CN108713028B - rapafucin文库的合成和组合物 - Google Patents

rapafucin文库的合成和组合物 Download PDF

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CN108713028B
CN108713028B CN201780010182.2A CN201780010182A CN108713028B CN 108713028 B CN108713028 B CN 108713028B CN 201780010182 A CN201780010182 A CN 201780010182A CN 108713028 B CN108713028 B CN 108713028B
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CN108713028A (zh
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J·刘
J·王
Z·郭
萨姆·洪
刘武坤
彭汉景
马尼沙·达斯
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Johns Hopkins University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K17/00—Carrier-bound or immobilised peptides; Preparation thereof
    • C07K17/02—Peptides being immobilised on, or in, an organic carrier
    • C07K17/08—Peptides being immobilised on, or in, an organic carrier the carrier being a synthetic polymer
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803—General methods of protein analysis not limited to specific proteins or families of proteins
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2570/00—Omics, e.g. proteomics, glycomics or lipidomics; Methods of analysis focusing on the entire complement of classes of biological molecules or subsets thereof, i.e. focusing on proteomes, glycomes or lipidomes
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/24—Immunology or allergic disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biotechnology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
CN201780010182.2A 2016-02-04 2017-02-03 rapafucin文库的合成和组合物 Active CN108713028B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662291437P 2016-02-04 2016-02-04
US62/291,437 2016-02-04
PCT/US2017/016481 WO2017136708A1 (en) 2016-02-04 2017-02-03 Synthesis and composition of rapafucin libraries

Publications (2)

Publication Number Publication Date
CN108713028A CN108713028A (zh) 2018-10-26
CN108713028B true CN108713028B (zh) 2021-12-28

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US (1) US10662220B2 (enExample)
EP (1) EP3411413A4 (enExample)
JP (2) JP6891183B2 (enExample)
CN (1) CN108713028B (enExample)
AU (1) AU2017214550B2 (enExample)
CA (1) CA3013589A1 (enExample)
MX (1) MX2018009405A (enExample)
WO (1) WO2017136708A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI852183B (zh) 2011-12-28 2024-08-11 日商中外製藥股份有限公司 胜肽化合物之環化方法
US10815489B2 (en) 2015-03-13 2020-10-27 Chugai Seiyaku Kabushiki Kaisha Modified aminoacyl-tRNA synthetase and use thereof
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
CN108697729B (zh) 2016-02-04 2023-05-09 约翰霍普金斯大学 新型GLUT抑制剂rapaglutin及其用途
WO2017136708A1 (en) * 2016-02-04 2017-08-10 The Johns Hopkins University Synthesis and composition of rapafucin libraries
AU2017214557B2 (en) * 2016-02-04 2022-05-19 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
US12391971B2 (en) 2017-01-31 2025-08-19 Chugai Seiyaku Kabushiki Kaisha Method for synthesizing peptides in cell-free translation system
EP3636807A4 (en) * 2017-06-09 2021-07-28 Chugai Seiyaku Kabushiki Kaisha CYCLIC PEPTIDE COMPOUND WITH HIGH MEMBRANE PERMEABILITY AND LIBRARY WITH IT
US12594275B2 (en) 2019-02-07 2026-04-07 The Regents Of The University Of California Immunophilin binding agents and uses thereof
KR102994657B1 (ko) * 2019-03-15 2026-07-22 추가이 세이야쿠 가부시키가이샤 방향족 아미노산 유도체의 제조 방법
WO2021067405A1 (en) * 2019-10-01 2021-04-08 The Johns Hopkins University Neuroprotective compounds and methods of use thereof
TW202126323A (zh) * 2019-10-01 2021-07-16 約翰斯赫普金斯大學 雷帕弗辛（Ｒａｐａｆｕｃｉｎ）衍生化合物及其使用方法
WO2021071931A1 (en) 2019-10-07 2021-04-15 The Johns Hopkins University Three-dimentional surface for protein and small molecule microarrays
CN120271673A (zh) * 2024-01-08 2025-07-08 重庆医科大学 一种化合物、包含其的药物组合物及其用途

