受容体二量体化、レセプター二量体化

WordNet

a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

=sense organ / 受信装置

UpToDate Contents

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1. インスリン受容体の構造および機能structure and function of the insulin receptor [show details]
… homologous IGF-I receptor provides compelling evidence that in the unliganded receptor the extracellular domain serves to prevent dimerization of the transmembrane domains and hence dimerization and activation …
2. 選択的エストロゲン受容体モジュレーター・受容体ダウンレギュレーターの作用機序mechanisms of action of selective estrogen receptor modulators and down regulators [show details]
…ligands and SERMs, causes dissociation of the receptor from its heat-shock chaperone proteins. However, because of its long side chain, receptor dimerization is sterically hindered and rapid proteasome-dependent …
3. HER2陰性ホルモン受容体陽性転移性乳癌への治療法：内分泌療法および分子標的薬treatment approach to metastatic hormone receptor positive her2 negative breast cancer endocrine therapy and targeted agents [show details]
… strategies. Fulvestrant is an estrogen receptor (ER) antagonist that blocks ER dimerization and DNA binding, increases ER turnover, and inhibits nuclear uptake of the receptor . Because it blocks ER function …
4. エストロゲン作用の分子生物学および生理学molecular biology and physiology of estrogen action [show details]
… affinity and specificity , with one receptor molecule in contact with each five-base-pair segment of the response element . Dimerization of ER complexes is facilitated by receptor binding to a response element …
5. トロンボポエチンの生物学および生理学biology and physiology of thrombopoietin [show details]
…presence of approximately 56 ± 17 receptors per human platelet with an affinity of 163 ± 31 pmol/L . Upon binding to thrombopoietin, the receptor undergoes dimerization that results in a number of signal …

English Journal

ERα dimerization: a key factor for the weak estrogenic activity of an ERα modulator unable to compete with estradiol in binding assays.

Leclercq G1, Laïos I1, Elie-Caille C2, Leiber D3,4, Laurent G5, Lesniewska E6, Tanfin Z3, Jacquot Y7.
Journal of receptor and signal transduction research.J Recept Signal Transduct Res.2017 Apr;37(2):149-166. doi: 10.1080/10799893.2016.1203940. Epub 2016 Jul 12.
Estrothiazine (ESTZ) is a weak estrogen sharing structural similarities with coumestrol. ESTZ failed to compete with [3H]17β-estradiol ([3H]17β-E2) for binding to the estrogen receptor α (ERα), questioning its ability to interact with the receptor. However, detection by atomic force spectroscopy
PMID 27400858

Engineered Multivalency Enhances Affibody-Based HER3 Inhibition and Downregulation in Cancer Cells.

Schardt JS, Oubaid JM, Williams SC, Howard JL, Aloimonos CM, Bookstaver ML, Lamichhane TN, Sokic S, Liyasova MS, O'Neill M, Andresson T, Hussain A, Lipkowitz S, Jay SM.
Molecular pharmaceutics.Mol Pharm.2017 Mar 1. doi: 10.1021/acs.molpharmaceut.6b00919. [Epub ahead of print]
The receptor tyrosine kinase HER3 has emerged as a therapeutic target in ovarian, prostate, breast, lung and other cancers due to its ability to potently activate the PI3K/Akt pathway, especially via dimerization with HER2, as well as for its role in mediating drug resistance. Enhanced efficacy of H
PMID 28248115

An update on the physiological and therapeutic relevance of GPCR oligomers.

Farran B1.
Pharmacological research.Pharmacol Res.2017 Mar;117:303-327. doi: 10.1016/j.phrs.2017.01.008. Epub 2017 Jan 11.
The traditional view on GPCRs held that they function as single monomeric units composed of identical subunits. This notion was overturned by the discovery that GPCRs can form homo- and hetero-oligomers, some of which are obligatory, and can further assemble into receptor mosaics consisting of three
PMID 28087443