Results 31 to 40 of about 5,696 (181)

Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αVβ3‐Targeted Cancer Therapy

open access: yesChemistry – A European Journal, EarlyView.
Integrin αVβ3‐targeting small‐molecule drug conjugates (SMDCs) were synthesized by conjugating a cryptophycin payload through a neutrophil elastase‐cleavable NPV‐PABC linker. RGD peptidomimetic and linker epimers served as controls for targeting and enzymatic cleavage, and the resulting conjugates displayed subnanomolar cytotoxicity in vitro.
Dominic Seißenschmidt   +3 more
wiley   +1 more source

Discovery and Biosynthesis of the Novel Glycotetrapeptide Antibiotic Biffamycin A

open access: yesAngewandte Chemie, Volume 138, Issue 26, 22 June 2026.
Genetic de‐regulation of a silent biosynthetic pathway allowed isolation and characterisation of a novel glycopeptide antibiotic named biffamycin A, which harbours unprecedented 5‐chloro‐4‐methoxy tryptophan and 3R‐hydroxy(α‐D‐mannoysl)‐D‐lysine moieties and is bioactive against MRSA and VRSA.
Michael W. Brigham   +11 more
wiley   +2 more sources

Hybrid Macrocyclic Peptides — Synthetic Strategies to Diversify and Cyclize Peptide Libraries in Phage Display Selections

open access: yesChemistry – A European Journal, EarlyView.
Hybrid macrocyclic peptides unite genetically encoded peptide libraries with the structural complexity of synthetic small molecules. This Review critically analyzes phage‐compatible cyclization and diversification chemistries, highlights emerging opportunities beyond traditional cysteine‐based approaches, and outlines how future advances may enable the
Titia Rixt Oppewal, Clemens Mayer
wiley   +1 more source

Total Synthesis and Antimicrobial Evaluation of Pagoamide A

open access: yesFrontiers in Chemistry, 2021
Natural products are often the starting point for drug development and also the testing ground for synthetic methods. Herein we describe the total synthesis and antimicrobial evaluation of a marine natural product, pagoamide A, which is a macrocyclic ...
Cheng-Han Wu, John Chu
doaj   +1 more source

Diarylethene‐Containing Photoswitchable Analogues of Tubulysins—Design, Synthesis, Biological, and Structural Evaluation

open access: yesEuropean Journal of Organic Chemistry, EarlyView.
Diarylethene‐containing cyclic tubulysin analogues were designed, synthesized, and evaluated as light‐responsive cytotoxic agents. One analogue showed reversible photoswitching, photoregulated tubulin polymerization inhibition, and photoform‐dependent cytotoxicity.
Anna Iampolska   +9 more
wiley   +1 more source

Epigenetic Dysregulation of Somatostatin Receptors (SSTR) 1–5 and Therapeutic Implications in Neuroendocrine and Non‐Neuroendocrine Malignancies

open access: yesInternational Journal of Cancer, EarlyView.
ABSTRACT Somatostatin receptors (SSTR) mediate the antiproliferative, antisecretory, and proapoptotic effects of somatostatin and its synthetic analogs. Their surface expression on neuroendocrine tumor (NET) cells is required for somatostatin analog therapy and radiopharmaceutical therapy (RPT).
Neeraj Kumari   +10 more
wiley   +1 more source

Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria

open access: yesMedicinal Research Reviews, EarlyView.
ABSTRACT Malaria is a global health threat, with an estimated 282 million cases and 610,000 malaria‐associated deaths reported in 2024. Most mortality is due to infection by Plasmodium falciparum parasites, with the highest burden occurring in Sub‐Saharan Africa.
Wisam A. Dawood   +7 more
wiley   +1 more source

Total Synthesis of the Depsipeptide FR‐901375. [PDF]

open access: yesChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Yanping, Chen   +4 more
openaire   +2 more sources

First genome sequence of a European Alternaria brassicae isolate and genes involved in early development of alternaria leaf spot on Brassica juncea

open access: yesPest Management Science, EarlyView.
This article reports the first genome sequence of a UK Alternaria brassicae isolate. Dual RNA‐sequencing profiling of A. brassicae‐infected Brassica juncea leaves identified differentially expressed genes involved in pathogenicity and host response pathways in moderately resistant Sej‐2 (2) and moderately susceptible Pusa Jaikisan cultivars.
Kevin M. King   +6 more
wiley   +1 more source

Cyclodepsipeptide Biosynthesis in Hypocreales Fungi and Sequence Divergence of The Non-Ribosomal Peptide Synthase Genes

open access: yesPathogens, 2020
Fungi from the Hypocreales order synthesize a range of toxic non-ribosomal cyclic peptides with antimicrobial, insecticidal and cytotoxic activities. Entomopathogenic Beauveria, Isaria and Cordyceps as well as phytopathogenic Fusarium spp.
Monika Urbaniak   +4 more
doaj   +1 more source

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