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Volumn 14, Issue 24, 2004, Pages 6071-6074

Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors

Author keywords

ADAM12; Inhibitors; Virtual screening

Indexed keywords

A DISINTEGRIN AND METALLOPROTEASE; A DISINTEGRIN AND METALLOPROTEASE 12 INHIBITOR; METALLOPROTEINASE; METALLOPROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 8844224202     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.09.082     Document Type: Article
Times cited : (21)

References (18)
  • 9
    • 0142050948 scopus 로고    scopus 로고
    • Accelrys, Inc.: San Diego, CA
    • INSIGHT2000; Accelrys, Inc.: San Diego, CA
    • INSIGHT2000
  • 10
    • 84862461053 scopus 로고    scopus 로고
    • http://www.idrtech.com
  • 13
    • 8844227145 scopus 로고    scopus 로고
    • note
    • Generation of pHS/GMII-AP was described elsewhere. A DNA fragment encoding ADAM12 cleavage site (amino acids 84-162 of HB-EGF) was amplified, and inserted into the HindIII/NheI site of pHS/GMII-AP, resulting in pHS/GMII-HB-EGF-AP. The full-length ADAM12 and catalytic site deletion mutant ADAM12 (Δ205 → 413) coding sequences were amplified and inserted into the XhoI/BamHI site of pMK33/pMtHygor, resulting in pMT/wtADAM12 and pMT/Δ mutant ADAM12, respectively. Therefore, the substrate and protease constructs are under the control of Drosophila hsp70 and metallothionein promoters, respectively
  • 14
    • 8844256990 scopus 로고    scopus 로고
    • The compounds were purchased from ChemBridge, Inc. (San Diego, CA)
    • The compounds were purchased from ChemBridge, Inc. (San Diego, CA)
  • 15
    • 8844258477 scopus 로고    scopus 로고
    • note
    • 2, 0.005% Brij 35, pH 9.0) for 4 h at 37°C. The cleavage of the substrate was measured with a fluorometer (Molecular Devices) at excitation and emission wavelengths of 320 nm and 405 nm, respectively. Dose-dependent inhibition of ADAM12 was analyzed using SigmaPlot (SPPS Inc.)
  • 17
    • 84862455289 scopus 로고    scopus 로고
    • http://www.accelrys.com/doc/life/insight2000.3L


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.