Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Conotoxins: chemistry and biology

AH Jin, M Muttenthaler, S Dutertre, SWA Himaya… - Chemical …, 2019 - ACS Publications
The venom of the marine predatory cone snails (genus Conus) has evolved for prey capture
and defense, providing the basis for survival and rapid diversification of the now estimated …

The chemical synthesis of insulin: an enduring challenge

JA Karas, JD Wade, MA Hossain - Chemical reviews, 2021 - ACS Publications
The pancreatic peptide hormone insulin, first discovered exactly 100 years ago, is essential
for glycemic control and is used as a therapeutic for the treatment of type 1 and, increasingly …

Heteroaryl rings in peptide macrocycles

IV Smolyar, AK Yudin, VG Nenajdenko - Chemical reviews, 2019 - ACS Publications
This Review is devoted to the chemistry of macrocyclic peptides having heterocyclic
fragments in their structure. These motifs are present in many natural products and synthetic …

Butelase‐Mediated Macrocyclization of d‐Amino‐Acid‐Containing Peptides

GKT Nguyen, X Hemu, JP Quek… - Angewandte Chemie, 2016 - Wiley Online Library
Macrocyclic compounds have received increasing attention in recent years. With their large
surface area, they hold promise for inhibiting protein–protein interactions, a chemical space …

Cytotoxic and antitumor peptides as novel chemotherapeutics

X Luan, Y Wu, YW Shen, H Zhang, YD Zhou… - Natural product …, 2021 - pubs.rsc.org
Covering: up to 2020 Treatment resistance and drug-induced refractory malignancies pose
significant challenges for current chemotherapy drugs. There have been increasing …

Structure-Based Design and Synthesis of Stapled 10Panx1 Analogues for Use in Cardiovascular Inflammatory Diseases

A Lamouroux, M Tournier, D Iaculli… - Journal of medicinal …, 2023 - ACS Publications
Following a rational design, a series of macrocyclic (“stapled”) peptidomimetics of 10Panx1,
the most established peptide inhibitor of Pannexin1 (Panx1) channels, were developed and …

Pd(II)-Catalyzed β-C(sp3)-H Alkynylation of Alanine in Di- and Tripeptides with Asn as an Endogenous Directing Group

XX Ding, BQ Ren, BT Li, ZJ Pang, YJ Xu… - The Journal of Organic …, 2024 - ACS Publications
The introduction of alkyne moieties into peptides remains in demand as it represents a
promising approach for further structural diversification of peptides. Herein, we describe the …

α-Conotoxin peptidomimetics: probing the minimal binding motif for effective analgesia

AC Kennedy, A Belgi, BW Husselbee, D Spanswick… - Toxins, 2020 - mdpi.com
Several analgesic α-conotoxins have been isolated from marine cone snails. Structural
modification of native peptides has provided potent and selective analogues for two of its …

Enhancing the therapeutic potential of peptide toxins

RS Norton - Expert Opinion on Drug Discovery, 2017 - Taylor & Francis
Introduction: Peptide toxins are potent and often exquisitely selective probes of the structure
and function of ion channels and receptors, and as such are of significant interest to the …