The multifaceted nature of antimicrobial peptides: Current synthetic chemistry approaches and future directions

BH Gan, J Gaynord, SM Rowe, T Deingruber… - Chemical Society …, 2021 - pubs.rsc.org
Bacterial infections caused by 'superbugs' are increasing globally, and conventional
antibiotics are becoming less effective against these bacteria, such that we risk entering a …

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 …

Peptide chemistry toolbox–Transforming natural peptides into peptide therapeutics

M Erak, K Bellmann-Sickert, S Els-Heindl… - Bioorganic & medicinal …, 2018 - Elsevier
The development of solid phase peptide synthesis has released tremendous opportunities
for using synthetic peptides in medicinal applications. In the last decades, peptide …

Disulfide-directed multicyclic peptide libraries for the discovery of peptide ligands and drugs

S Lu, S Fan, S Xiao, J Li, S Zhang, Y Wu… - Journal of the …, 2023 - ACS Publications
Multicyclic peptides with stable 3D structures are a kind of novel and promising peptide
formats for drug design and discovery as they have the potential to combine the best …

Cys–Cys and Cys–Lys stapling of unprotected peptides enabled by hypervalent iodine reagents

J Ceballos, E Grinhagena, G Sangouard… - Angewandte …, 2021 - Wiley Online Library
Easy access to a wide range of structurally diverse stapled peptides is crucial for the
development of inhibitors of protein‐protein interactions. Herein, we report bis‐functional …

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 …

Designing formulation strategies for enhanced stability of therapeutic peptides in aqueous solutions: A review

PP Nugrahadi, WLJ Hinrichs, HW Frijlink, C Schöneich… - Pharmaceutics, 2023 - mdpi.com
Over the past few decades, there has been a tremendous increase in the utilization of
therapeutic peptides. Therapeutic peptides are usually administered via the parenteral …

Designing chimeric molecules for drug discovery by leveraging chemical biology

C Borsari, DJ Trader, A Tait… - Journal of medicinal …, 2020 - ACS Publications
After the first seed concept introduced in the 18th century, different disciplines have
attributed different names to dual-functional molecules depending on their application …

Oxetane Grafts Installed Site‐Selectively on Native Disulfides to Enhance Protein Stability and Activity In Vivo

N Martínez‐Sáez, S Sun, D Oldrini… - Angewandte Chemie …, 2017 - Wiley Online Library
A four‐membered oxygen ring (oxetane) can be readily grafted into native peptides and
proteins through site‐selective bis‐alkylation of cysteine residues present as disulfides …

Co-crystal structures of HIV TAR RNA bound to lab-evolved proteins show key roles for arginine relevant to the design of cyclic peptide TAR inhibitors

SS Chavali, SM Mali, JL Jenkins, R Fasan… - Journal of Biological …, 2020 - ASBMB
RNA-protein interfaces control key replication events during the HIV-1 life cycle. The viral
trans-activator of transcription (Tat) protein uses an archetypal arginine-rich motif (ARM) to …