| pubmed-article:19807094 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C0242402 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C0013355 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C0392747 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C1554963 | lld:lifeskim |
| pubmed-article:19807094 | lifeskim:mentions | umls-concept:C1707271 | lld:lifeskim |
| pubmed-article:19807094 | pubmed:issue | 21 | lld:pubmed |
| pubmed-article:19807094 | pubmed:dateCreated | 2009-11-5 | lld:pubmed |
| pubmed-article:19807094 | pubmed:abstractText | Structural modifications affecting the efficacy of analogues of the endogenous opioid peptide dynorphin (Dyn) A have focused on the N-terminal "message" sequence based on the "message-address" concept. To test the hypothesis that changes in the C-terminal "address" domain could affect efficacy, modified amino acids and cyclic constraints were incorporated into this region of the partial agonist [N-benzylTyr(1)]Dyn A-(1-11). Modifications in the C-terminal domain of [N-benzylTyr(1)]Dyn A-(1-11)NH(2) resulted in increased kappa opioid receptor (KOR) affinity for all of the linear analogues but did not affect the efficacy of these peptides at KOR. Cyclization between positions 5 and 8 yielded [N-benzylTyr(1),cyclo(d-Asp(5),Dap(8))]Dyn A-(1-11)NH(2) (zyklophin, 13) ( J. Med. Chem. 2005 , 48 , 4500 - 4503 ) with high selectivity for KOR. In contrast to the linear peptides, this peptide exhibits negligible efficacy in the adenylyl cyclase (AC) assay and is a KOR antagonist. These data are consistent with our hypothesis that appropriate modifications in the "address" domain of Dyn A analogues may affect efficacy. | lld:pubmed |
| pubmed-article:19807094 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19807094 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19807094 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19807094 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:19807094 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:19807094 | pubmed:author | pubmed-author:MurrayThomas... | lld:pubmed |
| pubmed-article:19807094 | pubmed:author | pubmed-author:AldrichJane... | lld:pubmed |
| pubmed-article:19807094 | pubmed:author | pubmed-author:PatkarKshitij... | lld:pubmed |
| pubmed-article:19807094 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19807094 | pubmed:day | 12 | lld:pubmed |
| pubmed-article:19807094 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:19807094 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19807094 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19807094 | pubmed:pagination | 6814-21 | lld:pubmed |
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| pubmed-article:19807094 | pubmed:meshHeading | pubmed-meshheading:19807094... | lld:pubmed |
| pubmed-article:19807094 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19807094 | pubmed:articleTitle | The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues. | lld:pubmed |
| pubmed-article:19807094 | pubmed:affiliation | Department of Medicinal Chemistry, University of Kansas, Lawrence, Kansas 66045, USA. | lld:pubmed |
| pubmed-article:19807094 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:19807094 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19807094 | lld:chembl |
