The SARS-CoV-2 main protease as drug target

S Ullrich, C Nitsche - Bioorganic & medicinal chemistry letters, 2020 - Elsevier
The unprecedented pandemic of the severe acute respiratory syndrome coronavirus 2
(SARS-CoV-2) is threatening global health. The virus emerged in late 2019 and can cause a …

Curcumin: biological, pharmaceutical, nutraceutical, and analytical aspects

RR Kotha, DL Luthria - Molecules, 2019 - mdpi.com
Turmeric is a curry spice that originated from India, which has attracted great interest in
recent decades because it contains bioactive curcuminoids (curcumin, demethoxycurcumin …

The clinical KRAS (G12C) inhibitor AMG 510 drives anti-tumour immunity

J Canon, K Rex, AY Saiki, C Mohr, K Cooke, D Bagal… - Nature, 2019 - nature.com
KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling
protein in tumours,. The KRAS (G12C) mutant has a cysteine residue that has been …

Identification of pyrogallol as a warhead in design of covalent inhibitors for the SARS-CoV-2 3CL protease

H Su, S Yao, W Zhao, Y Zhang, J Liu, Q Shao… - Nature …, 2021 - nature.com
The ongoing pandemic of coronavirus disease 2019 (COVID-19) caused by severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2) urgently needs an effective cure. 3CL …

Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Put a ring on it: application of small aliphatic rings in medicinal chemistry

MR Bauer, P Di Fruscia, SCC Lucas… - RSC Medicinal …, 2021 - pubs.rsc.org
Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

Advances in covalent kinase inhibitors

A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Recent advances of SHP2 inhibitors in cancer therapy: current development and clinical application

X Yuan, H Bu, J Zhou, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
SHP2 (Src homology-2 domain-containing protein tyrosine phosphatase-2) is a non-
receptor protein tyrosine phosphatase that removes tyrosine phosphorylation. Functionally …

Structure-based design of targeted covalent inhibitors

R Lonsdale, RA Ward - Chemical Society Reviews, 2018 - pubs.rsc.org
Covalent inhibition is a rapidly growing discipline within drug discovery. Many historical
covalent inhibitors were discovered by serendipity, with such a mechanism of action often …

Perspectives on SARS-CoV-2 main protease inhibitors

K Gao, R Wang, J Chen, JJ Tepe… - Journal of medicinal …, 2021 - ACS Publications
The main protease (Mpro) plays a crucial role in severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) replication and is highly conserved, rendering it one of the …