Title:
BINDING MOLECULE EXHIBITING SELECTIVE BINDING FOR RAS(G12D) MUTANT
Document Type and Number:
WIPO Patent Application WO/2022/234851
Kind Code:
A1
Abstract:
It has been discovered that a large binding selectivity for the RAS(G12D) mutant is possessed by a binding molecule that has the following characteristic features: (i) direct interaction with the Asp12 in the RAS(G12D) mutant and (ii) interaction with the Switch 2 region in the RAS(G12D) mutant and intramolecular interaction between the Switch 2 region in the RAS(G12D) mutant and the Asp12 in the RAS(G12D) mutant. Such a molecule can be a promising candidate compound for the treatment and/or prevention of diseases associated with the expression of the RAS(G12D) mutant.
Inventors:
HAYASHI RYUJI (JP)
HASHIMOTO SATOSHI (JP)
MINAMI SAKI (JP)
HASHIMOTO SATOSHI (JP)
MINAMI SAKI (JP)
Application Number:
PCT/JP2022/019541
Publication Date:
November 10, 2022
Filing Date:
May 06, 2022
Export Citation:
Assignee:
CHUGAI PHARMACEUTICAL CO LTD (JP)
International Classes:
C07K7/54; C07K2/00
Domestic Patent References:
| WO2020230780A1 | 2020-11-19 | |||
| WO2013100132A1 | 2013-07-04 | |||
| WO2018225864A1 | 2018-12-13 | |||
| WO2021090855A1 | 2021-05-14 |
Foreign References:
| US20180319844A1 | 2018-11-08 | |||
| US20190119358A1 | 2019-04-25 | |||
| US20210032293A1 | 2021-02-04 | |||
| JP6880352B1 | 2021-06-02 |
Other References:
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ZHANG ZIYANG, GAO RONG, HU QI, PEACOCK HAYDEN, PEACOCK D. MATTHEW, DAI SHIZHONG, SHOKAT KEVAN M., SUGA HIROAKI: "GTP-State-Selective Cyclic Peptide Ligands of K-Ras(G12D) Block Its Interaction with Raf", ACS CENTRAL SCIENCE, vol. 6, no. 10, 28 October 2020 (2020-10-28), pages 1753 - 1761, XP055935151, ISSN: 2374-7943, DOI: 10.1021/acscentsci.0c00514
AYUMU NIIDA, SHIGEKAZU SASAKI, KAZUKO YONEMORI, TOMOYA SAMESHIMA, MASAHIRO YAGUCHI, TAIJI ASAMI, KOTARO SAKAMOTO, MASAHIRO KAMAURA: "Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 27, no. 12, 1 June 2017 (2017-06-01), Amsterdam NL , pages 2757 - 2761, XP055760728, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2017.04.063
NAT. REV. DRUG DISCOV., vol. 13, no. 11, November 2014 (2014-11-01), pages 828 - 851
NAT. REV. DRUG DISCOV., vol. 13, no. 12, December 2014 (2014-12-01), pages 928 - 942
NAT. REV. DRUG DISCOV., vol. 15, no. 11, November 2016 (2016-11-01), pages 771 - 785
ACS MED. CHEM. LETT., vol. 8, 2017, pages 732 - 736
ACS CENT. SCI., vol. 6, 2020, pages 1753 - 1761
J. APPL. CRYST., vol. 40, 2007, pages 658 - 674
ACTA CRYST, vol. D67, 2011, pages 355 - 467
MANDEL, M., HIGA, A., JOURNAL OF MOLECULAR BIOLOGY, vol. 53, 1970, pages 158 - 162
HANAHAN, D., JOURNAL OF MOLECULAR BIOLOGY, vol. 166, 1983, pages 557 - 580
MERCK, SOLID PHASE SYNTHESIS HANDBOOK, 1 May 2002 (2002-05-01)
CAS , no. 72914-19-3
CAS, no. 467435-07-0
Attorney, Agent or Firm:
HASEGAWA Yoshiki et al. (JP)
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