Irreversible inhibitors of serine, cysteine, and threonine proteases
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 …
enzymes. Proteases selectively catalyze the hydrolysis of peptide bonds and can be divided …
Activity-based profiling of proteases
Proteolytic enzymes are key signaling molecules in both normal physiological processes
and various diseases. After synthesis, protease activity is tightly controlled. Consequently …
and various diseases. After synthesis, protease activity is tightly controlled. Consequently …
Chemical tools for endogenous protein labeling and profiling
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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
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 …
enzyme and is of particular use for the profiling of proteases. The technique relies on a …