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Comparative analysis of stimulation and binding characteristics of adenosine analogs to AMP-activated protein kinase.
Gao, Feng; Qian, Yue-Jiao; Chen, Fei-Hu; Zhu, Hai-Bo.
Affiliation
  • Gao F; a State Key Laboratory for Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing 100050 , China.
  • Qian YJ; b Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University , Hefei 230032 , China.
  • Chen FH; b Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University , Hefei 230032 , China.
  • Zhu HB; a State Key Laboratory for Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing 100050 , China.
J Asian Nat Prod Res ; 21(9): 916-927, 2019 Sep.
Article in En | MEDLINE | ID: mdl-30187782
ABSTRACT
To compare the stimulation and binding characteristics of adenosine analogs including AMP, IMM-H007, and M1, to AMPK, and to explore the potential mechanism underlying the regulation effect of adenosine analogs on AMPK activity, [γ-32P]ATP assay, circular dichroism experiments and molecular docking test were performed. We found that the interactions with Thr86, Thr88, and His150 in site 1 are probably the reason why the affinities of IMM-H007, M1, and adenosine are comparable but their allosteric activation on AMPK varies greatly, partly interpreting the mechanism of AMPK activity regulated by adenosine analogs.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Adenosine / AMP-Activated Protein Kinases Type of study: Prognostic_studies Limits: Animals Language: En Journal: J Asian Nat Prod Res Journal subject: BOTANICA / QUIMICA Year: 2019 Document type: Article Affiliation country: China
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Adenosine / AMP-Activated Protein Kinases Type of study: Prognostic_studies Limits: Animals Language: En Journal: J Asian Nat Prod Res Journal subject: BOTANICA / QUIMICA Year: 2019 Document type: Article Affiliation country: China