Identification of Covalent Ligands–from Single Targets to Whole Proteome
C Ngo, A Ekanayake, C Zhang - Israel Journal of Chemistry, 2023 - Wiley Online Library
There has been a surge of interest and efforts in the discovery of covalent ligands for diverse
proteins as tool compounds or therapeutic candidates in recent years. We present two …
proteins as tool compounds or therapeutic candidates in recent years. We present two …
α‐Methylene‐β‐Lactone Scaffold for Developing Chemical Probes at the Two Ends of the Selectivity Spectrum
The utilities of an α‐methylene‐β‐lactone (MeLac) moiety as a warhead composed of
multiple electrophilic sites are reported. We demonstrate that a MeLac‐alkyne not only …
multiple electrophilic sites are reported. We demonstrate that a MeLac‐alkyne not only …
Kinetic principles of chemical cross-link formation for protein-protein interactions
KM Kammer, R Pellarin, F Stengel - bioRxiv, 2024 - biorxiv.org
Proteins play a central role in most biological processes within the cell and deciphering how
they interact is key to understand their function. Cross-linking coupled to mass spectrometry …
they interact is key to understand their function. Cross-linking coupled to mass spectrometry …
Light-induced efficient and residue-selective bioconjugation of native proteins via indazolone formation
AD Guo, KH Wu, XH Chen - RSC advances, 2021 - pubs.rsc.org
Chemical modification of proteins has emerged as a powerful tool to realize enormous
applications, such as development of novel biologics and functional studies of individual …
applications, such as development of novel biologics and functional studies of individual …
Global Assessment of Drug Target Engagement and Selectivity of Covalent Cysteine-Reactive Inhibitors Using Alkyne-Functionalized Probes
EM Rothweiler, KVM Huber - Chemogenomics: Methods and Protocols, 2023 - Springer
Covalent inhibitors are emerging as a promising therapeutic means for efficient and
sustained targeting of key disease-driving proteins. As for classic non-covalent inhibitors …
sustained targeting of key disease-driving proteins. As for classic non-covalent inhibitors …
Molecular Fluorescent Probes for the Detection and Imaging of Sulfane Sulfur and Reactive Selenium Species
Since the concept of oxidative stress was added to the field of redox biology and medicine in
1985, 1 the issues of oxidative stress have been evolving in physiology and …
1985, 1 the issues of oxidative stress have been evolving in physiology and …
[图书][B] Chemoproteomic Strategies for Drug Discovery and Natural Product Target Identification
BP Belcher - 2023 - search.proquest.com
Targeted protein therapeutics have garnered significant interest in modern drug discovery,
in part due to their ability to target classically “undruggable” proteins.“Undruggable” proteins …
in part due to their ability to target classically “undruggable” proteins.“Undruggable” proteins …
Atomistic simulations of the amine acetylation reaction and the covalent inhibition of the enzyme Phosphoinositide 3-kinase (PI3K)
V Fındık - 2022 - search.proquest.com
Yeni ilaç arayışı için, hedeflendirilmiş kovalent inhibitörler büyük umut vaadeder. Geleneksel
tersinir inhibitörlere göre, genişletilmiş alıkonma süresi ve arttırılmış potansiyele sahip …
tersinir inhibitörlere göre, genişletilmiş alıkonma süresi ve arttırılmış potansiyele sahip …
[图书][B] Chemoproteomics-enabled Discovery of Covalent Inhibitors and Novel Induced Proximity Platforms
L Boike - 2022 - search.proquest.com
Covalent drugs incorporate a mildly electrophilic functional group that reacts with protein
targets to confer additional affinity beyond the non-covalent interactions involved in drug …
targets to confer additional affinity beyond the non-covalent interactions involved in drug …
Protein-film-mediated strategies for the electrochemical immunosensing of circulating biomarkers
FM Fleschhut - 2024 - ora.ox.ac.uk
The electrochemical quantification of protein biomarkers from complex samples such as
human serum promises vast potential for the solution of future healthcare challenges …
human serum promises vast potential for the solution of future healthcare challenges …