The expanding repertoire of covalent warheads for drug discovery

NV Mehta, MS Degani - Drug Discovery Today, 2023 - Elsevier
The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …

Azapeptides as an Efficient Tool to Improve the Activity of Biologically Effective Peptides

K Tarchoun, M Yousef, Z Bánóczi - Future Pharmacology, 2022 - mdpi.com
Peptides are highly potent biological active compounds with excellent selectivity and
binding, but they have some drawbacks (eg, low stability in vivo because of the enzymatic …

Construction of the coexpression network involved in the pathogenesis of thyroid eye disease via bioinformatics analysis

J Hu, S Zhou, W Guo - Human Genomics, 2022 - Springer
Background Thyroid eye disease (TED) is the most common orbital pathology that occurs in
up to 50% of patients with Graves' disease. Herein, we aimed at discovering the possible …

Azapeptides-A history of synthetic milestones and key examples

K Fan Cheng, S VanPatten, M He… - Current Medicinal …, 2022 - ingentaconnect.com
For over 50 years of azapeptide synthetic techniques, developments have renewed the field
of peptidomimetic therapeutics. Azapeptides are close surrogates of natural peptides: they …

In-silico guided design, screening, and molecular dynamic simulation studies for the identification of potential SARS-CoV-2 main protease inhibitors for the targeted …

G Gutti, Y He, WH Coldren, RF Lalisse… - Journal of …, 2024 - Taylor & Francis
COVID-19, the disease responsible for the recent pandemic, is caused by a novel severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The main protease (Mpro) of …

A non-peptide-based chymotrypsin-targeted long-wavelength emission fluorescent probe with large Stokes shift and its application in bioimaging

C Fan, J Gao, Y Gao, X Yang, G Li, X Wang, F Li… - Chinese Chemical …, 2024 - Elsevier
As a hydrolase, chymotrypsin (CHT) is involved in many physiological activities, and its
abnormal activity is closely related to diabetes, pancreatic fibrosis, chronic pancreatitis and …

Solid phase submonomer azapeptide synthesis

M Bowles, C Proulx - Methods in Enzymology, 2021 - Elsevier
Azapeptides contain at least one aza-amino acid, where the α-carbon has been replaced by
a nitrogen atom, and have found broad applicability in fields ranging from medicinal …

Synthesis, structures and Hirshfeld surface analyses of 2-hydroxy-N′-methylacetohydrazide and 2-hydroxy-N-methylacetohydrazide

OV Vashchenko, DM Khomenko… - Structure …, 2024 - journals.iucr.org
The structures of the title compounds 2-hydroxy-N′-methylacetohydrazide, 1, and 2-
hydroxy-N-methylacetohydrazide, 2, both C3H8N2O2, as regioisomers differ in the position …

N-To C-Directed solid phase azapeptide synthesis

L Dif-Yaiche - 2024 - papyrus.bib.umontreal.ca
The use of peptides as therapeutic agents is a widespread strategy in the medicinal field, in
part due to pharmacological properties conferred by their three-dimensional structures …