リガンド
リガンド
出典: フリー百科事典『ウィキペディア(Wikipedia)』 (2021/05/10 13:30 UTC 版)
生化学や薬理学では、リガンド(Ligand; ライガンド)とは生体分子と複合体を形成して生物学的な目的を果たす物質のことを指す。 タンパク質-リガンド結合では、リガンドは通常、標的タンパク質上の結合部位に結合することでシグナルを生成する分子である。 この結合は、通常、標的タンパク質の配座異性体(コンフォメーション)の変化をもたらす。 DNA-リガンド結合研究では、リガンドはDNA二重らせんに結合する低分子、イオン[1]、タンパク質[2]のいずれかである。 リガンドと結合相手の関係は、電荷、疎水性、分子構造の関数である。 結合のインスタンスは、時間と空間の無限の範囲で発生するので、その速度定数は通常、非常に小さな数である。
- ^ “Ligand-induced DNA condensation: choosing the model”. Biophysical Journal 89 (4): 2574–87. (October 2005). Bibcode: 2005BpJ....89.2574T. doi:10.1529/biophysj.105.063909. PMC 1366757. PMID 16085765 .
- ^ “Statistical-mechanical lattice models for protein-DNA binding in chromatin”. Journal of Physics: Condensed Matter 22 (41): 414105. (October 2010). arXiv:1004.5514. Bibcode: 2010JPCM...22O4105T. doi:10.1088/0953-8984/22/41/414105. PMID 21386588.
- ^ “Water in cavity-ligand recognition”. Journal of the American Chemical Society 132 (34): 12091–7. (September 2010). doi:10.1021/ja1050082. PMC 2933114. PMID 20695475 .
- ^ “The difference between Ki, Kd, IC50, and EC50 values”. The Science Snail (2019年12月31日). 2020年7月19日閲覧。
- ^ See Homologous competitive binding curves Archived 2007-12-19 at the Wayback Machine., A complete guide to nonlinear regression, curvefit.com.
- ^ “Optical thermophoresis for quantifying the buffer dependence of aptamer binding”. Angewandte Chemie 49 (12): 2238–41. (March 2010). doi:10.1002/anie.200903998. PMID 20186894 (February 24, 2010).
- ^ “Protein-binding assays in biological liquids using microscale thermophoresis”. Nature Communications 1 (7): 100. (October 2010). Bibcode: 2010NatCo...1..100W. doi:10.1038/ncomms1093. PMID 20981028.
- ^ Vu-Quoc, L., Configuration integral (statistical mechanics), 2008. this wiki site is down; see this article in the web archive on 2012 April 28.
- ^ Kenakin, Terrance P. (November 2006). A pharmacology primer: theory, applications, and methods. Academic Press. p. 79. ISBN 978-0-12-370599-0
- ^ Cabanos, C; Wang, M; Han, X; Hansen, SB (8 August 2017). “A Soluble Fluorescent Binding Assay Reveals PIP2 Antagonism of TREK-1 Channels.”. Cell Reports 20 (6): 1287–1294. doi:10.1016/j.celrep.2017.07.034. PMC 5586213. PMID 28793254 .
- ^ a b Matera, Carlo; Pucci, Luca; Fiorentini, Chiara; Fucile, Sergio; Missale, Cristina; Grazioso, Giovanni; Clementi, Francesco; Zoli, Michele et al. (2015-08-28). “Bifunctional compounds targeting both D2 and non-α7 nACh receptors: Design, synthesis and pharmacological characterization”. European Journal of Medicinal Chemistry 101: 367–383. doi:10.1016/j.ejmech.2015.06.039. PMID 26164842.
- ^ Matera, Carlo; Flammini, Lisa; Quadri, Marta; Vivo, Valentina; Ballabeni, Vigilio; Holzgrabe, Ulrike; Mohr, Klaus; De Amici, Marco et al. (2014-03-21). “Bis(ammonio)alkane-type agonists of muscarinic acetylcholine receptors: Synthesis, in vitro functional characterization, and in vivo evaluation of their analgesic activity”. European Journal of Medicinal Chemistry 75: 222–232. doi:10.1016/j.ejmech.2014.01.032. PMID 24534538.
- ^ “Narcotic antagonistic potency of bivalent ligands which contain beta-naltrexamine. Evidence for bridging between proximal recognition sites”. Journal of Medicinal Chemistry 25 (7): 847–9. (July 1982). doi:10.1021/jm00349a016. PMID 7108900.
- ^ “Opioid agonist and antagonist bivalent ligands as receptor probes”. Life Sciences 31 (12–13): 1283–6. (1982). doi:10.1016/0024-3205(82)90362-9. PMID 6292615.
- ^ “Heteromer Induction: An Approach to Unique Pharmacology?”. ACS Chemical Neuroscience 8 (3): 426–428. (January 2017). doi:10.1021/acschemneuro.7b00002. PMID 28139906.
