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Synonyms: compound 6 [PMID:14561098]  | MK-429 | MK0429
Compound class: Synthetic organic
Comment: MK-0429 is an orally active, non-peptide inhibitor/antagonist of αv integrins [1-2,4]. It was initially identified as a clinical lead with potential utility for the prevention and treatment of osteoporosis , but has since shown activity in other biological settings. MK-0429 binds to the αv's Arg-Gly-Asp (RGD)-motif binding domain (the RGD-motif is a conserved sequence in proteins that bind to αv integrins), thereby preventing interaction with RGD-containing binding partners such as osteopontin, bone sialoprotein, vitronectin, and fibrinogen.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD et al.. (2003)
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
J Med Chem, 46 (22): 4790-8. [PMID:14561098]
2. Pickarski M, Gleason A, Bednar B, Duong LT. (2015)
Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis.
Oncol Rep, 33 (6): 2737-45. [PMID:25872534]
3. Rosenthal MA, Davidson P, Rolland F, Campone M, Xue L, Han TH, Mehta A, Berd Y, He W, Lombardi A. (2010)
Evaluation of the safety, pharmacokinetics and treatment effects of an alpha(nu)beta(3) integrin inhibitor on bone turnover and disease activity in men with hormone-refractory prostate cancer and bone metastases.
Asia Pac J Clin Oncol, 6 (1): 42-8. [PMID:20398037]
4. Zhou X, Zhang J, Haimbach R, Zhu W, Mayer-Ezell R, Garcia-Calvo M, Smith E, Price O, Kan Y, Zycband E et al.. (2017)
An integrin antagonist (MK-0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model.
Pharmacol Res Perspect, 5 (5). [PMID:28971604]