(Lys(DOTA)4)BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.

Guerin B; Dumulon Perreault V; Tremblay M

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(Lys(DOTA)4)BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.

机译：（Lys（DOTA）4）BVD15，一种新型且有效的神经肽Y类似物，设计用于针对Y1受体的乳腺肿瘤成像。

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We substituted a truncated neuropeptide Y (NPY) analog, [Pro(30), Tyr(32), Leu(34)]NPY(28-36)NH(2) also called BVD15, at various positions with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7-10-tetraacetic acid) and evaluated the effect of the coupling position with the binding affinity for NPY Y(1) receptors (NPY1R). Our data suggest that [Lys(DOTA)(4)]BVD15 (K(i)=63+/-25 nM vs. K(i)=39+/-34 nM for BVD15) is a potent NPY analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.

机译：我们用DOTA（1,4）在各个位置替换了截短的神经肽Y（NPY）类似物[Pro（30），Tyr（32），Leu（34）] NPY（28-36）NH（2），也称为BVD15 ，7,10-四氮杂十二烷-1,4,7-10-四乙酸），并评估偶联位置对NPY Y（1）受体（NPY1R）的结合亲和力的影响。我们的数据表明[Lys（DOTA）（4）] BVD15（BVD15的K（i）= 63 +/- 25 nM vs. K（i）= 39 +/- 34 nM）是适用于放射性标记的有效NPY类似物与金属正电子发射体一起用于乳腺癌的PET成像。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共4页
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Guerin B; Dumulon Perreault V; Tremblay M;
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1. (Lys(DOTA)4)BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging. [J] . Guerin B, Dumulon Perreault V, Tremblay M Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：（Lys（DOTA）4）BVD15，一种新型且有效的神经肽Y类似物，设计用于针对Y1受体的乳腺肿瘤成像。
2. HYNIC and DOMA conjugated radiolabeled bombesin analogs as receptor-targeted probes for scintigraphic detection of breast tumor [J] . Kakali De, Dibyanti Mukherjee, Samarendu Sinha, EJNMMI Research . 2019,第1期

机译：HYNIC和DOMA缀合的放射性标记的蛙皮素类似物作为受体闪烁探针，用于乳腺闪烁扫描
3. Preclinical Comparison of (111)In-Labeled DTPA- or DOTA-Bombesin Analogs for Receptor-Targeted Scintigraphy and Radionuclide Therapy. [J] . Breeman WA, De Jong M, Erion JL, The Journal of Nuclear Medicine . 2002,第12期

机译：临床前比较（111）贴有标签的DTPA或DOTA-Bombesin类似物在受体靶向闪烁显像和放射性核素治疗中的作用。
4. Synthesis and Characterization of DOTA-Coupled Bimeric Y1 Receptors Antagonists for Breast Cancer Targeting [C] . David Chateeet, Renzo Cescato, Beatrice Waser American Peptide Symposium . 2011

机译：乳腺癌靶向乳腺癌靶向乳腺癌拮抗剂的合成与表征
5. Part I. Synthetic efforts towards a total synthesis of Haterumalide NA/Oocydin A. Part II. Deciphering the coupling constants of Spiruchostatins A and B. Part III. Design and synthesis of analogs of Latrunculin A and B, potent actin polymerization inhibitors. [D] . Wang, Jizhou. 2005

机译：第一部分：为完全合成Haterumalide NA / Oocydin A的合成努力。第二部分。破译螺旋藻抑素A和B的偶联常数。第三部分。设计和合成Latrunculin A和B，强肌动蛋白聚合抑制剂的类似物。
6. HYNIC and DOMA conjugated radiolabeled bombesin analogs as receptor-targeted probes for scintigraphic detection of breast tumor [O] . Kakali De, Dibyanti Mukherjee, Samarendu Sinha, 2019

机译：HYNIC和DOMA缀合的放射性标记的boombins类似物作为受体闪烁探针用于乳腺闪烁扫描
7. Potent neuropeptide Y Y1 receptor antagonist, 1229U91: blockade of neuropeptide Y-induced and physiological food intake. [O] . A Kanatani, A Ishihara, S Asahi, 1996

机译：有效的神经肽Y Y1受体拮抗剂，1229U91：阻断神经肽Y诱导和生理食物摄入量。
8. Beta-Amino Acid Analogs of an Insect Neuropeptide Feature Potent Bioactivity and Resistance to Peptidase Hydrolysis [R] . Zubrzak, P., Williams, H., Coast, G. M., 2006

机译：昆虫神经肽的β-氨基酸类似物具有强效生物活性和对肽酶水解的抗性

(Lys(DOTA)4)BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.

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