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 Protein Profiling: Applications to Biomarker Discovery, In Vivo Imaging and Drug Discovery

AB Berger, PM Vitorino, M Bogyo - American Journal of …, 2004 - Springer
The genomic revolution has created a wealth of information regarding the fundamental
genetic code that defines the inner workings of a cell. However, it has become clear that …

The membrane-anchored serine protease, TMPRSS2, activates PAR-2 in prostate cancer cells

S Wilson, B Greer, J Hooper, A Zijlstra… - Biochemical …, 2005 - portlandpress.com
TMPRSS2 is a type II transmembrane-bound serine protease that has gained interest owing
to its highly localized expression in the prostate and its overexpression in neoplastic …

Activity based probes for proteases: applications to biomarker discovery, molecular imaging and drug screening

M Fonovic, M Bogyo - Current pharmaceutical design, 2007 - ingentaconnect.com
Recent advances in global genomic and proteomic methods have lead to a greater
understanding of how genes and proteins function in complex networks within a cell. One of …

Mucosal allergic sensitization to cockroach allergens is dependent on proteinase activity and proteinase-activated receptor-2 activation

NG Arizmendi, M Abel, K Mihara… - The Journal of …, 2011 - journals.aai.org
We have shown that proteinase-activated receptor-2 (PAR 2) activation in the airways leads
to allergic sensitization to concomitantly inhaled Ags, thus implicating PAR 2 in the …

Kallikrein-related peptidases: proteolysis and signaling in cancer, the new frontier

K Oikonomopoulou, EP Diamandis, MD Hollenberg - 2010 - degruyter.com
The exact mechanism (s) by which kallikrein-related peptidases (KLKs) function, their levels
of activity and their potential endogenous targets in vivo have only recently begun to be …

Development of activity-based probes for trypsin-family serine proteases

Z Pan, DA Jeffery, K Chehade, J Beltman… - Bioorganic & medicinal …, 2006 - Elsevier
A series of diphenylphosphonate-based probes were developed for the trypsin-like serine
proteases. These probes selectively target serine proteases rather than general serine …

[HTML][HTML] Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases

A Ramos-Llorca, L Decraecker, VMY Cacheux… - Frontiers in …, 2023 - frontiersin.org
Activity-based probes (ABP) are molecules that bind covalently to the active form of an
enzyme family, making them an attractive tool for target and biomarker identification and …

Discovery and evaluation of new activity‐based probes for serine hydrolases

C Wang, D Abegg, BG Dwyer, A Adibekian - ChemBioChem, 2019 - Wiley Online Library
Serine hydrolases play crucial biological roles and are important therapeutic targets in many
clinical applications. Activity‐based protein profiling of serine hydrolases by using …

Interfering with host proteases in SARS-CoV-2 entry as a promising therapeutic strategy

P Müller, H Maus, SJ Hammerschmidt… - Current Medicinal …, 2022 - ingentaconnect.com
Due to its fast international spread and substantial mortality, the coronavirus disease COVID-
19 evolved to a global threat. Since there is currently no causative drug against this viral …