Comparison of neurotoxicity of different aggregated forms of A β40, Aβ42 and Aβ43 in cell cultures
The abnormal deposition of amyloid‐β (Aβ) peptides in the brain is the main neuropathological hallmark of Alzheimer's disease (AD). Amyloid deposits are formed by a heterogeneous mixture of Aβ peptides, among which the most studied are Aβ40 and Aβ42. Aβ40 is abundantly produced in the human brain, but the level of Aβ42 is remarkably increased in the brain of AD patients. Aside from Aβ40 and Aβ42, recent data have raised the possibility that Aβ43 peptides may be instrumental in AD pathogenesis. Besides its length, whether the Aβ aggregated form accounts for the neurotoxicity is also particularly controversial. ...
Source: Journal of Peptide Science - December 31, 2016 Category: Biochemistry Authors: Lu Fu, Yao Sun, Yongqing Guo, Yan Chen, Bin Yu, Haihong Zhang, Jiaxin Wu, Xianghui Yu, Wei Kong, Hui Wu Tags: Research Article Source Type: research

Design of fluorogenic probes and fluorescent ‐tagged inhibitors for γ‐glutamyl cyclotransferase
A tumor‐related protein, human chromosome 7 ORF 24 (C7orf24), is involved in regulation of the glutathione homeostasis cycle as a γ‐glutamyl cyclotransferase (GGCT). The singular substrate preference of this enzyme had long hampered its chemical probe development. That is, substrate of GGCT is definitely ‘γ‐Glu‐Xaa’, where Xaa is an L‐α‐amino acid. Based on the structure of substrates and GGCT fluorogenic probes, LISA‐4/101, we succesfully developed a fluorescent‐tagged inhibitor, gKFA. These chemical tools will assist cancer‐related researches in the future. Copyright © 2017 European Peptide Soci...
Source: Journal of Peptide Science - December 31, 2016 Category: Biochemistry Authors: Taku Yoshiya, Hiromi Ii, Shugo Tsuda, Masayoshi Mochizuki, Susumu Kageyama, Tatsuhiro Yoshiki Tags: Special Issue Article Source Type: research

Infectivity inhibition by overlapping synthetic peptides derived from the gH/gL heterodimer of herpes simplex virus type 1
Herpes simplex virus (HSV) is a human pathogen that infects epithelial cells. The cutaneous lesions, caused by the virus, spread to the nervous system creating several complications. Fusion of host membranes with the viral envelope is mandatory and mediated by a group of glycoproteins conserved in all Herpesviridae subfamilies, such as the glycoproteins B (gB), H (gH), L (gL) and D (gD). We investigated the inhibitory activity mediated by synthetic overlapping peptides spanning the entire ectodomains of gH and gL glycoproteins. We have performed a brute analysis of the complete gH/gL heterodimer in order to explore the inh...
Source: Journal of Peptide Science - December 31, 2016 Category: Biochemistry Authors: Franci Gianluigi, Falanga Annarita, Zannella Carla, Folliero Veronica, Martora Francesca, Galdiero Marilena, Galdiero Stefania, Morelli Giancarlo, Galdiero Massimiliano Tags: Special Issue Article Source Type: research

Effects of arginine and leucine substitutions on anti ‐endotoxic activities and mechanisms of action of cationic and amphipathic antimicrobial octadecapeptide from rice α‐amylase
This study shows that the arginine‐substituted and leucine‐substituted AmyI‐1‐18 analogs with improved anti‐endotoxic and antimicrobial activities have clinical potential as dual‐function host defense agents. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd. Several AmyI‐1‐18 analogs containing arginine or leucine substitutions were designed on the basis of the helical wheel projection of AmyI‐1‐18 (parent peptide). Anti‐endotoxic activity of AmyI‐1‐18 is enhanced with increased cationicity and hydrophobicity. This study shows that the arginine‐substituted and leucine...
Source: Journal of Peptide Science - December 31, 2016 Category: Biochemistry Authors: Masayuki Taniguchi, Akihito Ochiai, Ryu Toyoda, Teppei Sato, Eiichi Saitoh, Tetsuo Kato, Takaaki Tanaka Tags: Research Article Source Type: research

Synergistic activity profile of an antimicrobial peptide against multidrug ‐resistant and extensively drug‐resistant strains of Gram‐negative bacterial pathogens
Infection sustained by multidrug‐resistant and extensively drug‐resistant bacterial pathogens is often untreatable with the standard of care antibiotics, and the combination of anti‐infective compounds often represents the only therapeutic strategy to face this major clinical treat. SET‐M33 is a novel antimicrobial peptide (AMP) that has demonstrated in vitro and in vivo antimicrobial activity against Gram‐negative bacteria and has shown interesting features in preclinical evaluations. Particularly, it showed efficacy against a number of multidrug‐resistant and extensively drug‐resistant clinical strains of G...
Source: Journal of Peptide Science - December 31, 2016 Category: Biochemistry Authors: Simona Pollini, Jlenia Brunetti, Samanta Sennati, Gian Maria Rossolini, Luisa Bracci, Alessandro Pini, Chiara Falciani Tags: Special Issue Article Source Type: research