左圖中,對黑色框起之部份作局部放大,結果如左下圖
此部份表示HSP90之Geldanamycin Dimer binding site 附近電子雲的分布情形
The structure of HSP90
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RasMol> show info molecular name-----heat shock protein 90classification-----chaperone protein brookheaven code---1yes number of chains---2 number of groups---213[246] number of atoms----1679[246] number of bonds----1706
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RasMol>select all 1925 atoms selected! RasMol> cartoons RasMol> collor structure RasMol> rotate x 180 ----右圖一 RasMol> rotate x -180 RasMol> rotate y 180 ----右圖二 RasMol> rotate y -180 RasMol> rotate z 180 ----右圖三 |
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RasMol>restrict 28-135 685 atoms selected! ResMol>strands ResMol>color CPK RasMol>select helex 702 atoms selected! ResMol>color structure ResMol>select 32 8 atoms selected! RosMol>sticks RosMol>color temparature RosMol>select 749 atoms selected! RosMol>sticks RosMol>color temparature RosMol>selecct 974 atoms selected! RosMol>sticks RosMol>color CPK RosMol>select 748 atoms selected! RosMol>sticks RosMol>color temparature |
The picture below shows the K32, R74, K97,and R101 that are mentioned in the paper.
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RasMol>select all 1925 atoms selected! RasMol>backbone RasMol>color structure RasMol>select sheet 389 atoms selected! RasMol>strands RasMol>select helix 702 atoms selected! RasMol>strands RasMol>color chain RasMol>select 130-140 84 atoms selected! RasMol>dots |
Intresting Paper About HSP90
TI: Title Identification of a Geldanamycin Dimer That Induces the Selective Degradation of HER-Family Tyrosine Kinases
AU: Author Zheng, FF; Kuduk, SD; Chiosis, G; Muenster, PN; Sepp-Lorenzino, L; Danishefsky, SJ; Rosen, N
AF: Author Affiliation Program in Cell Biology, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, Box 271, New York, NY 10021, USA;
E-mail: zhengf@mskcc.org
SO: Source Cancer Research [Cancer Res.], vol. 60, no. 8, pp. 2090-2094, 15 Apr 2000
IS: ISSN 0008-5472
AB: Abstract Geldanamycin (GM) is a natural antibiotic that binds Hsp90 and induces the degradation of receptor tyrosine kinases, steroid receptors, and Raf. It is a potent inhibitor of cancer cells that overexpress HER-kinases, but its effects on other important proteins may cause significant toxicity and limit its clinical use. We report the synthesis and identification of a GM dimer, GMD-4c, which had selective activity against HER-kinases. Selectivity was a function of linker length and required two intact GM moieties. GMD-4c is a potent inducer of G sub(1) block and apoptosis of breast cancer cell lines that overexpress HER2, but does not appreciably inhibit the growth of 32D cells that lack HER-kinases. GMD-4c could be useful in the treatment of carcinomas dependent on HER-kinases.
LA: Language English
SL: Summary Language English
PY: Publication Year 2000
PD: Publication Date 20000415
PT: Publication Type Journal Article
DE: Descriptors Protein-tyrosine kinase; Antitumor antibiotics; Apoptosis; geldanamycin; HER protein
ID: Identifiers tumor cell lines; man
CL: Classification B 26020 EGF & EGF receptor family/TGF alpha /Her/ErbB-2 (Neu)/ErbB-3/ErbB-4/amphiregulin
UD: Update 200008
SF: Subfile Oncogenes & Growth Factors Abstracts
AN: Accession Number 4731063
