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Volumn 19, Issue 16, 2009, Pages 4622-4625

Design of selective Cathepsin inhibitors

Author keywords

Cathepsin; Cathepsin B; Cathepsin K; Cathepsin L; Cathepsin L2; Cathepsin S; Cathepsin V; Covalent inhibitor; Cysteine protease; Electrostatic; Hot spot; Hydrogen bond; Hydrogen bonding; Nitrile; Protein structure; Selectity; Structure based design; X ray crystallography

Indexed keywords

CATHEPSIN; CATHEPSIN INHIBITOR; ENZYME INHIBITOR; UNCLASSIFIED DRUG;

EID: 67749118106     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.06.090     Document Type: Article
Times cited : (26)

References (23)
  • 12
    • 67749123530 scopus 로고    scopus 로고
    • note
    • There are four protein molecules in the asymmetric unit of the crystal structure of the complex of Cathepsin L with 2. The ranges for the H-H distance and angle between the NH vectors are 2.77 Å to 2.84 Å and 25° to 27°, respectively.
  • 16
    • 67749138960 scopus 로고    scopus 로고
    • note
    • 50/M).
  • 17
    • 67749117330 scopus 로고    scopus 로고
    • note
    • 50 for inhibition of Cathepsins L, L2, S, K and B were determined from dose dependent inhibition of cleavage of fluorogenic, AMC-tagged, peptide substrates. See also Ref. 18.
  • 20
    • 67749115530 scopus 로고    scopus 로고
    • note
    • Diffraction data for compound 35 were collected at 100 K on beamline PX at the Swiss Light Source (SLS, Villigen, Switzerland). The structure was solved by molecular replacement and refined to a final resolution of 2.33 Å and R-factor of 25.0% using the CCP4 (Ref. 21) and Coot (Ref. 22) software packages. This structure has been deposited in the RSB (home.rcsb.org) Protein Data Bank (www.rcsb.org/pdb/home/home.do) with reference code 3HWN.
  • 21
    • 33744820336 scopus 로고
    • Number 4; (http://www.ccp4.ac.uk)
    • Collaborative Computational Project
    • Collaborative Computational Project, Number 4; (http://www.ccp4.ac.uk) Acta Crystallogr. 1994, D50, 760.
    • (1994) Acta Crystallogr , vol.D50 , pp. 760
  • 22
    • 67749117329 scopus 로고    scopus 로고
    • Coot: http://www.ysbl.york.ac.uk/~emsley/coot.
    • Coot: http


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.