Title:
Ras PROTEIN DEGRADATION INDUCING MOLECULE AND PHARMACEUTICAL COMPOSITION
Document Type and Number:
WIPO Patent Application WO/2018/092723
Kind Code:
A1
Abstract:
A Ras protein degradation inducing molecule that can induce degradation of Ras proteins, and a pharmaceutical composition that contains this Ras protein degradation inducing molecule are provided. The Ras protein degradation inducing molecule is a conjugate of a Ras protein affinity molecule which has affinity to Ras proteins, and a proteolysis-inducing tag which has affinity to protease and does not inhibit proteolysis of proteins by the protease.
Inventors:
MIYAMOTO ETSUKO (JP)
OZAWA MASAAKI (JP)
OZAWA MASAAKI (JP)
Application Number:
PCT/JP2017/040779
Publication Date:
May 24, 2018
Filing Date:
November 13, 2017
Export Citation:
Assignee:
UNIV TOKYO SCIENCE FOUND (JP)
International Classes:
A61K47/51; A61K45/00; A61P1/16; A61P25/00; A61P25/28; A61P31/00; A61P35/00; A61P37/00; A61P43/00
Domestic Patent References:
| WO2016204197A1 | 2016-12-22 |
Foreign References:
| US20160264627A1 | 2016-09-15 | |||
| JP2013056837A | 2013-03-28 | |||
| US7208157B2 | 2007-04-24 | |||
| JP2016222683A | 2016-12-28 |
Other References:
INOBE, TOMONAO: "Molecular Structure of Protein Degradation by Proteasomes", 44TH ANNUAL RESEARCH REPORT (ASTELLAS FOUNDATION FOR RESEARCH ON METABOLIC DISORDERS NON-OFFICIAL TRANSLATION), 2012, pages 1 - 3, XP009507890
KOVRIGINA, E.A. ET AL.: "The Ras G Domain Lacks the Intrinsic Propensity to form Dimers", BIOPHYSICAL JOURNAL, vol. 109, no. 5, 1 September 2015 (2015-09-01), pages 1000 - 1008, XP055598401, ISSN: 0006-3495, DOI: 10.1016/j.bpj.2015.07.020
ITOH, Y. ET AL.: "Development of target protein-selective degradation inducer for protein knockdown", BIOORG. MED. CHEM., vol. 19, 2011, pages 3229 - 3241, XP028384646, DOI: doi:10.1016/j.bmc.2011.03.057
DEMIZU, Y. ET AL.: "Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy", BIOORG. MED. CHEM. LETT., vol. 15, 2012, pages 1793 - 1796
HINES, J. ET AL.: "Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs", PROC. NATL. ACAD. SCI. U.S.A., vol. 110, no. 22, 2013, pages 8942 - 8947
SASAKI, A. T. ET AL., SCI. SIGNAL., vol. 4, 2011, pages ral3
SCIENCE, vol. 265, 1994, pages 1234 - 1237
SCIENCE, vol. 316, 2007, pages 1349 - 1353
KISSELEV, A.F. ET AL., CHEMISTRY & BIOLOGY, vol. 19, 2012, pages 99 - 115
SUN, Q. ET AL., ANGEW. CHEM. INT. ED., vol. 51, 2012, pages 6140 - 6143
LONG, M. J. ET AL., CHEM. BIOL., vol. 19, no. 5, 2012, pages 629 - 637
KAISER, M. ET AL., CHEM. BIO. CHEM., vol. 5, 2004, pages 1256 - 1266
KOVRIGINA, E.A. ET AL.: "The Ras G Domain Lacks the Intrinsic Propensity to form Dimers", BIOPHYSICAL JOURNAL, vol. 109, no. 5, 1 September 2015 (2015-09-01), pages 1000 - 1008, XP055598401, ISSN: 0006-3495, DOI: 10.1016/j.bpj.2015.07.020
ITOH, Y. ET AL.: "Development of target protein-selective degradation inducer for protein knockdown", BIOORG. MED. CHEM., vol. 19, 2011, pages 3229 - 3241, XP028384646, DOI: doi:10.1016/j.bmc.2011.03.057
DEMIZU, Y. ET AL.: "Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy", BIOORG. MED. CHEM. LETT., vol. 15, 2012, pages 1793 - 1796
HINES, J. ET AL.: "Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs", PROC. NATL. ACAD. SCI. U.S.A., vol. 110, no. 22, 2013, pages 8942 - 8947
SASAKI, A. T. ET AL., SCI. SIGNAL., vol. 4, 2011, pages ral3
SCIENCE, vol. 265, 1994, pages 1234 - 1237
SCIENCE, vol. 316, 2007, pages 1349 - 1353
KISSELEV, A.F. ET AL., CHEMISTRY & BIOLOGY, vol. 19, 2012, pages 99 - 115
SUN, Q. ET AL., ANGEW. CHEM. INT. ED., vol. 51, 2012, pages 6140 - 6143
LONG, M. J. ET AL., CHEM. BIOL., vol. 19, no. 5, 2012, pages 629 - 637
KAISER, M. ET AL., CHEM. BIO. CHEM., vol. 5, 2004, pages 1256 - 1266
Attorney, Agent or Firm:
SHOBAYASHI Masayuki (JP)
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