Irreversible inhibitors of serine, cysteine, and threonine proteases

JC Powers, JL Asgian, ÖD Ekici, KE James - Chemical reviews, 2002 - ACS Publications
Proteases or proteolytic enzymes form one of the largest and more important groups of
enzymes. Proteases selectively catalyze the hydrolysis of peptide bonds and can be divided …

Activity-based profiling of proteases

LE Sanman, M Bogyo - Annual review of biochemistry, 2014 - annualreviews.org
Proteolytic enzymes are key signaling molecules in both normal physiological processes
and various diseases. After synthesis, protease activity is tightly controlled. Consequently …

Chemical tools for endogenous protein labeling and profiling

K Shiraiwa, R Cheng, H Nonaka, T Tamura… - Cell Chemical …, 2020 - cell.com
Protein analysis under biological conditions is now regarded as indispensable for
understanding the structure and function of proteins, in addition to in vitro studies using …

Protein organic chemistry and applications for labeling and engineering in live‐cell systems

Y Takaoka, A Ojida, I Hamachi - … Chemie International Edition, 2013 - Wiley Online Library
The modification of proteins with synthetic probes is a powerful means of elucidating and
engineering the functions of proteins both in vitro and in live cells or in vivo. Herein we …

Natural products and their biological targets: proteomic and metabolomic labeling strategies

T Böttcher, M Pitscheider… - Angewandte Chemie …, 2010 - Wiley Online Library
Activity‐based protein profiling (ABPP) has matured into a standard method for the fast,
sensitive, and selective identification of enzyme activity and inhibitors in proteomes. By …

Irreversible inhibition of serine proteases-design and in vivo activity of diaryl α-Aminophosphonate derivatives

M Sienczyk, J Oleksyszyn - Current medicinal chemistry, 2009 - ingentaconnect.com
Diaryl esters of α-aminophosphonates are a group of low molecular weight inhibitors of
serine proteases. For over 30 years these molecules have captured the attention of …

Activity‐based probes for the study of proteases: recent advances and developments

S Serim, U Haedke, SHL Verhelst - ChemMedChem, 2012 - Wiley Online Library
Proteases are important targets for the treatment of human disease. Several protease
inhibitors have failed in clinical trials due to a lack of in vivo specificity, indicating the need …

Investigation of osteoclast cathepsin K activity in osteoclastogenesis and bone loss using a set of chemical reagents

T Janiszewski, S Kołt, I Ciastoń, M Vizovisek… - Cell Chemical …, 2023 - cell.com
Cathepsin K (CatK) is a lysosomal cysteine protease whose highest expression is found in
osteoclasts, which are the cells responsible for bone resorption. Investigations of the …

Recent advances in activity-based protein profiling of proteases

S Chakrabarty, JP Kahler, MAT van de Plassche… - Activity-Based Protein …, 2019 - Springer
The activity of proteases is tightly regulated, and dysregulation is linked to a variety of
human diseases. For this reason, ABPP is a well-suited method to study protease biology …

Phosphinate esters as novel warheads for activity-based probes targeting serine proteases

JP Kahler, SHL Verhelst - RSC Chemical Biology, 2021 - pubs.rsc.org
Activity-based protein profiling enables the specific detection of the active fraction of an
enzyme and is of particular use for the profiling of proteases. The technique relies on a …