- ^ “Gonadotropin-releasing hormone stimulation of luteinizing hormone release: A ligand-receptor-effector model”. Proceedings of the National Academy of Sciences of the United States of America 79 (23): 7307–11. (December 1982). Bibcode: 1982PNAS...79.7307B. doi:10.1073/pnas.79.23.7307. JSTOR 13076. PMC 347328. PMID 6296828 .
- ^ “Conversion of a gonadotropin-releasing hormone antagonist to an agonist”. Nature 296 (5858): 653–5. (April 1982). Bibcode: 1982Natur.296..653C. doi:10.1038/296653a0. PMID 6280058.
- ^ “Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB₂R selective benzimidazoles reveal unexpected intrinsic properties”. Bioorganic & Medicinal Chemistry 22 (15): 3938–46. (August 2014). doi:10.1016/j.bmc.2014.06.008. PMID 24984935.
- ^ “Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers”. Journal of Medicinal Chemistry 50 (18): 4482–92. (September 2007). doi:10.1021/jm070552t. PMID 17676726.
- ^ “Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies”. Journal of Medicinal Chemistry 48 (20): 6220–8. (October 2005). doi:10.1021/jm050234z. PMID 16190749.
- ^ a b “Design and Characterization of Superpotent Bivalent Ligands Targeting Oxytocin Receptor Dimers via a Channel-Like Structure”. Journal of Medicinal Chemistry 59 (15): 7152–66. (August 2016). doi:10.1021/acs.jmedchem.6b00564. PMID 27420737.
- ^ “A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NH2 versus the Bivalent Agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp-NH2: A Bivalent Advantage”. ACS Chemical Neuroscience 8 (6): 1262–1278. (February 2017). doi:10.1021/acschemneuro.6b00399. PMC 5679024. PMID 28128928 .
- ^ a b “Heterobivalent ligands target cell-surface receptor combinations in vivo”. Proceedings of the National Academy of Sciences of the United States of America 109 (52): 21295–300. (December 2012). Bibcode: 2012PNAS..10921295X. doi:10.1073/pnas.1211762109. JSTOR 42553664. PMC 3535626. PMID 23236171 .
- ^ a b “An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers”. Journal of Medicinal Chemistry 59 (7): 3112–28. (April 2016). doi:10.1021/acs.jmedchem.5b01894. PMC 5679017. PMID 26959173 .
- ^ “Design strategies for bivalent ligands targeting GPCRs”. ChemMedChem 6 (6): 963–74. (June 2011). doi:10.1002/cmdc.201100101. PMID 21520422.
- ^ “Bivalent ligands as specific pharmacological tools for G protein-coupled receptor dimers”. Current Drug Discovery Technologies 5 (4): 312–8. (December 2008). doi:10.2174/157016308786733591. PMID 19075611.
- ^ “Inhibition of Inflammatory and Neuropathic Pain by Targeting a Mu Opioid Receptor/Chemokine Receptor5 Heteromer (MOR-CCR5)”. Journal of Medicinal Chemistry 58 (21): 8647–57. (November 2015). doi:10.1021/acs.jmedchem.5b01245. PMC 5055304. PMID 26451468 .
- ^ “Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series”. Proceedings of the National Academy of Sciences of the United States of America 102 (52): 19208–13. (December 2005). Bibcode: 2005PNAS..10219208D. doi:10.1073/pnas.0506627102. JSTOR 4152590. PMC 1323165. PMID 16365317 .
- ^ “Targeting putative mu opioid/metabotropic glutamate receptor-5 heteromers produces potent antinociception in a chronic murine bone cancer model”. European Journal of Pharmacology 743: 48–52. (November 2014). doi:10.1016/j.ejphar.2014.09.008. PMC 4259840. PMID 25239072 .
- ^ “Ligand Binding Site Structure Shapes Folding, Assembly and Degradation of Homomeric Protein Complexes.”. Journal of Molecular Biology 431 (19): 3871-3888. (2019). doi:10.1016/j.jmb.2019.07.014. PMC 6739599. PMID 31306664 .
- ^ “Ligand Binding Site Structure Influences the Evolution of Protein Complex Function and Topology.”. Cell Reports 22 (12): 3265-3276. (2018). doi:10.1016/j.celrep.2018.02.085. PMC 5873459. PMID 29562182 .
- ^ “Ligand-Binding-Site Structure Shapes Allosteric Signal Transduction and the Evolution of Allostery in Protein Complexes.”. Molecular Biology and Evolution 36 (8): 1711-1727. (2019). doi:10.1093/molbev/msz093. PMC 6657754. PMID 31004156 .
- ^ “Privileged scaffolds for library design and drug discovery”. Current Opinion in Chemical Biology 14 (3): 347–61. (June 2010). doi:10.1016/j.cbpa.2010.02.018. PMC 2908274. PMID 20303320 .
- ^ “BioCores: identification of a drug/natural product-based privileged structural motif for small-molecule lead discovery”. Molecular Diversity 14 (1): 193–200. (February 2010). doi:10.1007/s11030-009-9157-5. PMID 19468851.
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