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METHOD FOR MEASURING TYROSINE PHOSPHATASE AND TYROSINE KINASE ACTIVITY

外国特許コード F170009095
整理番号 (S2015-1473-N0)
掲載日 2017年5月30日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP078224
国際公開番号 WO 2017061288
国際出願日 平成28年9月26日(2016.9.26)
国際公開日 平成29年4月13日(2017.4.13)
優先権データ
  • 特願2015-198320 (2015.10.6) JP
発明の名称 (英語) METHOD FOR MEASURING TYROSINE PHOSPHATASE AND TYROSINE KINASE ACTIVITY
発明の概要(英語) Provided is a method for measuring tyrosine phosphatase and tyrosine kinase activity, as a high-sensitivity measuring method, which is suitable for high throughput and which uses a compound represented by general formula (I) (in the formula, A represents a conjugated ring; L represents a linker or the like having a labeling substance at an end; R1 represents a hydrogen atom or the like; and R2 and R3 each represent a hydrogen atom, an alkyl group or the like).
特許請求の範囲(英語) [claim1]
1. Measuring method of the thyrosin phosphatase activity which features that process below is included,
The process which (1) reacts the thyrosin phosphatase which is made the measuring object and the peptide which includes the phosphorylation thyrosin residue, deviation from phosphorylates the phosphorylation thyrosin residue,
(2) deviation from in the thyrosin residue which is made to phosphorylate, under existing of the oxidizer and the metal catalyst, below-mentioned general formula (i)
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the process which makes the chemical compound connect which is displayed,
The process which (3) measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide calculates thyrosin phosphatase activity from that quantity.
[claim2]
2. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 1 which features that it is the chemical compound which is displayed measuring method of thyrosin phosphatase activity of statement.
[claim3]
3. In the claim 1 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects the fluorophor to the peptide which includes the phosphorylation thyrosin residue, the chemical compound which is displayed with general formula (i) it connects to peptide making use of the carrier which is connected with the chemical compound which is displayed with general formula (i) uniquely, is isolated, it connects to peptide with the aforementioned fluorophor is measured or 2 measuring method of thyrosin phosphatase activity of statement.
[claim4]
4. In the claim 1 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide the fluorophor where it makes the fluorophor the peptide connect which includes the phosphorylation thyrosin residue, the chemical compound connect which is displayed with general formula (i), makes the quencher for the aforementioned fluorophor and the fluorophor or the aforementioned fluorophor which forms FRET pair, makes peptide connect and/or with the change of fluorescence of the fluorophor which is made to connect to the chemical compound which is displayed with general formula (i), is measured or 2 measuring method of thyrosin phosphatase activity of statement.
[claim5]
5. Peptide and below-mentioned general formula (i) the phosphorylation thyrosin residue is included
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the kit for thyrosin phosphatase active measurement which features that the chemical compound which is displayed is included.
[claim6]
6. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 5 which features that it is the chemical compound which is displayed the kit for thyrosin phosphatase active measurement of statement.
[claim7]
7. Screening method of the thyrosin phosphatase inhibiter or the activator which features that process below is included,
(1) under existing of the suffering *** substance, the process which makes thyrosin phosphatase and the peptide contact which includes the phosphorylation thyrosin residue,
(2) the peptide which includes the phosphorylation thyrosin residue which was made to contact with thyrosin phosphatase, under existing of the oxidizer and the metal catalyst, below-mentioned general formula (i)
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the process which is made to contact with the chemical compound which is displayed,
The process which (3) measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide calculates thyrosin phosphatase activity from that quantity.
[claim8]
8. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 7 which features that it is the chemical compound which is displayed screening method of the thyrosin phosphatase inhibiter or the activator of statement.
[claim9]
9. In the claim 7 which features that the quantity of the chemical compound which is displayed with general formula (i) by the fluorophor where it connects the fluorophor to the peptide which includes the phosphorylation thyrosin residue, the chemical compound which is displayed with general formula (i) it connects to peptide making use of the carrier which is connected with the chemical compound which is displayed with general formula (i) uniquely, is isolated, connects to peptide is measured or 8 screening method of the thyrosin phosphatase inhibiter or the activator of statement.
[claim10]
10. In the claim 7 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide the fluorophor where it makes the fluorophor the peptide connect which includes the phosphorylation thyrosin residue, the chemical compound connect which is displayed with general formula (i), makes the quencher for the aforementioned fluorophor and the fluorophor or the aforementioned fluorophor which forms FRET pair, makes peptide connect and/or with the change of fluorescence of the fluorophor which is made to connect to the chemical compound which is displayed with general formula (i), is measured or 8 screening method of the thyrosin phosphatase inhibiter or the activator of statement.
[claim11]
11. Peptide and below-mentioned general formula (i) the phosphorylation thyrosin residue is included
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the diagnostic medicine of the diabetes which features that the chemical compound which is displayed is included.
[claim12]
12. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 11 which features that it is the chemical compound which is displayed the diagnostic medicine of diabetes of statement.
