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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (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)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Food Science & Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Magnetic Resonance Imaging Apparatus (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 (https=)
EP (1) EP3411413A4 (https=)
JP (2) JP6891183B2 (https=)
CN (1) CN108713028B (https=)
AU (1) AU2017214550B2 (https=)
CA (1) CA3013589A1 (https=)
MX (1) MX2018009405A (https=)
WO (1) WO2017136708A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI787670B (zh) 2011-12-28 2022-12-21 日商中外製藥股份有限公司 具有環狀部之胜肽化合物及其醫藥組成物
DK3269809T3 (da) 2015-03-13 2022-09-12 Chugai Pharmaceutical Co Ltd MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF
MX2018009405A (es) * 2016-02-04 2018-11-09 Univ Johns Hopkins Sintesis y composicion de bibliotecas de rapafucina.
US10774110B2 (en) * 2016-02-04 2020-09-15 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
CA3013783A1 (en) 2016-02-04 2017-08-10 The Johns Hopkins University Rapaglutins, novel inhibitors of glut and use thereof
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
US12391971B2 (en) 2017-01-31 2025-08-19 Chugai Seiyaku Kabushiki Kaisha Method for synthesizing peptides in cell-free translation system
JP7232758B2 (ja) * 2017-06-09 2023-03-06 中外製薬株式会社 膜透過性の高い環状ペプチド化合物、及びこれを含むライブラリ
WO2020163594A1 (en) 2019-02-07 2020-08-13 The Regents Of The University Of California Immunophilin binding agents and uses thereof
KR20210139366A (ko) * 2019-03-15 2021-11-22 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
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)

* 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

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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
US5696135A (en) 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US7056935B2 (en) 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
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
MX2018009405A (es) 2016-02-04 2018-11-09 Univ Johns Hopkins Sintesis y composicion de bibliotecas de rapafucina.

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

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