Highly Selective Binding and Inhibition of Pyr-His-Pro-NH<sub>2</sub> (TRH) Function using a Polypyridinyl Macrocyclic Receptor with an Amphiphilic Cavity.

Hou, Chao-Ping; Yang, Jian; Zhang, Lei; Ma, Zhen-Hua; Li, Qian; Xiang, Jun-Feng; Gong, Han-Yuan

Highly Selective Binding and Inhibition of Pyr-His-Pro-NH₂ (TRH) Function using a Polypyridinyl Macrocyclic Receptor with an Amphiphilic Cavity.

Hou, Chao-Ping; Yang, Jian; Zhang, Lei; Ma, Zhen-Hua; Li, Qian; Xiang, Jun-Feng; Gong, Han-Yuan.

Afiliação

Hou CP; College of Chemistry, Beijing Normal University, No. 19, Xinjiekouwai Street, Beijing, 100875, P. R. China.
Yang J; College of Chemistry, Beijing Normal University, No. 19, Xinjiekouwai Street, Beijing, 100875, P. R. China.
Zhang L; Chongqing Customs Technical Center, No. 8 Honghuang Road, Jiangbei District, Chongqing, 400020, P. R. China.
Ma ZH; College of Chemistry, Beijing Normal University, No. 19, Xinjiekouwai Street, Beijing, 100875, P. R. China.
Li Q; Beijing National Laboratory for Molecular Sciences, Zhongguancunbeiyijie 2, Beijing, 100190, P. R. China.
Xiang JF; University of Chinese Academy of Sciences, Beijing, 100049, P. R. China.
Gong HY; Beijing National Laboratory for Molecular Sciences, Zhongguancunbeiyijie 2, Beijing, 100190, P. R. China.

Chemistry ; 26(43): 9466-9470, 2020 Aug 03.

Article em En | MEDLINE | ID: mdl-32259330

ABSTRACT

ABSTRACT

Macrocycle, cyclo[4] [(1,3-(4,6)-dimethylbezene)[4](2,6-(3,5)-dimethylpyridine (B4P4), shows highly selective binding affinity with protirelin (Pyr-His-Pro-NH2 ; TRH) among the tested 26 drug or drug adductive substrates. The stable complexation in a 11 manner was fully characterized in solution, gas phase, and solid state study. Furthermore, B4P4 acts as an efficient TRH inhibitor even at [macrocycle][drug] <1300, both in membrane transport and cellar incubation. The current work provides an unprecedented strategy for macrocycles to be efficiently used in drug target therapy.

Assuntos

Dipeptídeos/química; Piridinas/química; Hormônio Liberador de Tireotropina/farmacologia; Dipeptídeos/metabolismo; Hormônio Liberador de Tireotropina/química; Hormônio Liberador de Tireotropina/metabolismo

Palavras-chave

adductive dosage; drug inhibition; host-guest systems; macrocyclic receptors; molecular recognition

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Hormônio Liberador de Tireotropina / Dipeptídeos Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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