Human 5,10-methenyltetrahydrofolate and its compound crystallization methods, crystals and application thereof

A technology of methylenetetrahydrofolate and leucovorin, which is applied in the field of crystallization, crystallization and application of human 5,10-methylenetetrahydrofolate synthase and its complexes, can solve strong cytotoxicity , the effect is not obvious enough, problems such as discovery

Inactive Publication Date: 2012-09-05
北京普赛资产管理有限责任公司
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Problems solved by technology

There are two problems with the use of folic acid derivatives for cancer treatment. (1) After decades of use of these drugs, drug resistance has been found in many cases, and for some patients, the effect of these two drugs is not obvious enough (2) Most of these drugs have relatively strong cytotoxicity

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  • Human 5,10-methenyltetrahydrofolate and its compound crystallization methods, crystals and application thereof
  • Human 5,10-methenyltetrahydrofolate and its compound crystallization methods, crystals and application thereof
  • Human 5,10-methenyltetrahydrofolate and its compound crystallization methods, crystals and application thereof

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Embodiment approach

[0062] The crystallization method of the crystallization of human source 5,10-methinetetrahydrofolate synthase, firstly, the concentrated solution of the human source 5,10-methinetetrahydrofolate synthase is mixed with the pool solution; the above-mentioned enzyme protein The solution was centrifuged at 14,000rpm in an Eppendorf refrigerated centrifuge for 15 minutes; the crystal screening kit from Hampton was used for crystallization, and the composition of the crystallized pool liquid was 0.02MMgCl 2 , 0.02M NiCl 2 , HEPES (0.1 M, pH 6.6) and 20% PEG3350, and the resulting crystals were collected after about two days.

[0063] The crystallization method of the crystal of the complex of human source 5,10-methinetetrahydrofolate synthase and ADP, firstly add the final concentration of 5mM to the solution of human source 5,10-methinetetrahydrofolate synthase ATP solution, then add reducing agent and magnesium ions, mix to obtain human source 5,10-methinetetrahydrofolate syntha...

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Abstract

The invention relates to a crystal of humaniz 5,10-methenyltetrahydrofolate (MTHFS) and a crystallization method thereof, also relates to a crystal of a composite of the human 5,10-methenyltetrahydrofolate and ADP and a crystallization method thereof, a crystal of a composite of the human 5,10-methenyltetrahydrofolate and glutamic acid and a crystallization method thereof, a crystal of a composite of the human 5,10-methenyltetrahydrofolate and N5-imide phosphoric acid and a crystallization method thereof, and a crystal of a composite of the human 5,10-methenyltetrahydrofolate and a product, namely 10- methenyltetrahydrofolate and a crystallization method thereof, and also relates to important structure domains or peptide fragments in the crystals, and a method for designing and screening medicaments by using the structure domains or the peptide fragments.

Description

technical field [0001] The present invention relates to a crystal of human source 5,10-methinetetrahydrofolate synthase (MTHFS) and its crystallization method, and also relates to the synthesis of human source 5,10-methinetetrahydrofolate synthase and ADP Crystal of complex and method for crystallization thereof, Crystal of complex of human 5,10-methenetetrahydrofolate synthase and glutamic acid and method for crystallization thereof, human source 5,10-methinetetrahydrofolate Crystal of complex of folate synthase and N5-imine phosphate transition state and crystallization method thereof, crystal of complex of human source 5,10-methylenetetrahydrofolate synthase and product 10-formyltetrahydrofolate and its crystallization method Its crystallization method; it also relates to the structural domains or peptide fragments that play a key role in the enzymatic activity of human 5,10-methylenetetrahydrofolate synthase in these crystals; and the use of these important structural doma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12N9/00C30B29/54C30B7/00C07K16/40C07K2/00C12N15/11
Inventor 刘志杰武栋尼尔·肖恩成冲云宋高洁李杨
Owner 北京普赛资产管理有限责任公司
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