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

Info

Publication number
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
Authority
CN
China
Prior art keywords
dmphe
pro
sub
mval
ala
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201780010182.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN108713028A (zh
Inventor
J·刘
J·王
Z·郭
萨姆·洪
刘武坤
彭汉景
马尼沙·达斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Johns Hopkins University
Original Assignee
Johns Hopkins University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Johns Hopkins University filed Critical Johns Hopkins University
Publication of CN108713028A publication Critical patent/CN108713028A/zh
Application granted granted Critical
Publication of CN108713028B publication Critical patent/CN108713028B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • G01N33/574—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (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)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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

Family

ID=59501078

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780010182.2A Active CN108713028B (zh) 2016-02-04 2017-02-03 rapafucin文库的合成和组合物

Country Status (8)

Country Link
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 (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2813512B1 (en) 2011-12-28 2021-03-31 Chugai Seiyaku Kabushiki Kaisha Peptide-compound cyclization method
DK3269809T3 (da) 2015-03-13 2022-09-12 Chugai Pharmaceutical Co Ltd MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF
EP3411046B1 (en) 2016-02-04 2025-07-16 The Johns Hopkins University Rapaglutins, novel inhibitors of glut and use thereof
CN108713028B (zh) * 2016-02-04 2021-12-28 约翰霍普金斯大学 rapafucin文库的合成和组合物
AU2017214557B2 (en) * 2016-02-04 2022-05-19 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses 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
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
US20220372014A1 (en) * 2019-10-01 2022-11-24 The Johns Hopkins University Neuroprotective compounds and methods of use thereof
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN108713028B (zh) 2016-02-04 2021-12-28 约翰霍普金斯大学 rapafucin文库的合成和组合物

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)

* Cited by examiner, † Cited by third party
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 *

Also Published As

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

Similar Documents

Publication Publication Date Title
CN108713028B (zh) rapafucin文库的合成和组合物
Powell et al. Selective degradation of GSPT1 by cereblon modulators identified via a focused combinatorial library
Olsen et al. Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic α3β-tetrapeptides
Mobley et al. Predicting binding free energies: frontiers and benchmarks
Robbins et al. Discovery and preclinical pharmacology of NX-2127, an orally bioavailable degrader of Bruton’s tyrosine kinase with immunomodulatory activity for the treatment of patients with B cell malignancies
Matthew et al. Lyngbyastatin 4, a dolastatin 13 analogue with elastase and chymotrypsin inhibitory activity from the marine cyanobacterium Lyngbya confervoides
Di Bonaventura et al. Chemical space guided discovery of antimicrobial bridged bicyclic peptides against Pseudomonas aeruginosa and its biofilms
Itoh et al. Chemical construction and structural permutation of potent cytotoxin polytheonamide B: discovery of artificial peptides with distinct functions
Gunasekaran et al. Development of a polo-like kinase-1 polo-box domain inhibitor as a tumor growth suppressor in mice models
Wu et al. Creating diverse target-binding surfaces on FKBP12: synthesis and evaluation of a rapamycin analogue library
Marini et al. Investigation into the Use of Encorafenib to Develop Potential PROTACs Directed against BRAFV600E Protein
Bahatheg et al. Short tryptamine-based peptoids as potential therapeutics for microbial keratitis: Structure-function correlation studies
CN107033100B (zh) 一种苯并噻唑衍生物、制备方法及其医药用途
Kumaresan et al. Synthesis and characterization of a novel inhibitor of C-reactive protein–mediated proinflammatory effects
WO2005110456A2 (en) T-cell death-inducing epitopes
Koay et al. Blocking the heat shock response and depleting HSF-1 levels through heat shock protein 90 (hsp90) inhibition: a significant advance on current hsp90 chemotherapies
Boudou et al. Synthesis, characterization, antimicrobial activity, and in silico assessment of a novel pyrazoline carboxamide heterocyclic compound
Xu et al. Short divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers
Booth et al. Unmasking ligand binding motifs: identification of a chemokine receptor motif by NMR studies of antagonist peptides
Georgiou et al. Conformational Properties and Putative Bioactive Targets for Novel Thiosemicarbazone Derivatives
CN105997992A (zh) 化合物dy1在制备抗大肠癌药物中的应用
Hungerford et al. Interaction of Clitoria ternatea L. flower extract with alpha-amylase by photon streaming time-resolved fluorescence
Belcher Chemoproteomic Strategies for Drug Discovery and Natural Product Target Identification
Soini Identification of molecular glues of 14-3-3 Protein-Protein Interactions
Rouzi et al. Novel 1, 3, 4‐Oxadiazole Acetamide Derivatives as Potential Antimicrobial Agents: Design, Synthesis, Biological Evaluation, and Molecular Modelling Studies

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant