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Method of treating cancer by inhibition of protein kinase-like endoplasmic reticulum protein kinase
专利权人:
Timothy Cardozo;David Ron;Hong Wang
发明人:
Timothy Cardozo,Hong Wang,David Ron
申请号:
US13111769
公开号:
US09198891B2
申请日:
2011.05.19
申请国别(地区):
US
年份:
2015
代理人:
摘要:
The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK. The present invention further relates to compounds that can be used for inhibition of PERK, for example human PERK, and methods related to treatment of PERK-mediated diseases.
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