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Structural insights into the dual-targeting mechanism of Nutlin-3

หน่วยงาน Nanyang Technological University, Singapore

รายละเอียด

ชื่อเรื่อง : Structural insights into the dual-targeting mechanism of Nutlin-3
นักวิจัย : Shin, Jae-Sun , Ha, Ji-Hyang , He, Fahu , Muto, Yutaka , Ryu, Kyoung-Seok , Yoon, Ho Sup , Kang, Sunghyun , Park, Sung Goo , Park, Byoung Chul , Choi, Sang-Un , Chi, Seung-Wook
คำค้น : DRNTU::Science::Biological sciences.
หน่วยงาน : Nanyang Technological University, Singapore
ผู้ร่วมงาน : -
ปีพิมพ์ : 2555
อ้างอิง : Shin, J.-S., Ha, J.-H., He, F., Muto, Y., Ryu, K.-S., Yoon, H. S., et al. (2012). Structural insights into the dual-targeting mechanism of Nutlin-3. Biochemical and Biophysical Research Communications, 420(1), 48-53. , 0006-291X , http://hdl.handle.net/10220/11029 , http:dx.doi.org/10.1016/j.bbrc.2012.02.113
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : Biochemical and biophysical research communications
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Multi-targeting therapy is an emerging strategy of drug discovery to improve therapeutic efficacy, safety and resistance profiles. In this study, we monitored the binding of a potent MDM2 inhibitor Nutlin-3 with anti-apoptotic Bcl-2 family proteins using NMR spectroscopy. Our results showed the universal binding of Nutlin-3 with diverse anti-apoptotic Bcl-2 family proteins. Taken together with the binding data for Nutlin-3 analogs, the structural model of the Bcl-XL/Nutlin-3 complex showed that the binding mode of Nutlin-3 resembles that of the Bcl-XL/Bcl-2 inhibitors, suggesting the molecular mechanism of transcription-independent mitochondrial apoptosis by Nutlin-3. Finally, our structural comparison provides structural insights into the dual-targeting mechanism of how Nutlin-3 can bind to two different target proteins, MDM2 and anti-apoptotic Bcl-2 family proteins in a similar manner.

บรรณานุกรม :
Shin, Jae-Sun , Ha, Ji-Hyang , He, Fahu , Muto, Yutaka , Ryu, Kyoung-Seok , Yoon, Ho Sup , Kang, Sunghyun , Park, Sung Goo , Park, Byoung Chul , Choi, Sang-Un , Chi, Seung-Wook . (2555). Structural insights into the dual-targeting mechanism of Nutlin-3.
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Shin, Jae-Sun , Ha, Ji-Hyang , He, Fahu , Muto, Yutaka , Ryu, Kyoung-Seok , Yoon, Ho Sup , Kang, Sunghyun , Park, Sung Goo , Park, Byoung Chul , Choi, Sang-Un , Chi, Seung-Wook . 2555. "Structural insights into the dual-targeting mechanism of Nutlin-3".
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Shin, Jae-Sun , Ha, Ji-Hyang , He, Fahu , Muto, Yutaka , Ryu, Kyoung-Seok , Yoon, Ho Sup , Kang, Sunghyun , Park, Sung Goo , Park, Byoung Chul , Choi, Sang-Un , Chi, Seung-Wook . "Structural insights into the dual-targeting mechanism of Nutlin-3."
    กรุงเทพมหานคร : Nanyang Technological University, Singapore, 2555. Print.
Shin, Jae-Sun , Ha, Ji-Hyang , He, Fahu , Muto, Yutaka , Ryu, Kyoung-Seok , Yoon, Ho Sup , Kang, Sunghyun , Park, Sung Goo , Park, Byoung Chul , Choi, Sang-Un , Chi, Seung-Wook . Structural insights into the dual-targeting mechanism of Nutlin-3. กรุงเทพมหานคร : Nanyang Technological University, Singapore; 2555.