Amino acid Asp181 of 5'-flap endonuclease 1 is a useful target for chemotherapeutic development

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From: Biochemistry(Vol. 48, Issue 42)
Publisher: American Chemical Society
Document Type: Report
Length: 78 words

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Abstract :

Site-directed mutagenesis approach was used to identify an important role for amino acid Asp81 (involved in [Mg.sup.2+] binding in the active site) of 5'-Flap endonuclease 1 (Fen1) in its endonuclease activity. The findings from the study provide guidelines for the development of highly specific and safer structure-based small molecular inhibitors targeting the base excision repair (BER) pathway which could be used along with existing chemotherapeutic agents, like Temozolomide (TMZ), as combination therapy for the treatment of colorectal cancer.

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Gale Document Number: GALE|A212941561