4-(Dimethylamino)pyridine N-Oxide-Catalyzed Macrolactamization Using 2-Methyl-6-nitrobenzoic Anhydride in the Synthesis of the Depsipeptidic Analogue of FE399 [PDF]
Takayuki Tonoi +2 more
exaly +3 more sources
Synthetic Studies Towards Darobactin A. [PDF]
The urgent need for new antibiotics led us to develop a new methodology for the synthesis of the natural product darobactin A selectively targeting gram‐negative bacteria. This study provides new insights into the synthesis of strained indole‐containing macrocycles.
Steiner T +4 more
europepmc +2 more sources
Synthesis of a Conformationally Fixed Bicyclomarin Derivative. [PDF]
The synthesis of a new bicyclic derivative of cyclomarin is described. Cyclomarin is a marine cyclopeptide with excellent antituberculosis activity. The synthesis of the linear heptapeptide and the two macrolactamizations proceed smoothly. Based on an X‐ray structure of cyclomarin bound to ClpC1, a new conformationally fixed, bicyclic cyclomarin ...
Greve J, Kiefer AF, Kazmaier U.
europepmc +2 more sources
Leader peptide removal in lasso peptide biosynthesis based on penultimate isoleucine residue [PDF]
Lasso peptides are ribosomally synthesized peptides that undergo post-translational modifications including leader peptide removal by B (or the segregated B1 and B2) proteins and core peptide macrolactamization by C proteins to form a unique lariat ...
Yuwei Duan +11 more
doaj +2 more sources
A Short Synthesis of Cyclo(‐RGDfK) Using a Microflow Reactor
Cyclic RGD‐containing peptides are highly potent and useful as selective inhibitors of the αvβ3 integrin. Their derivatives have been utilized as the integrin‐targeted radiotracers for molecular imaging and therapeutic applications.
Naoto Yamasaki +6 more
doaj +2 more sources
Chemical Ligation of Backbone N-hydroxylated Peptides. [PDF]
Peptide backbone N‐hydroxylation enables sequence‐agnostic fragment ligation via hydroxamate O‐acyl capture and O→N acyl transfer in water. Broad tolerance of sterically demanding nucleophilic residues is observed, and reductive N─O cleavage restores the native amide bond.
Cano-Sampaio N, Del Valle JR.
europepmc +2 more sources
Concise Total Syntheses of Leuconoxine-Type Alkaloids Enabled by Palladium/Norbornene-Catalyzed Pyrrole Difunctionalization. [PDF]
Concise total syntheses of five leuconoxine alkaloids have been achieved using a pyrrole‐centered strategy, which features a newly developed palladium/norbornene‐catalyzed pyrrole double C─H functionalization method, a divergent late‐stage oxidative dearomatization tactic, and no use of protecting groups.
Liu X +5 more
europepmc +3 more sources
Therapeutic Potential of Stylissatin A and Related Cyclic Peptides From Marine Sponges. [PDF]
Synthesis and biologicals activities of the natural cyclic peptide stylissatin A and its various analogues arereported. The findings suggest that specific amino acid residues such as Ile at position 2, Pro at 4 and 6, and Tyr at position 1 are key contributors to the peptide's therapeutic potential.
Ullah A +4 more
europepmc +2 more sources
Cyclization by Intramolecular Suzuki-Miyaura Cross-Coupling-A Review. [PDF]
The application of the Suzuki‐Miyaura cross‐coupling as the ring‐forming step in the synthesis of natural products/natural product analogs and synthetic bioactive molecules is reviewed. The reaction has been successfully employed for ring construction across a wide range of ring sizes (from 4 to ≫12) in a stereoselective fashion.
Caso C, Altmann KH.
europepmc +2 more sources
Discovery and Heterologous Expression of Trilenodin, an Antimicrobial Lasso Peptide with a Unique Tri-Isoleucine Motif. [PDF]
A new antimicrobial lasso peptide, trilenodin, was bioinformatically identified, isolated, and characterized from Firmicutes bacterium Paenibacillus taiwanensis DSM18679. We connected production of trilenodin to its biosynthetic gene cluster by establishing a Firmicutes‐based lasso peptide heterologous expression system and report trilenodin as the ...
Pulliam C +4 more
europepmc +2 more sources

