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Related publications (29)

In vitro synergistic action of TAT-RasGAP 317-326 peptide with antibiotics against Gram-negative pathogens

Grazia Vizzarro

Objectives: Multidrug-resistant (MDR) bacteria are a continuously increasing threat for medicine, caus-ing infections recalcitrant to antibiotics. Antimicrobial peptides (AMPs) were identified as alternatives to antibiotics, being naturally occurring short ...

2022

Methods for the generation of large combinatorial macrocycle libraries

Sevan Mleh Habeshian

Macrocycles are an attractive class of molecules due to their good binding properties and yet rather small size that allows, in many cases, crossing membranes to reach intracellular targets. In comparison to classical small molecule drugs, macrocycles are ...

EPFL2021

Small peptide diversification through photoredox-catalyzed oxidative C-terminal modification

Jérôme Waser, Eliott Hugo Joran Le Du, Marion Marie-Agnès Garreau

A photoredox-catalyzed oxidative decarboxylative coupling of small peptides is reported, giving access to a variety of N,O-acetals. They were used as intermediates for the addition of phenols and indoles, leading to novel peptide scaffolds and bioconjugate ...

2021

A minimalistic cyclic ice-binding peptide from phage display

Harm-Anton Klok, Luciano Andres Abriata, Matthew Gibson, Xudong Kong, Corey Alfred Stevens

Developing molecules that emulate the properties of naturally occurring ice-binding proteins (IBPs) is a daunting challenge. Rather than relying on the (limited) existing structure–property relationships that have been established for IBPs, here we report ...

Nature Research2021

Hypervalent Iodine-Mediated Late-Stage Peptide and Protein Functionalization

Jérôme Waser, Elija Grinhagena, Emmanuelle Madeline Dominique Allouche

Hypervalent iodine compounds are powerful reagents for the development of novel transformations. As they exhibit low toxicity, high functional group tolerance, and stability in biocompatible media, they have been used for the functionalization of biomolecu ...

Wiley-VCH Verlag GmbH2022

Amphiphilic Iodine(III) Reagents for the Lipophilization of Peptides in Water

Jérôme Waser, Durga Prasada Rao Hari, Romain Gaëtan Tessier, Abhaya Kumar Mishra

We report the functionalization of cysteine residues with lipophilic alkynes bearing a silyl group or an alkyl chain using amphiphilic ethynylbenziodoxolone reagents (EBXs). The reactions were carried out in buffer (pH 6 to 9), without organic co-solvent o ...

Wiley-VCH Verlag GmbH2021

Macrocyclization of omega-Isocyanoaldehydes and Towards the Total Synthesis of Jamaicensamide A

Teerawat Songsichan

In the first chapter of this thesis, the macrocyclization of a new type of bifunctional substrates, omega-isocyanoaldehyde derivatives, is described. Ten different omega-isocyanoaldehydes in terms of different ring sizes and functional groups were prepared ...

EPFL2021

The Drosophila Baramicin polypeptide gene protects against fungal infection

Bruno Lemaitre, Mark Austin Hanson, Igor Iatsenko, Alice Marra

The fruit fly Drosophila melanogaster combats microbial infection by producing a battery of effector peptides that are secreted into the haemolymph. Technical difficulties prevented the investigation of these short effector genes until the recent advent of ...

2021

De novo development of proteolytically resistant therapeutic peptides for oral administration

Christian Heinis, Luciano Andres Abriata, Florence Pojer, Xudong Kong, Vanessa Carle, Kaycie Marie Butler, Jun Moriya

The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...

2020

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