[HTML][HTML] Therapeutic strategies for COVID-19: progress and lessons learned

G Li, R Hilgenfeld, R Whitley, E De Clercq - Nature Reviews Drug …, 2023 - nature.com
Abstract The coronavirus disease 2019 (COVID-19) pandemic has stimulated tremendous
efforts to develop therapeutic strategies that target severe acute respiratory syndrome …

Expanding chemical probe space: quality criteria for covalent and degrader probes

IV Hartung, J Rudolph, MM Mader… - Journal of Medicinal …, 2023 - ACS Publications
Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

[HTML][HTML] Structure-based development and preclinical evaluation of the SARS-CoV-2 3C-like protease inhibitor simnotrelvir

X Jiang, H Su, W Shang, F Zhou, Y Zhang… - Nature …, 2023 - nature.com
The persistent pandemic of coronavirus disease 2019 (COVID-19) caused by severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2) and its variants accentuates the great …

[HTML][HTML] Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - … and Targeted Therapy, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

An analysis of successful hit-to-clinical candidate pairs

DG Brown - Journal of medicinal chemistry, 2023 - ACS Publications
An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Reversible dual-covalent molecular locking of the 14-3-3/ERRγ protein–protein interaction as a molecular glue drug discovery approach

BA Somsen, RJC Schellekens… - Journal of the …, 2023 - ACS Publications
Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool
compounds for biophysics and (structural) biology, and as starting points for molecular glue …

The local vibrational mode theory and its place in the vibrational spectroscopy arena

E Kraka, M Quintano, HW La Force… - The Journal of …, 2022 - ACS Publications
This Feature Article starts highlighting some recent experimental and theoretical advances
in the field of IR and Raman spectroscopy, giving a taste of the breadth and dynamics of this …

Thiomethyltetrazines Are Reversible Covalent Cysteine Warheads Whose Dynamic Behavior can be “Switched Off” via Bioorthogonal Chemistry Inside Live Cells

AM Tallon, Y Xu, GM West, CW Am Ende… - Journal of the American …, 2023 - ACS Publications
Electrophilic small molecules that can reversibly modify proteins are of growing interest in
drug discovery. However, the ability to study reversible covalent probes in live cells can be …

Targeting the estrogen receptor for the treatment of breast cancer: recent advances and challenges

RK Rej, JE Thomas, RK Acharyya… - Journal of Medicinal …, 2023 - ACS Publications
Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of
ER-positive (ER+) breast cancers. Despite the tremendous successes achieved with …