Citations (5)

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Publication number Priority date Publication date Assignee Title
CN1187127A (zh) * 1995-06-07 1998-07-08 吉尔福特药品有限公司 旋转异构酶活性抑制剂
WO1999041258A1 (en) * 1998-02-13 1999-08-19 President And Fellows Of Harvard College Novel dimerizing agents, their production and use
WO2010004304A1 (en) * 2008-06-17 2010-01-14 Biotica Technology Limited Novel compounds and methods for their production
CN103282362A (zh) * 2010-11-30 2013-09-04 约翰·霍普金斯大学 杂交环状文库和其筛选
WO2014201405A1 (en) * 2013-06-14 2014-12-18 The Board Of Regents Of The University Of Texas System Novel allosteric inhibitors of proteasome and methods of use thereof

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US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US7056935B2 (en) 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US5696135A (en) 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US6984635B1 (en) 1998-02-13 2006-01-10 Board Of Trustees Of The Leland Stanford Jr. University Dimerizing agents, their production and use
GB0417852D0 (en) * 2004-08-11 2004-09-15 Biotica Tech Ltd Production of polyketides and other natural products
US20080306098A1 (en) * 2006-11-06 2008-12-11 Mutz Mitchell W Pharmacokinetics of protease inhibitors and other drugs
EP2607352A1 (en) 2011-12-22 2013-06-26 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Pipecolate-diketoamides for treatment of psychiatric disorders
WO2017136708A1 (en) * 2016-02-04 2017-08-10 The Johns Hopkins University Synthesis and composition of rapafucin libraries

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1187127A (zh) * 1995-06-07 1998-07-08 吉尔福特药品有限公司 旋转异构酶活性抑制剂
WO1999041258A1 (en) * 1998-02-13 1999-08-19 President And Fellows Of Harvard College Novel dimerizing agents, their production and use
WO2010004304A1 (en) * 2008-06-17 2010-01-14 Biotica Technology Limited Novel compounds and methods for their production
CN103282362A (zh) * 2010-11-30 2013-09-04 约翰·霍普金斯大学 杂交环状文库和其筛选
WO2014201405A1 (en) * 2013-06-14 2014-12-18 The Board Of Regents Of The University Of Texas System Novel allosteric inhibitors of proteasome and methods of use thereof

Non-Patent Citations (4)

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Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library;Xianghong Wu et al.;《ACS Comb. Sci.》;20110719;第13卷;486-495 *
Design and synthesis of a rapamycin-based high affinity binding FKBP12 ligand;TK Chakraborty et al.;《Chemistry & Biology》;19951231;第2卷(第3期);157-161 *
Inhibition of Ras Signaling by Blocking Ras-Effector Interactions with Cyclic Peptides,;P. Upadhyaya et al.;《Angew. Chem. Int. Ed.》;20150507;第54卷;7602-7606 *
Inhibition of Ras-effector interactions by cyclic Peptides;Xianghong Wu et al.;《Med. Chem. Comm.》;20121127;第4卷;378-382 *

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Publication number Publication date
EP3411413A1 (en) 2018-12-12
JP2019510738A (ja) 2019-04-18
JP7158532B2 (ja) 2022-10-21
JP6891183B2 (ja) 2021-06-18
CN108713028A (zh) 2018-10-26
US20190092808A1 (en) 2019-03-28
WO2017136708A1 (en) 2017-08-10
JP2021138726A (ja) 2021-09-16
EP3411413A4 (en) 2019-09-18
US10662220B2 (en) 2020-05-26
AU2017214550B2 (en) 2024-03-07
MX2018009405A (es) 2018-11-09
CA3013589A1 (en) 2017-08-10
AU2017214550A1 (en) 2018-08-16

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