Dopamine Receptor D5 is a Modulator of Tumor Response to Dopamine Receptor D2 Antagonism

Prabhu Varun V.; Madhukar Neel S.; Gilvary Coryandar; Kline C. Leah B.; Oster Sophie; El-Deiry Wafik S.; Elemento Olivier; Doherty Faye; VanEngelenburg Alexander; Durrant Jessica; Tarapore Rohinton S.; Deacon Sean; Charter Neil; Jung Jinkyu; Park Deric M.; Gilbert Mark R.; Rusert Jessica; Wechsler-Reya Robert; Arrillaga-Romany Isabel; Batchelor Tracy T.; Wen Patrick Y.; Oster Wolfgang; Allen Joshua E.

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Dopamine Receptor D5 is a Modulator of Tumor Response to Dopamine Receptor D2 Antagonism

机译：多巴胺受体D5是对多巴胺受体D2拮抗作用的肿瘤反应的调节剂

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Purpose: Dopamine receptor D2 (DRD2) is a G protein-coupled receptor antagonized by ONC201, an anticancer small molecule in clinical trials for high-grade gliomas and other malignancies. DRD5 is a dopamine receptor family member that opposes DRD2 signaling. We investigated the expression of these dopamine receptors in cancer and their influence on tumor cell sensitivity to ONC201.

机译：目的：多巴胺受体D2（DRD2）是由ONC201拮抗的G蛋白偶联受体，抗癌小分子在临床试验中为高级胶质瘤和其他恶性肿瘤。 DRD5是一种二巴胺受体家庭成员，反对DRD2信号传导。我们研究了这些多巴胺受体在癌症中的表达及其对肿瘤细胞敏感性对ONC201的影响。

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《Clinical cancer research: an official journal of the American Association for Cancer Research》 |2019年第7期|共9页
作者
Prabhu Varun V.; Madhukar Neel S.; Gilvary Coryandar; Kline C. Leah B.; Oster Sophie; El-Deiry Wafik S.; Elemento Olivier; Doherty Faye; VanEngelenburg Alexander; Durrant Jessica; Tarapore Rohinton S.; Deacon Sean; Charter Neil; Jung Jinkyu; Park Deric M.; Gilbert Mark R.; Rusert Jessica; Wechsler-Reya Robert; Arrillaga-Romany Isabel; Batchelor Tracy T.; Wen Patrick Y.; Oster Wolfgang; Allen Joshua E.;
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作者单位

Oncoceutics Inc Philadelphia PA 19104 USA;

Weill Cornell Med Coll New York NY USA;

Weill Cornell Med Coll New York NY USA;

Fox Chase Canc Ctr 7701 Burholme Ave Philadelphia PA 19111 USA;

Fox Chase Canc Ctr 7701 Burholme Ave Philadelphia PA 19111 USA;

Fox Chase Canc Ctr 7701 Burholme Ave Philadelphia PA 19111 USA;

Weill Cornell Med Coll New York NY USA;

HistoTox Labs Inc Boulder CO USA;

HistoTox Labs Inc Boulder CO USA;

HistoTox Labs Inc Boulder CO USA;

Oncoceutics Inc Philadelphia PA 19104 USA;

Eurofins DiscoverX Corp Fremont CA USA;

Eurofins DiscoverX Corp Fremont CA USA;

NCI Neurooncol Branch NIH Bethesda MD 20892 USA;

Univ Chicago Chicago IL 60637 USA;

NCI Neurooncol Branch NIH Bethesda MD 20892 USA;

Sanford Burnham Prebys Med Discovery Inst La Jolla CA USA;

Sanford Burnham Prebys Med Discovery Inst La Jolla CA USA;

Massachusettes Gen Hosp Boston MA USA;

Massachusettes Gen Hosp Boston MA USA;

Dana Farber Canc Inst Boston MA 02115 USA;

Oncoceutics Inc Philadelphia PA 19104 USA;

Oncoceutics Inc Philadelphia PA 19104 USA;

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正文语种 eng
中图分类肿瘤学;
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1. Dopamine Receptor D5 is a Modulator of Tumor Response to Dopamine Receptor D2 Antagonism [J] . Prabhu Varun V., Madhukar Neel S., Gilvary Coryandar, Clinical cancer research: an official journal of the American Association for Cancer Research . 2019,第7期

机译：多巴胺受体D5是对多巴胺受体D2拮抗作用的肿瘤反应的调节剂
2. Dopamine activity in the lateral anterior hypothalamus modulates AAS-induced aggression through D2 but not D5 receptors [J] . Schwartzer J.J., Melloni R.H. Behavioral neuroscience . 2010,第5期

机译：下丘脑外侧前部的多巴胺活性通过D2而非D5受体调节AAS诱导的攻击
3. Estrogen increases the sensitivity of ovariectomized rats to the disruptive effects produced by antagonism of D2 but not D1 dopamine receptors during performance of a response learning task. [J] . Daniel JM, Sulzer JK, Hulst JL Hormones and behavior . 2006,第1期

机译：雌激素增加了卵巢切除大鼠对D2（而不是D1多巴胺）受体拮抗作用所产生的破坏性作用的敏感性，该反应是在学习过程中进行的。
4. Inverse agonism at dopamine D2 receptors: a receptor recalcitrant to high levels of constitutive activation [C] . Thierry Wurch, Elisa A. Boutet-Robinet, Petrus J. Pauwels Fundaci髇 Dr. Antonio Esteve . 2003

机译：多巴胺D2受体的反向激动：一种受体顽固到高水平的组成型活化
5. Deconstructing G Protein-Coupled Receptor Dimer Pharmacology: Case Studies in Dopamine D1 and D2 Receptors. [D] . Yano, Hideaki. 2012

机译：解构G蛋白偶联受体二聚体药理学：多巴胺D1和D2受体的案例研究。
6. Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors generates intracellular calcium signaling by different mechanisms [O] . Ahmed Hasbi, Brian F. O’Dowd, Susan R. George -1

机译：多巴胺D2受体与多巴胺D1或D5受体的Heteromerization生成由不同的机制的细胞内钙信号传导
7. Dopamine Receptor D5 is a Modulator of Tumor Response to Dopamine Receptor D2 Antagonism [O] . Varun V. Prabhu, Neel S. Madhukar, Coryandar Gilvary, 2018

机译：多巴胺受体D5是对多巴胺受体D2拮抗作用的肿瘤反应的调节剂

Dopamine Receptor D5 is a Modulator of Tumor Response to Dopamine Receptor D2 Antagonism

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