Fluorogenic probes for disease-relevant enzymes

J Zhang, X Chai, XP He, HJ Kim, J Yoon… - Chemical Society …, 2019 - pubs.rsc.org
Traditional biochemical methods for enzyme detection are mainly based on antibody-based
immunoassays, which lack the ability to monitor the spatiotemporal distribution and, in …

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

MD Hall, A Yasgar, T Peryea, JC Braisted… - … and applications in …, 2016 - iopscience.iop.org
The sensitivity of fluorescence polarization (FP) and fluorescence anisotropy (FA) to
molecular weight changes has enabled the interrogation of diverse biological mechanisms …

Fluorescence anisotropy (polarization): from drug screening to precision medicine

H Zhang, Q Wu, MY Berezin - Expert opinion on drug discovery, 2015 - Taylor & Francis
Introduction: Fluorescence anisotropy (FA) is one of the major established methods
accepted by industry and regulatory agencies for understanding the mechanisms of drug …

Caspase selective reagents for diagnosing apoptotic mechanisms

M Poreba, K Groborz, M Navarro, SJ Snipas… - Cell Death & …, 2019 - nature.com
Apical caspases initiate and effector caspases execute apoptosis. Reagents that can
distinguish between caspases, particularly apical caspases-8, 9, and 10 are scarce and …

Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities

HS Roth, PJ Hergenrother - Current medicinal chemistry, 2016 - ingentaconnect.com
PAC-1 induces the activation of procaspase-3 in vitro and in cell culture by chelation of
inhibitory labile zinc ions via its ortho-hydroxy-N-acylhydrazone moiety. First reported in …

Turning on caspases with genetics and small molecules

CW Morgan, O Julien, EK Unger, NM Shah… - Methods in …, 2014 - Elsevier
Caspases, aspartate-specific cysteine proteases, have fate-determining roles in many
cellular processes including apoptosis, differentiation, neuronal remodeling, and …

New alkoxy flavone derivatives targeting caspases: Synthesis and antitumor activity evaluation

J Moreira, D Ribeiro, PMA Silva, N Nazareth… - Molecules, 2018 - mdpi.com
The antitumor activity of natural flavonoids has been exhaustively reported. Previously it has
been demonstrated that prenylation of flavonoids allows the discovery of new compounds …

Discovery of a highly selective caspase-3 substrate for imaging live cells

CJ Vickers, GE González-Páez… - ACS Chemical Biology, 2014 - ACS Publications
Caspases are a family of cysteine proteases that are well-known for their roles in apoptosis
and inflammation. Recent studies provide evidence that caspases are also integral to many …

Removal of metabolic liabilities enables development of derivatives of procaspase-activating compound 1 (PAC-1) with improved pharmacokinetics

HS Roth, RC Botham, SC Schmid, TM Fan… - Journal of medicinal …, 2015 - ACS Publications
Procaspase-activating compound 1 (PAC-1) is an o-hydroxy-N-acylhydrazone that induces
apoptosis in cancer cells by chelation of labile inhibitory zinc from procaspase-3. PAC-1 has …

Fluorescence-Polarization-Based Assaying of Lysozyme with Chitooligosaccharide Tracers

LI Mukhametova, DO Zherdev, AN Kuznetsov… - Biomolecules, 2024 - mdpi.com
Lysozyme is a well-known enzyme found in many biological fluids which plays an important
role in the antibacterial protection of humans and animals. Lysozyme assays are used for …