Modulation of the multidrug resistance P-glycoprotein: detection with technetium-99m-sestamibi in vivo.
Modulation of the multidrug resistance P-glycoprotein: detection with technetium-99m-sestamibi in vivo.
复制标题
多药耐药性 P-糖蛋白的调节：体内用 technetium-99m-sestamibi 进行检测。
DOI：
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发表时间：
1997
影响因子：
9.3
通讯作者：
D. Piwnica
中科院分区：
文献类型：
--
作者：
G. Luker;P. Fracasso;J. Dobkin;D. Piwnica
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多药耐药(MDR1)P-糖蛋白(Pgp)在几乎所有类型的人类癌症中都有过表达，在一些肿瘤中Pgp水平升高与治疗反应差有关。~(99m)Tm-Sestamibi最近被证实是一种PGP转运底物。Pgp也通常在肝细胞的胆小管表面和肾脏近端小管细胞的管腔一侧表达，而在心脏不表达。
方法
针对这些已知Pgp状态的器官，我们报告了三名难治性癌症患者在服用第二代Pgp高效调节剂SDZ PSC 833前后的99mTC-Sestamibi核素显像结果。
结果
在SDZ PSC 833治疗前，99mTC-Sestamibi核素扫描显示放射性示踪剂从肝脏和肾脏相对于心脏正常、迅速地清除。给予PGP调节剂后，99mTC-Sestamibi选择性地保留在肝脏和肾脏中。
结论
99mTC-Sestamibi对肝、胆、肾的清除是由Pgp介导的，患者体内这些器官对Pgp转运的抑制可被99mTC-Sestamibi成功地显像化。这种药物和相关的放射性药物可能会得到类似的结果，用于肿瘤中Pgp转运和调制的功能成像。
UNLABELLED
Overexpression of the multidrug resistance (MDR1) P-glycoprotein (Pgp) has been documented in nearly all forms of human cancers and increased levels of Pgp in some tumors correlate with poor response to treatment. Technetium-99m-sestamibi has recently been validated as a Pgp transport substrate. Pgp is also normally expressed along the biliary canalicular surface of hepatocytes and the luminal side of proximal tubule cells in the kidney, while not expressed in heart.
METHODS
Focused on these organs with known Pgp status, we present the findings on 99mTc-sestamibi scintigraphy of three patients with refractory cancer who were imaged before and after administration of SDZ PSC 833, a second-generation, high-potency modulator of Pgp.
RESULTS
Before treatment with SDZ PSC 833, scintigraphy using 99mTc-sestamibi showed normal, prompt clearance of the radiotracer from the liver and kidneys relative to the heart. After administration of the Pgp modulator, 99mTc-sestamibi was selectively retained in the liver and kidneys.
CONCLUSION
Hepatobiliary and renal clearance of 99mTc-sestamibi are Pgp-mediated, and inhibition of Pgp transport in these organs can be successfully imaged using 99mTc-sestamibi in patients. Similar results might be expected with this and related radiopharmaceuticals for functional imaging of Pgp transport and modulation in tumors.
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影响因子：
21.1
作者：
J. M. Ford;W. Hait
通讯作者：
J. M. Ford;W. Hait
MDR1 基因特异性单克隆抗体 C494 与丙酮酸羧化酶发生交叉反应。
影响因子：
11.2
作者：
Rao,VV;Anthony,DC;Piwnica-Worms,D
通讯作者：
Piwnica-Worms,D
影响因子：
158.5
作者：
CHAN, HSL;HADDAD, G;LING, V
通讯作者：
LING, V
影响因子：
45.3
作者：
MILLER, TP;GROGAN, TM;SALMON, SE
通讯作者：
SALMON, SE
重组人多药耐药性 P-糖蛋白在昆虫细胞中的表达可减少 technetium-99m-sestamibi 的积累。
DOI：
--
发表时间：
1994
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
Rao,VV;Chiu,ML;Kronauge,JF;Piwnica-Worms,D
通讯作者：
Piwnica-Worms,D