A gold mine for drug discovery: Strategies to develop cyclic peptides into therapies

X Jing, K Jin - Medicinal research reviews, 2020 - Wiley Online Library
As a versatile therapeutic modality, peptides attract much attention because of their great
binding affinity, low toxicity, and the capability of targeting traditionally “undruggable” protein …

[HTML][HTML] Natural and synthetic halogenated amino acids—Structural and bioactive features in antimicrobial peptides and peptidomimetics

M Mardirossian, M Rubini, MFA Adamo, M Scocchi… - Molecules, 2021 - mdpi.com
The 3D structure and surface characteristics of proteins and peptides are crucial for
interactions with receptors or ligands and can be modified to some extent to modulate their …

[HTML][HTML] Halogenation as a tool to tune antimicrobial activity of peptoids

N Molchanova, JE Nielsen, KB Sørensen… - Scientific reports, 2020 - nature.com
Antimicrobial peptides have attracted considerable interest as potential new class of
antibiotics against multi-drug resistant bacteria. However, their therapeutic potential is …

Biomimetic engineering of the molecular recognition and self-assembly of peptides and proteins via halogenation

A Pizzi, C Pigliacelli, G Bergamaschi, A Gori… - Coordination Chemistry …, 2020 - Elsevier
Halogenation is widespread in Nature, as witnessed by the several thousands of naturally
occurring halogenated compounds. This review seeks to provide an overview on the …

[HTML][HTML] Going beyond host defence peptides: horizons of chemically engineered peptides for multidrug-resistant bacteria

B Cavallazzi Sebold, J Li, G Ni, Q Fu, H Li, X Liu… - BioDrugs, 2023 - Springer
Multidrug-resistant (MDR) bacteria are considered a health threat worldwide, and this
problem is set to increase over the decades. The ESKAPE, a group of six pathogens …

[HTML][HTML] Investigation of tetrasubstituted heterocycles reveals hydantoins as a promising scaffold for development of novel antimicrobials with membranolytic …

MK Langer, A Rahman, H Dey, T Anderssen… - European Journal of …, 2023 - Elsevier
Mimics of antimicrobial peptides (AMPs) have been proposed as a promising class of
antimicrobial agents. We report the analysis of five tetrasubstituted, cationic, amphipathic …

[HTML][HTML] A concise SAR-analysis of antimicrobial cationic amphipathic barbiturates for an improved activity-toxicity profile

MK Langer, A Rahman, H Dey, T Anderssen… - European Journal of …, 2022 - Elsevier
An amphipathic barbiturate mimic of the marine eusynstyelamides is reported as a
promising class of antimicrobial agents. We hereby report a detailed analysis of the structure …

Bioactivity profiling and mode of action studies of antibacterial and antibiofilm agents of marine origin

A Rahman - 2024 - munin.uit.no
The emergence of drug-resistant strains and new pathogens intensifies the need for new
antimicrobials. Additionally, bacterial biofilms, which contribute to persistent infections …

Synthesis and structure-activity relationship studies of marine-derived antimicrobial peptides and small cyclic peptidomimetics

D Simonovic - 2023 - munin.uit.no
Effective antimicrobial drugs are the very core of modern medicine enabling successful
prevention and treatment of infectious diseases. However, systemic misuse and overuse of …

Halogenated antimicrobial peptoids

N Molchanova, A Barron, H Jenssen - US Patent App. 17/606,761, 2022 - Google Patents
(2) Date: Oct. 27, 2021 Related US Application Data (60) Provisional application No.
62/841,227, filed on Apr. 30, 2019. is provided, wherein A is a terminal N-alkyl substituted …