New Cysteine Covalent Modification Strategies Enable Advancement of Proteome‐wide Selectivity of Kinase Modulators
I Guan, K Williams, J Pan, X Liu - Asian Journal of Organic …, 2021 - Wiley Online Library
There has been tremendous progress in covalent inhibitors as evidenced by the ascent of
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …
Beyond cysteine: recent developments in the area of targeted covalent inhibition
H Mukherjee, NP Grimster - Current opinion in chemical biology, 2018 - Elsevier
Over the past decade targeted covalent inhibitors have undergone a renaissance due to the
clinical validation and regulatory approval of several small molecule therapeutics that are …
clinical validation and regulatory approval of several small molecule therapeutics that are …
Recent progress in covalent warheads for in vivo targeting of endogenous proteins
N Shindo, A Ojida - Bioorganic & Medicinal Chemistry, 2021 - Elsevier
Covalent drugs exert potent and durable activity by chemical modification of the
endogenous target protein in vivo. To maximize the pharmacological efficacy while …
endogenous target protein in vivo. To maximize the pharmacological efficacy while …
Covalent kinase inhibitors: An overview
M Gehringer - Proteinkinase Inhibitors, 2021 - Springer
Covalent targeting has experienced a revival in the last decade, especially in the area of
protein kinase inhibitor development. Generally, covalent inhibitors make use of an …
protein kinase inhibitor development. Generally, covalent inhibitors make use of an …
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 …
discovery. Covalency affords a unique set of advantages as well as challenges relative to …
Covalent inhibitors: an opportunity for rational target selectivity
R Lagoutte, R Patouret, N Winssinger - Current opinion in chemical biology, 2017 - Elsevier
There is a resurging interest in compounds that engage their target through covalent
interactions. Cysteine's thiol is endowed with enhanced reactivity, making it the nucleophile …
interactions. Cysteine's thiol is endowed with enhanced reactivity, making it the nucleophile …
A road map for prioritizing warheads for cysteine targeting covalent inhibitors
Targeted covalent inhibitors have become an integral part of a number of therapeutic
protocols and are the subject of intense research. The mechanism of action of these …
protocols and are the subject of intense research. The mechanism of action of these …
Catalyst-free late-stage functionalization to assemble α-acyloxyenamide electrophiles for selectively profiling conserved lysine residues
Y Zhao, K Duan, Y Fan, S Li, L Huang, Z Tu… - Communications …, 2024 - nature.com
Covalent probes coupled with chemical proteomics represent a powerful method for
investigating small molecule and protein interactions. However, the creation of a reactive …
investigating small molecule and protein interactions. However, the creation of a reactive …
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update
L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …
decades, with a variety of new targeted covalent drugs having been approved in recent …
Never gonna give you up–current developments in covalent protein kinase inhibitors
L Hillebrand, M Gehringer - Chimia, 2022 - chimia.ch
Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors
addressing non-catalytic cysteine residues with weakly reactive electrophiles have been …
addressing non-catalytic cysteine residues with weakly reactive electrophiles have been …