RGD Reference Report - Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties. - Rat Genome Database

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Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.

Authors: Joossens, J  Ali, OM  El-Sayed, I  Surpateanu, G  Van der Veken, P  Lambeir, AM  Setyono-Han, B  Foekens, JA  Schneider, A  Schmalix, W  Haemers, A  Augustyns, K 
Citation: Joossens J, etal., J Med Chem. 2007 Dec 27;50(26):6638-46. Epub 2007 Dec 1.
RGD ID: 6484140
Pubmed: PMID:18052026   (View Abstract at PubMed)
DOI: DOI:10.1021/jm700962j   (Journal Full-text)

A set of small nonpeptidic diaryl phosphonate inhibitors was prepared. Some of these inhibitors show potent and highly selective irreversible uPA inhibition. The biochemical and modeling data prove that the combination of a benzylguanidine moiety with a diaryl phosphonate ester results in optimized molecules for derivatizing the serine alcohol in the uPA active site. Selected compounds show significant antimetastatic effects in the BN-472 rat mammary carcinoma model. We report in this paper a preclinical proof of concept that selective, irreversible uPA inhibitors could be valuable in antimetastatic therapy.

RGD Manual Disease Annotations    Click to see Annotation Detail View
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
Experimental Mammary Neoplasms disease_progressionISOPlau (Rattus norvegicus)6484140; 6484140 RGD 
Experimental Mammary Neoplasms disease_progressionIMP 6484140 RGD 

Objects Annotated

Genes (Rattus norvegicus)
Plau  (plasminogen activator, urokinase)

Genes (Mus musculus)
Plau  (plasminogen activator, urokinase)

Genes (Homo sapiens)
PLAU  (plasminogen activator, urokinase)


Additional Information