Drug compound high-throughput screening method

A technology of pharmaceutical compounds and screening methods, applied in the field of drug screening, to achieve good metabolic stability and improve drugability

Active Publication Date: 2018-09-28
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the problem that traditional high-throughput screening only focuses on target activity, the present invention provides a high-throughput screening method for pharmaceutical compounds. The compounds screened by this method have the dual advantages of pharmacological activity and metabolic stability, which will greatly improve the high-throughput screening method of drugs. Success Rate of Throughput Screening

Method used

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Embodiment 1

[0037]Opioid Receptor Ligand Binding Activity Screening Simultaneous Metabolic Stability Screening Assay

[0038] Experimental steps:

[0039] 1. Expressing opioid receptors on CHO cells: For specific steps, see literature reports: Li Yulei, et al., Establishment of a Stable Expression System for Human Recombinant Opioid Receptors in CHO Cells, Journal of the Academy of Military Medical Sciences, 2009, 33, (5): 409-485);

[0040] 2. Cell treatment: cell collection, lysis, and membrane protein extraction: the specific steps are to take out the cell bottle that is 90% full, discard the culture medium, and wash twice with 3ml PBS. Add 3ml of trypsin solution to each bottle of culture flask, digest the cells for 8-10min, blow down the cells, collect them into a 10ml centrifuge tube, centrifuge at 1500rpm, 4°C for 8min. Pour off the supernatant, add PBS buffer and incubate for 30min. Pass the needle (No. 4 needle, 0.45×13mm disposable syringe) 5-10 times under ice bath. Add lys...

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Abstract

The invention relates to the technical field of drug screening and discloses a drug compound high-throughput screening method. A metabolic enzyme source and an auxiliary reaction factor thereof are added into a traditional drug high-throughput activity screening incubation system, a drug body interior acting environment is simulated, a drug compound with target effect efficacy and meanwhile good metabolic stability is screened according to an activity inhibition curve, and the screened compound has higher druggability; and meanwhile an active metabolite can further be found, and accordingly anew candidate compound is found.

Description

technical field [0001] The invention relates to the technical field of drug screening, in particular to a high-throughput screening method for drug compounds. Background technique [0002] Innovative drug screening requires the cooperation of multiple disciplines such as medicinal chemistry, pharmacology, drug metabolism, toxicology, and preparations. The current de novo research and development of innovative drugs is often carried out sequentially by several disciplines. Medicinal chemistry uses combinatorial chemistry to design and synthesize a large number of compounds according to the target structure. Pharmacology uses high-throughput screening technology to quickly evaluate the activity and then screen out hit compounds. Drug metabolism And toxicology application early drug metabolism and discovery toxicology technology platform cooperate with high-throughput evaluation to further determine the lead compound. Although this mode has promoted the speed and success rate o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/02
CPCG01N33/5067
Inventor 庄笑梅张文鹏张天宏李正张云霞王娟相亚楠
Owner ACADEMY OF MILITARY MEDICAL SCI
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