A Multifunctional Protease Inhibitor To Regulate Endolysosomal Function

A Multifunctional Protease Inhibitor To Regulate Endolysosomal Function

Proteases constitute a major class of drug targets. Endosomal compartments harbor several protease families whose attenuation may be beneficial to a number of biological processes, including inflammation, cancer metastasis, antigen presentation, and parasite clearance. As a step toward the goal of generalized but targeted protease inhibition in the endocytic pathway, we describe here the synthe...

A protease inhibitor unsticks cells

A protease inhibitor unsticks cells AI-1 is unique among protease inhibitors because it binds to the matrix protein vitronectin (VN). PAI-1 binding blocks VN's binding site for the cell surface receptor uPAR and for integrin family members. Czekay et al. (page 781) now show that PAI-1 is also able to detach cells through a less direct approach. Unlike the direct competition method, PAI-1 also d...

Effect of Biomolecular Conformation on Docking Simulation: A Case Study on a Potent HIV-1 Protease Inhibitor

Human immunodeficiency virus infection / acquired immunodeficiency syndrome (HIV/AIDS) is a disease pertained to the human immune system. Given its crucial role in viral replication, HIV-1 protease (HIV-1 PR) is a prime therapeutic target in AIDS therapy. In this regard, the dynamic aspects of ligand-enzyme interactions may indicate an important role of conformational variability in HIV-1 PR in...

HIV Protease Inhibitor : Past

C1 inhibitor, a multi-functional serine protease inhibitor.

C1 inhibitor (C1INH) is a serpin that regulates both complement and contact (kallikrein-kinin) system activation. It consists of a serpin domain that is highly homologous to other serpins and an amino terminal non-serpin mucin-like domain. Deficiency of C1INH results in hereditary angioedema, a disease characterised by episodes of angioedema of the skin or the mucosa of the gastrointestinal tra...