Discovery of Inhibitors of MicroRNA-21 Processing Using Small Molecule Microarrays

Perspectives in Pharmacology Ligand Discovery Using Small Molecule Microarrays

Small molecule microarrays have recently been used to identify ligands for several proteins, and several themes regarding screening strategies and limitations have emerged. In this review, some of the technical issues related to the manufacture and screening of small molecule microarrays, as well as prospects for small molecule microarrays in several areas of drug discovery and chemistry, are d...

PiP 1 Ligand discovery using small molecule microarrays

Discovery of small-molecule inhibitors of tyrosinase.

To identify novel inhibitors of tyrosinase, a fluorescent assay was developed which is suitable for high-throughput screening. In the assay, oxidation of the substrate by tyrosinase leads to the release of a fluorescent coumarin. Several small molecules were identified that inhibited mushroom tyrosinase in vitro and human tyrosinase in cell culture. These compounds may represent lead structures...

Discovery of selective small-molecule CD80 inhibitors.

Protein-protein interactions are widely found in biological systems controlling diverse cellular events. Because these interactions are implicated in many diseases such as autoimmunity and cancer, regulation of protein-protein interactions provides ideal targets for drug intervention. The CD80-CD28 costimulatory pathway plays a critical role in regulation of the immune response and thus constit...

Activity-based high-throughput profiling of metalloprotease inhibitors using small molecule microarrays.

We herein describe a high-throughput small molecule microarray (SMM) method that enables quick and cost-effective identification of potent inhibitors of metalloproteases in an activity-dependent manner, thereby offering a rapid means for inhibitor discovery and profiling.