Article

A novel cell-based sensor detecting the activity of individual basic proprotein convertases

2018-11-06

Abstract excerpt

<h4>ABSTRACT</h4> The basic proprotein convertases (PCs) furin, PC1/3, PC2, PC5/6, PACE4, PC4, and PC7 are promising drug targets for human diseases. However, developing selective inhibitors remains challenging due to overlapping substrate recognition motifs and limited structural information. Classical drug screening approaches for basic PC inhibitors involve homogeneous biochemical assays using soluble recombin...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: ee52601b-84f8-5598-9b40-cc73761847d8
DOI: 10.1101/464032

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

A novel cell-based sensor detecting the activity of individual basic proprotein convertasesDOI 10.1101/464032Read

Curbing activation: proprotein convertases in homeostasis and pathologySemantic proximity Read

Solid-Phase Synthesis of ProTide Fluorogenic Probes Enables Systematic Profiling of Carboxypeptidase ActivitySemantic proximity Read

High-throughput Activity Reprogramming of Proteases (HARP)Semantic proximity Read

Comparative study of the binding pockets of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors.Semantic proximity Read

Programming cell behavior with synthetic protease-activated receptorsSemantic proximity Read

Single amino acid substitution in the PC1/3 propeptide can induce significant modifications of its inhibitory profile toward its cognate enzyme.Semantic proximity Read

Enzyme activity as an actionable axis for small-molecule precision oncologySemantic proximity Read

Orthogonal dual reporter-based gain-of-signal assay for probing SARS-CoV-2 3CL protease activity in living cells: inhibitor identification and mutation investigation.Semantic proximity Read

Characterization of missense mutations in the signal peptide and propeptide of FIX in hemophilia B by a cell-based assaySemantic proximity Read

Near-Infrared Fluorescent Probes for the Detection of Cancer-Associated ProteasesSemantic proximity Read

Massively parallel, computationally-guided design of a pro-enzymeSemantic proximity Read

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9Semantic proximity Read