| pubmed-article:10212120 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0023621 | lld:lifeskim |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0058171 | lld:lifeskim |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0205250 | lld:lifeskim |
| pubmed-article:10212120 | lifeskim:mentions | umls-concept:C0962754 | lld:lifeskim |
| pubmed-article:10212120 | pubmed:issue | 8 | lld:pubmed |
| pubmed-article:10212120 | pubmed:dateCreated | 1999-5-18 | lld:pubmed |
| pubmed-article:10212120 | pubmed:abstractText | Thiol-containing diketopiperazines have been recently identified as novel heterocyclic inhibitors of matrix metalloproteinase (MMPs). The compounds described had similar activities against the MMPs collagenase-1 and gelatinase-B. An inhibitor that showed greater than 10-fold selectivity for collagenase-1 over gelatinase-B was desired. Previously published work with peptidyl hydroxamates and thiols indicated that while preparing gelatinase selective inhibitors was straightforward, there was not an obvious route to selective inhibitors of collagenase-1. Combinatorial libraries were prepared and evaluated for their ability to inhibit collagenase-1 and gelatinase-B substrate hydrolysis. A method for estimating the IC50 values of compounds generated by high-throughput parallel synthesis aided in the identification of compounds with the desired properties. We have found that thiol diketopiperazines derived from nitrophenylalanine are both potent and selective inhibitors of collagenase-1. In addition, we have demonstrated that combinatorial chemistry can be utilized to identify molecules with a desired selectivity profile without access to the traditional tools of rational drug design. | lld:pubmed |
| pubmed-article:10212120 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10212120 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:10212120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10212120 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10212120 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:10212120 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:WangYY | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:IdaSS | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:CampbellD ADA | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:ShiLL | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:NavreMM | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:SzardeningsA... | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:SharkovNN | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:TienDD | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:AntonenkoVV | lld:pubmed |
| pubmed-article:10212120 | pubmed:author | pubmed-author:DeFranciscoNN | lld:pubmed |
| pubmed-article:10212120 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10212120 | pubmed:day | 22 | lld:pubmed |
| pubmed-article:10212120 | pubmed:volume | 42 | lld:pubmed |
| pubmed-article:10212120 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10212120 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10212120 | pubmed:pagination | 1348-57 | lld:pubmed |
| pubmed-article:10212120 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:meshHeading | pubmed-meshheading:10212120... | lld:pubmed |
| pubmed-article:10212120 | pubmed:year | 1999 | lld:pubmed |
| pubmed-article:10212120 | pubmed:articleTitle | Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines. | lld:pubmed |
| pubmed-article:10212120 | pubmed:affiliation | Affymax Research Institute, 3410 Central Expressway, Santa Clara, California 95051, USA. | lld:pubmed |
| pubmed-article:10212120 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:10212120 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10212120 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10212120 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10212120 | lld:pubmed |
