219616-31-6Relevant academic research and scientific papers
Synthesis of an inhibitor-tethered resin for detection of active matrix metalloproteinases involved in disease
Hesek, Dusan,Toth, Marta,Krchnak, Viktor,Fridman, Rafael,Mobashery, Shahriar
, p. 5848 - 5854 (2006)
Matrix metalloproteinases (MMPs), of which 26 members are known in humans, are implicated in a number of diseases. Their activity is strictly controlled, but when the biological control over the activity is lost, disease processes set in. In an attempt to delineate what MMP activity has gone awry in what diseases, including metastatic cancers that are of special interest to our laboratories, we conceived and synthesized two chromatographic resins incorporated with a multifunctional broad-spectrum inhibitor for MMPs. The broad-spectrum inhibitor contains three sterogentic centers and was synthesized in 13 steps. Two structural variants of the inhibitors were linked to the polymer support via disulfide moieties. These resins are intended for use in cellular systems to selectively fish out from a complex mixture of all cellular proteins the active MMP forms important for the specific disease for identification.
Design and synthesis of the cartilage protective agent (CPA, Ro32-3555)
Broadhurst,Brown,Lawton,Ballantyne,Borkakoti,Bottomley,Cooper,Eatherton,Kilford,Malsher,Nixon,Lewis,Sutton,Johnson
, p. 2299 - 2302 (2007/10/03)
A novel series of MMP inhibitors has been identified. The compounds are potent selective inhibitors of collagenase with good solubility and oral bioavailability. One compound, designated Ro32-3555, has been selected for development as a cartilage protective agent for use in the treatment of rheumatoid- and osteoarthritis.
