Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization

被引：5
|
作者：
Gilliam, Amanda J. H. [1 ]
Smith, Joshua N. [2 ]
Flather, Dylan [2 ]
Johnston, Kevin M. [1 ]
Gansmiller, Andrew M. [1 ]
Fishman, Dmitry A. [1 ]
Edgar, Joshua M. [1 ]
Balk, Mark [1 ,3 ]
Majumdar, Sudipta [1 ]
Weiss, Gregory A. [1 ,2 ]
机构：
[1] Univ Calif Irvine, Dept Chem, Irvine, CA 92697 USA
[2] Univ Calif Irvine, Dept Mol Biol & Biochem, Irvine, CA 92697 USA
[3] Eindhoven Univ Technol, Den Dolech 2, NL-5612 AZ Eindhoven, Netherlands
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 59卷 / 08期
关键词：
SPOT-SYNTHESIS; SCAFFOLDING DOMAIN; LIPID RAFTS; PROTEIN; BINDING; PEPTIDE; CELLS; CHOLESTEROL; PARALLEL; SUPPORT;
D O I：
10.1021/acs.jmedchem.5b01536
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Caveoliu-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide W147 (1), a small, high-affinity, selective disrupter of caveolin-1 oligomers. Developed and optimized through screening and analysis of synthetic peptide libraries, ligand 1 has 7500 -fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. Ligand 1 will permit targeted study of caveoliri-1 function.
引用
收藏
页码：4019 / 4025
页数：7
相关论文
共 50 条
  • [31] CAVEOLIN-1 IN HUMAN PREECLAMPTIC PLACENTAS
    Mauricio, Castro-Parodi
    Aban, Cintya
    Nora, Martinez
    Vanesa, Herlax
    Sabina, Mate
    Mariana, Farina
    Damiano Alicia, E.
    PLACENTA, 2015, 36 (04) : 514 - 514
  • [32] Nestin and caveolin-1 in the diagnosis of GISTs
    Enache, Simona
    Arsene, D.
    Iosif, Cristina
    Stoicea, M.
    Grigore, Alina
    Petrescu, Angela
    Enache, V.
    Ardeleanu, Carmen
    ROMANIAN JOURNAL OF MORPHOLOGY AND EMBRYOLOGY, 2012, 53 (01): : 41 - 46
  • [33] Caveolin-1与组织再生
    杨婷
    刘东生
    丁隆
    曲义坤
    路艳
    杨宇
    中国民康医学, 2010, 22 (10) : 1313 - 1314
  • [34] Caveolin-1 regulation of experimental colitis
    Greer, James Joshua M.
    Chidlow, John H.
    Bernatchez, Pascal N.
    Sessa, William C.
    Shukla, Deepti
    Kevil, Christopher G.
    GASTROENTEROLOGY, 2006, 130 (04) : A555 - A555
  • [35] Probing the structure and topology of caveolin-1
    Glover, Kerney
    FASEB JOURNAL, 2014, 28 (01):
  • [36] Involvement of caveolin-1 in skin diseases
    Takamura, Naoko
    Yamaguchi, Yukie
    FRONTIERS IN IMMUNOLOGY, 2022, 13
  • [37] The Role of Caveolin-1 in Retinal Inflammation
    Gurley, Jami M.
    Elliott, Michael H.
    RETINAL DEGENERATIVE DISEASES: MECHANISMS AND EXPERIMENTAL THERAPY, 2019, 1185 : 169 - 173
  • [38] Caveolin-1 stops profibrogenic signaling?
    Kim, Hong Pyo
    Choi, Augustine M. K.
    AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY, 2008, 294 (05) : L841 - L842
  • [39] Caveolin-1 in sarcomas: friend or foe?
    Sainz-Jaspeado, Miguel
    Martin-Liberal, Juan
    Lagares-Tena, Laura
    Mateo-Lozano, Silvia
    Garcia del Muro, Xavier
    Tirado, Oscar M.
    ONCOTARGET, 2011, 2 (04) : 305 - 312
  • [40] Caveolin-1 in oncogenic metabolic symbiosis
    Raudenska, Martina
    Gumulec, Jaromir
    Balvan, Jan
    Masarik, Michal
    INTERNATIONAL JOURNAL OF CANCER, 2020, 147 (07) : 1793 - 1807
12345