[claim13]
13. Measuring method of the thyrosin kinase activity which features that process below is included,
The process which (1) reacts the thyrosin kinase which is made the measuring object and the peptide which includes the non phosphorylation thyrosin residue, phosphorylates the non phosphorylation thyrosin residue,
(2) in the thyrosin residue which is not phosphorylated, under existing of the oxidizer and the metal catalyst, below-mentioned general formula (i)
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the process which makes the chemical compound connect which is displayed,
The process which measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide (3) in process (2),
(4) process in the non phosphorylation thyrosin residue of the peptide which includes the non phosphorylation thyrosin residue which is used with (1), under existing of the oxidizer and the metal catalyst, the process which makes the chemical compound connect which is displayed with general formula (i),
The process which measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide (5) in process (4),
(6) process the quantity and process of the chemical compound which is displayed with general formula (i) it connects to the peptide which was measured with (3) the process which calculates thyrosin kinase activity from the quantity of the chemical compound which is displayed with general formula (i) it connects to the peptide which was measured with (5).
[claim14]
14. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 13 which features that it is the chemical compound which is displayed measuring method of thyrosin kinase activity of statement.
[claim15]
15. In the claim 13 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects the fluorophor to the peptide which includes the non phosphorylation thyrosin residue, the chemical compound which is displayed with general formula (i) it connects to peptide making use of the carrier which is connected with the chemical compound which is displayed with general formula (i) uniquely, is isolated, it connects to peptide with the aforementioned fluorophor is measured or 14 measuring method of thyrosin kinase activity of statement.
[claim16]
16. In the claim 13 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide the fluorophor where it makes the fluorophor the peptide connect which includes the non phosphorylation thyrosin residue, the chemical compound connect which is displayed with general formula (i), makes the quencher for the aforementioned fluorophor and the fluorophor or the aforementioned fluorophor which forms FRET pair, makes peptide connect and/or with the change of fluorescence of the fluorophor which is made to connect to the chemical compound which is displayed with general formula (i), is measured or 14 measuring method of thyrosin kinase activity of statement.
[claim17]
17. Peptide and below-mentioned general formula (i) the non phosphorylation thyrosin residue is included
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the kit for thyrosin kinase active measurement which features that the chemical compound which is displayed is included.
[claim18]
18. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 17 which features that it is the chemical compound which is displayed the kit for thyrosin kinase active measurement of statement.
[claim19]
19. Screening method of the thyrosin kinase inhibiter or the activator which features that process below is included,
(1) under existing of the suffering *** substance, the process which makes the thyrosin kinase and the peptide contact which includes the non phosphorylation thyrosin residue,
(2) the peptide which includes the non phosphorylation thyrosin residue which was made to contact with the thyrosin kinase, under existing of the oxidizer and the metal catalyst, below-mentioned general formula (i)
(In formula, A displays conjugate ring, L displays the hydrogen atom, or displays the linker which possesses the sign substance in linker or the end which possesses the functional group which is used for the click reaction for the end which exists in optional position with respect to conjugate ring, 1 or 2 amino groups where R (1) displays the hydrogen atom, or 1 radioisotopes which exist in optional position with respect to conjugate ring, or the functional group which is used for the click reaction displays, or exists in optional position with respect to conjugate ring, the acetamide basis and the hydroxy basis, displaying the alkyl group, or alkoxy groupR (2) and R (3) the respective hydrogen atom, displays the aromatic basis which is possible to have possessed the alkyl group and the substituent.)
So the process which is made to contact with the chemical compound which is displayed,
The process which measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide (3) in process (2),
(4) process the peptide which includes the non phosphorylation thyrosin residue which is used with (1), under existing of the oxidizer and the metal catalyst, the process which is made to contact with the chemical compound which is displayed with general formula (i),
The process which measures the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide (5) in process (4),
(6) process the quantity and process of the chemical compound which is displayed with general formula (i) it connects to the peptide which was measured with (3) the process which calculates thyrosin kinase activity from the quantity of the chemical compound which is displayed with general formula (i) it connects to the peptide which was measured with (5).
[claim20]
20. Is displayed with general formula (i) the chemical compound which, the below-mentioned general formula (Ia)
(In formula, L in the same sense as description above.)
So in the claim 19 which features that it is the chemical compound which is displayed screening method of the thyrosin kinase inhibiter or the activator of statement.
[claim21]
21. In the claim 19 which features that the quantity of the chemical compound which is displayed with general formula (i) by the fluorophor where it connects the fluorophor to the peptide which includes the non phosphorylation thyrosin residue, the chemical compound which is displayed with general formula (i) it connects to peptide making use of the carrier which is connected with the chemical compound which is displayed with general formula (i) uniquely, is isolated, connects to peptide is measured or 20 screening method of the thyrosin kinase inhibiter or the activator of statement.
[claim22]
22. In the claim 19 which features that the quantity of the chemical compound which is displayed with general formula (i) it connects to peptide the fluorophor where it makes the fluorophor the peptide connect which includes the non phosphorylation thyrosin residue, the chemical compound connect which is displayed with general formula (i), makes the quencher for the aforementioned fluorophor and the fluorophor or the aforementioned fluorophor which forms FRET pair, makes peptide connect and/or with the change of fluorescence of the fluorophor which is made to connect to the chemical compound which is displayed with general formula (i), is measured or 20 screening method of the thyrosin kinase inhibiter or the activator of statement.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • TOKYO INSTITUTE OF TECHNOLOGY
  • 発明者(英語)
  • SATO SHINICHI
  • NAKAMURA HIROYUKI
  • NAKANO HIROFUMI
国際特許分類(IPC)
指定国 (WO201761288)
National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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