[图书][B] The design of covalent-based inhibitors
RA Ward, N Grimster - 2021 - books.google.com
Annual Report on Medicinal Chemistry series, highlights new advances in the field with this
new volume presenting interesting chapters. Each chapter is written by an international …
new volume presenting interesting chapters. Each chapter is written by an international …
Drug discovery considerations in the development of covalent inhibitors
In recent years, the number of drug candidates with a covalent mechanism of action
progressing through clinical trials or being approved by the FDA has increased significantly …
progressing through clinical trials or being approved by the FDA has increased significantly …
Recent advances in the development of covalent inhibitors
The use of covalent inhibitors in the field of drug discovery has attracted considerable
attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market …
attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market …
Covalent inhibitors: a rational approach to drug discovery
F Sutanto, M Konstantinidou, A Dömling - RSC medicinal chemistry, 2020 - pubs.rsc.org
Covalent inhibitors are recognized as an important component in drug discovery and
therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the …
therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the …
Covalent inhibitors: back on track?
M Gehringer - Future Medicinal Chemistry, 2020 - Taylor & Francis
Covalent drugs have a long history and such medicines are used for diverse therapeutic
indications. Prominent blockbuster drugs relying on covalent target engagement include …
indications. Prominent blockbuster drugs relying on covalent target engagement include …
Targeted covalent inhibitors for novel therapeutics
J Zhang, W Gao, Y Wang, J Chang… - Future Medicinal …, 2023 - Taylor & Francis
Targeted covalent inhibitors (TCIs) are a class of small-molecule compounds that can
covalently bind to conserved amino acids of specific target proteins, thereby inhibiting their …
covalently bind to conserved amino acids of specific target proteins, thereby inhibiting their …
The resurgence of covalent drugs
J Singh, RC Petter, TA Baillie, A Whitty - Nature reviews Drug discovery, 2011 - nature.com
Covalent drugs haveproved to be successful therapies for various indications, but largely
owing to safety concerns, they are rarely considered when initiating a target-directed drug …
owing to safety concerns, they are rarely considered when initiating a target-directed drug …
10 years into the resurgence of covalent drugs
E De Vita - Future Medicinal Chemistry, 2021 - Taylor & Francis
In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …
previous trend that had impeded the use of covalent inhibition in drug development …
1.2 Designing Covalent Inhibitors: A Medicinal Chemistry Challenge
F Lopes, MMM Santos, R Moreira - Biomedical Chemistry, Sciendo …, 2015 - degruyter.com
The design of enzyme inhibitors is one of the most attractive research topics in Medicinal
Chemistry. In particular, covalent inhibitors provide the opportunity of combining concepts of …
Chemistry. In particular, covalent inhibitors provide the opportunity of combining concepts of …
Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies
RA Bauer - Drug discovery today, 2015 - Elsevier
Highlights•High potencies and prolonged effects achievable with covalent drugs may result
in less frequent dosing and improved therapeutic margins for patients.•Covalent inhibition …
in less frequent dosing and improved therapeutic margins for patients.•Covalent inhibition …