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Volumn 19, Issue 2, 2009, Pages 352-355

Synthesis and initial evaluation of novel, non-peptidic antagonists of the αv-integrins αvβ3 and αvβ5

Author keywords

Inhibitors; Integrin

Indexed keywords

ALPHAVBETA5 INTEGRIN; CD51 ANTIGEN; INTEGRIN INHIBITOR; PEPTIDE LIBRARY; PROTEIN INHIBITOR; UNCLASSIFIED DRUG; VITRONECTIN RECEPTOR;

EID: 57749118590     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.11.074     Document Type: Article
Times cited : (9)

References (28)
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    • 11844302202 scopus 로고    scopus 로고
    • For an excellent review see: (and references therein)
    • For an excellent review see:. Cacciari B., and Spalluto G. Curr. Med. Chem. 12 (2005) 51 (and references therein)
    • (2005) Curr. Med. Chem. , vol.12 , pp. 51
    • Cacciari, B.1    Spalluto, G.2
  • 17
    • 57749107051 scopus 로고    scopus 로고
    • note
    • 3) in buffer A plus 20 μM DTPA, 0.05% BSA were then added to the wells followed by 1-h incubation at room temperature. The plate was washed with buffer A. The enhancement solution was added and the fluorescence was measured after 10-min incubation on the shaker.
  • 19
    • 57749087937 scopus 로고    scopus 로고
    • note
    • Physicochemical properties, including FPSA, were calculated using ADME Profiler: Program for discreet compound analysis and calculation of physicochemical properties, version 1.6.0; Pharmacopeia Inc., 2004.
  • 22
    • 57749119898 scopus 로고    scopus 로고
    • Letourneau, J. J.; Paradkar, V.; Ohlmeyer, M. H. J.; Dillard, L. W.; Baldwin, J. J.; Riviello, C. M.; Wong, A.; Rong, Y. U.S. Patent 7,365,209, April 29, 2008.
    • Letourneau, J. J.; Paradkar, V.; Ohlmeyer, M. H. J.; Dillard, L. W.; Baldwin, J. J.; Riviello, C. M.; Wong, A.; Rong, Y. U.S. Patent 7,365,209, April 29, 2008.
  • 25
    • 57749084946 scopus 로고    scopus 로고
    • note
    • 2 for 24 h. The media was then decanted and 200 μL of proliferation media containing EBM-2 plus 2% FBS and 3 ng/mL FGF with the compound was added and the cells were incubated for an additional 48 h. Cells were then fixed with 2.5% glutaraldehyde for 30 min, washed and stained with 0.1% crystal violet. Absorbance at 595 nM was measured after being washed and destained using 10% acetic acid.
  • 27
    • 57749113971 scopus 로고    scopus 로고
    • note
    • 2 for 1 h at 37 °C, followed by blocking with 2% BSA in the coating buffer for 1 h at 37 °C. HUVEC cells were then seeded to the upper chamber at 20,000 per well in 100 μL of migration buffer in the presence or absence of the compound. Migration buffer (500 μL) was added to the bottom chamber followed by incubation at 37 °C for 4 h. The non-migrated cells were removed from the upper side of the filters with a cotton ball. The migrated cells were fixed with 2.5% glutaraldehyde followed by washing and staining using 0.1% crystal violet. The stained cells were photographed and analyzed using ScanImage.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.