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 …

α‐Methylene‐β‐Lactone Scaffold for Developing Chemical Probes at the Two Ends of the Selectivity Spectrum

L Wang, LP Riel, B Bajrami, B Deng, AR Howell… - …, 2021 - Wiley Online Library
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 …

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 …

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 …

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 …

Molecular Fluorescent Probes for the Detection and Imaging of Sulfane Sulfur and Reactive Selenium Species

Z Wang, F Yu, Y Xing, R Wang, H Liu, Z Cheng, J Jin… - 2023 - books.rsc.org
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 …

[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 …

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 …

[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 …

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 …