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New methods for developing (bi)cyclic peptides by phage display

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Solid-phase peptide synthesis in 384-well plates

Christian Heinis, Edward Jeffrey Will, Anne Sofie Luise Zarda, Alexander Lund Nielsen, Sevan Mleh Habeshian, Mischa Schüttel, Gontran Sangouard

Newer solid-phase peptide synthesis and release strategies enable the production of short peptides with high purity, allowing direct screening for desired bioactivity without prior chromatographic purification. However, the maximum number of peptides that ...

Hoboken2024

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative motor disorder, which results in death within a few years of diagnosis. While the cause of most cases of ALS is unknown, 10% of cases are familial (fALS), and associated with mutations in one of ov ...

EPFL2023

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...

Berlin2023

Synthesis of Trifluoromethylated Alkenes: Hypervalent Iodine Meets High-Valent Copper

Jérôme Waser, Tobias Michael Milzarek

The first trifluoromethylation of vinylbenziodoxolones (VBX) is reported herein. The synthetic method is based on the use of bench-stable, high-valent copper(III) species, and the reaction can be initiated under thermal conditions and/or irradiation (365 n ...

WILEY-V C H VERLAG GMBH2023

De novo developed small cyclic peptides that are orally available

Manuel Leonardo Merz

Cyclic peptides are ring-shaped molecules that emerged as a promising class of therapeutics. While it is often difficult to find small molecule binders for challenging disease targets, cyclic peptides can bind to featureless surfaces or inhibit protein-pro ...

EPFL2022

Urinary tract infections (UTIs) are amongst the most common bacterial infections and are the second-most frequent reason for antibiotic prescriptions. Moreover, in about 25% of all treated cases, recurrence of infection occurs. Uropathogenic Escherichia co ...

EPFL2021

Carbohydrate recognition by lectins governs critical host-microbe interactions. MpPA14 (Marinomonas primoryensis PA14 domain) lectin is a domain of a 1.5-MDa adhesin responsible for a symbiotic bacterium-diatom interaction in Antarctica. Here, we show that ...

Washington2021

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Mycobacterium leprae, the causative agent of leprosy, is an unculturable bacterium with a considerably reduced genome (3.27 Mb) compared to homologues mycobacteria from the same ancestry. In 2001, the genome ofM. lepraewas first described and subsequently ...

FRONTIERS MEDIA SA2020

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The success of phage display, used for developing target-specific binders based on peptides and proteins, depends on the size and diversity of the library screened, but generating large libraries of phage-encoded polypeptides remains challenging. New pepti ...

2020

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We report the one-pot synthesis of 4-amino thiochromans using simple aminocyclopropanes and thiophenols through a formal [3+3] annulation reaction. This reaction proceeds under mild conditions with good functional group tolerance. The thiochroman core was ...

AMER CHEMICAL SOC2020