Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets

K Colas, D Bindl, H Suga - Chemical Reviews, 2024 - ACS Publications
Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …

Thioamides in medicinal chemistry and as small molecule therapeutic agents

G Huang, T Cierpicki, J Grembecka - European Journal of Medicinal …, 2024 - Elsevier
Thioamides, which are fascinating isosteres of amides, have garnered significant attention in
drug discovery and medicinal chemistry programs, spanning peptides and small molecule …

CycPeptMP: enhancing membrane permeability prediction of cyclic peptides with multi-level molecular features and data augmentation

J Li, K Yanagisawa, Y Akiyama - Briefings in Bioinformatics, 2024 - academic.oup.com
Cyclic peptides are versatile therapeutic agents that boast high binding affinity, minimal
toxicity, and the potential to engage challenging protein targets. However, the …

Peptide and peptidomimetic inhibitors targeting the interaction of collapsin response mediator protein 2 with the N-type calcium channel for pain relief

S Perez-Miller, K Gomez, R Khanna - ACS Pharmacology & …, 2024 - ACS Publications
Ion channels serve pleiotropic functions. Often found in complexes, their activities and
functions are sculpted by auxiliary proteins. We discovered that collapsin response mediator …

De Novo Discovery of a Noncovalent Cell-Penetrating Bicyclic Peptide Inhibitor Targeting SARS-CoV-2 Main Protease

Y Tan, J Yang, M Wang, Q Peng, Y Li, L Fu… - Journal of Medicinal …, 2024 - ACS Publications
Macrocyclic peptides have garnered significant attention as promising drug candidates.
However, they typically face challenges in achieving and enhancing cell permeability for …

Influence of Aza-Glycine substitution on the internalization of penetratin

K Tarchoun, D Soltész, V Farkas, HJ Lee, I Szabó… - Pharmaceutics, 2024 - mdpi.com
The cell-penetrating peptide (CPP) penetratin has gained much attention over many years
due to its potential role as a transporter for a broad range of cargo into cells. The …

Novel Flurbiprofen Derivatives as Antioxidant and Anti-Inflammatory Agents: Synthesis, In Silico, and In Vitro Biological Evaluation

I Ivanov, S Manolov, D Bojilov, G Marc, D Dimitrova… - Molecules, 2024 - mdpi.com
In this study, we present the synthesis of five novel compounds by combining flurbiprofen
with various substituted 2-phenethylamines. The synthesized derivatives underwent …

An Insight into the Pharmacology of Sulphur Containing Peptide Drugs

A Sharma, LR Singh - European Journal of Medicinal Chemistry, 2024 - Elsevier
Since last century, peptides have emerged as potential drugs with> 90 FDA approvals for
various targets with several in the pipeline. Sulphur, in peptides is present either as thiol …

Expanding the Scope of Ribosome‐Mediated Biosynthesis in vitro using tRNA‐Aminoacylating Ribozyme

N Cho, H Jin, H Jeon, K Lee… - Israel Journal of Chemistry, 2024 - Wiley Online Library
Proteins are synthesized within ribosomes through the polymerization of amino acids (AAs).
This process requires prior activation of AAs through aminoacylation that attaches them to …

Thioimidate solutions to thioamide problems during thionopeptide deprotection

J Byerly-Duke, B VanVeller - Organic letters, 2024 - ACS Publications
Thioamides have structural and chemical similarity to peptide bonds, offering valuable
insights when probing peptide backbone interactions, but are prone to side reactions during …