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Hypoxia-inducible factor 1a HIF-1 variants and methods for identifying HIF-1 modulators.
Hypoxia-inducible factor 1a HIF-1 variants and methods for identifying HIF-1 modulators.
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机译:低氧诱导因子1a HIF-1变体和鉴定HIF-1调节剂的方法。
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摘要
The present invention relates to a method for identifying compounds capable of modulating the function of a functional domain of human HIF-1 alpha , said method comprising (i) contacting a candidate compound with a variant of human HIF-1 alpha , said variant essentially lacking at least one functional domain of human HIF-1 alpha , or having a mutation making at least one functional domain of human HIF-1 alpha essentially inactive, said functional domain or domains being selected from the group consisting of (a) the PAS-B domain located in human HIF-1 alpha between amino acids 178 and 390, (b) the C-terminal nuclear localization sequence (NLS) located in human HIF-1 alpha essentially at amino acids 718 to 721, and (c) the transactivator / coactivator domain (N-TAD) located in human HIF-1 alpha essentially between amino acids 531 to 584, and (d) the transactivator / coactivator domain (C-TAD) located in human HIF-1 alpha essentially between amino acids 813 and 826, and (ii) determining the effect of the candidate compound on the said variant.
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