Inhibitory effect of phloroglucinol on α-glucosidase: Kinetics and molecular dynamics simulation integration study.

Binding Sites Catalytic Domain Enzyme Activation / drug effects Glycoside Hydrolase Inhibitors / chemistry Kinetics Molecular Docking Simulation Molecular Dynamics Simulation Phloroglucinol / chemistry Protein Binding Structure-Activity Relationship alpha-Glucosidases / chemistry
Aggregation Kinetics Non-competitive inhibition Phloroglucinol α-Glucosidase

Journal

International journal of biological macromolecules
ISSN: 1879-0003
Titre abrégé: Int J Biol Macromol
Pays: Netherlands
ID NLM: 7909578

Informations de publication

Date de publication:
01 Mar 2019
Historique:
received: 14 07 2018
revised: 22 11 2018
accepted: 28 11 2018
pubmed: 7 12 2018
medline: 24 4 2019
entrez: 4 12 2018
Statut: ppublish

Résumé

Regulation of α-glucosidase (EC 3.2.1.20) and its inhibitors is of great interest to researchers due to its clinical relevance as a target enzyme for the treatment of α-glucosidase-mediated diseases, such as type 2 diabetes mellitus and Pompe disease. In this study, we conducted a phloroglucinol-induced inhibition kinetics assay and performed computational molecular dynamics (MD) simulations to assess binding manner in α-glucosidase. The results showed that phloroglucinol reversibly inhibited α-glucosidase in a dose-dependent but non-competitive manner (K

Identifiants

DOI: 10.1016/j.ijbiomac.2018.11.268 PMID: 30503787
pubmed: 30503787
pii: S0141-8130(18)33600-6
doi: 10.1016/j.ijbiomac.2018.11.268
pii:
doi:

Substances chimiques

Glycoside Hydrolase Inhibitors 0
Phloroglucinol DHD7FFG6YS
alpha-Glucosidases EC 3.2.1.20

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

771-779

Informations de copyright

Copyright © 2018. Published by Elsevier B.V.

Auteurs

Jia-Xin Wan (JX)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

Gyutae Lim (G)

Genome Editing Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Gwahak-ro, Yuseong-gu, Daejeon 34141, Republic of Korea; Department of Bioinformatics, KRIBB School of Bioscience, Korea University of Science and Technology (UST), 217 Gajung-ro, Yuseong-gu, Daejeon 34113, Republic of Korea.

Jinhyuk Lee (J)

Genome Editing Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Gwahak-ro, Yuseong-gu, Daejeon 34141, Republic of Korea; Department of Bioinformatics, KRIBB School of Bioscience, Korea University of Science and Technology (UST), 217 Gajung-ro, Yuseong-gu, Daejeon 34113, Republic of Korea.

Xiao-Bao Sun (XB)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

De-Ying Gao (DY)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

Yue-Xiu Si (YX)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

Xin-Lei Shi (XL)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

Guo-Ying Qian (GY)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China.

Qian Wang (Q)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China. Electronic address: wangq@zwu.edu.cn.

Yong-Doo Park (YD)

College of Biological and Environmental Sciences, Zhejiang Wanli University, Ningbo 315100, PR China; Department of Dermatology, Sungkyunkwan University School of Medicine, Samsung Medical Center, Seoul 135-710, Republic of Korea; Skin Diseases Research Center, Yangtze Delta Region Institute of Tsinghua University, 705 Yatai Road, Jiaxing 314006, PR China. Electronic address: parkyd@hotmail.com.

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Éléments structuraux des protéines › Domaine catalytique › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Métabolisme › Activation enzymatique › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Hypoglycémiants › Inhibiteurs des glycoside hydrolases › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de dynamique moléculaire › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures cycliques › Hydrocarbures aromatiques › Dérivés du benzène › Phénols › Phloroglucinol › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Inhibitory effect of phloroglucinol on...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Glycosidases › Glucosidases › alpha-Glucosidase › Inhibitory effect of phloroglucinol on...