http://purl.uniprot.org/citations/26151189 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/26151189 | http://www.w3.org/2000/01/rdf-schema#comment | "On the basis of a crystal structure of a phenylpyrrolidine lead and subsequent molecular modeling results, we designed and synthesized a novel series of macrocyclic FVIIa inhibitors. The optimal 16-membered macrocycle was 60-fold more potent than an acyclic analog. Further potency optimization by incorporation of P1' alkyl sulfone and P2 methyl groups provided a macrocycle with TF/FVIIa Ki = 1.6 nM, excellent selectivity against a panel of seven serine proteases, and FVII-deficient prothrombin time EC2x = 1.2 μM. Discovery of this potent, selective macrocyclic scaffold opens new possibilities for the development of orally bioavailable FVIIa inhibitors."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.5b00788"xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Rendina A.R."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Wong P.C."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Wei A."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Cheney D.L."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Luettgen J.M."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Wexler R.R."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "Priestley E.S."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/author | "DeLucca I."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/date | "2015"xsd:gYear |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/pages | "6225-6236"xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/title | "Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors."xsd:string |
http://purl.uniprot.org/citations/26151189 | http://purl.uniprot.org/core/volume | "58"xsd:string |
http://purl.uniprot.org/citations/26151189 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/26151189 |
http://purl.uniprot.org/citations/26151189 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/26151189 |
http://purl.uniprot.org/uniprot/#_P08709-mappedCitation-26151189 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/26151189 |
http://purl.uniprot.org/uniprot/P08709 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/26151189 |