HEXOKINASE 2 INHIBITOR SCREENING METHOD AND APPLICATION OF SMALL MOLECULE COMPOUND IN PREPARATION OF ANTITUMOR DRUG

WIPO Patent Application WO/2022/222261

A1

A hexokinase 2 inhibitor screening method and an application of a small molecule compound in the preparation of an antitumor drug. The screening method comprises: mixing a candidate inhibitor with a buffer solution, incubating, and terminating the reaction to obtain a reacted solution, the buffer solution comprising hexokinase 2 and glucose; uniformly mixing the reacted solution with an equal volume of glucose-1-13C to obtain a substance to be analyzed; and dropwise adding said substance to the surface of a graphite structure-type nanomaterial matrix, performing MALDI-MS detection after drying, and screening to obtain a hexokinase 2 inhibitor. By using a graphite structure-type nanomaterial as a matrix, and combining MALDI‑MS detection, ultra-fast screening and detection are realized; a series of small molecule drugs having high inhibition of brain tumor growth activity are obtained; and drug efficacy analysis/pharmacokinetic detection of a docked small molecule drug is performed without transferring the drug to other detection platforms.

LIU JIAN (CN)
SHI RUI (CN)
PAN PEICHEN (CN)
LV RUI (CN)
KANG ZHENHUI (CN)
HOU TINGJUN (CN)

PCT/CN2021/101767

October 27, 2022

June 23, 2021

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UNIV SOOCHOW (CN)

G01N27/64; A61K31/165; A61K31/381; A61K31/4164; A61K31/4439; A61K45/00; A61P35/00; C12Q1/68

CN113109418A	2021-07-13
CN102335221A	2012-02-01
CN107406485A	2017-11-28
CN107628615A	2018-01-26
CN107346379A	2017-11-14
CN103063730A	2013-04-24
CN101386882A	2009-03-18
US20200063183A1	2020-02-27
US5213966A	1993-05-25

UNITALEN ATTORNEYS AT LAW (CN)

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