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Potency and Selectivity of SMAC/DIABLO Mimetics in Solid Tumor Therapy

Laboratory of Cancer Biology and Epigenetics, Department of Cell Biology and Genetics, Shantou University Medical College, Shantou 515041, China
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Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Cells 2020, 9(4), 1012; https://doi.org/10.3390/cells9041012
Received: 9 February 2020 / Revised: 10 April 2020 / Accepted: 13 April 2020 / Published: 18 April 2020
(This article belongs to the Special Issue Inhibitor of Apoptosis Proteins (IAPs) in Cancer Therapy)
Aiming to promote cancer cell apoptosis is a mainstream strategy of cancer therapy. The second mitochondria-derived activator of caspase (SMAC)/direct inhibitor of apoptosis protein (IAP)-binding protein with low pI (DIABLO) protein is an essential and endogenous antagonist of inhibitor of apoptosis proteins (IAPs). SMAC mimetics (SMs) are a series of synthetically chemical compounds. Via database analysis and literature searching, we summarize the potential mechanisms of endogenous SMAC inefficiency, degradation, mutation, releasing blockage, and depression. We review the development of SMs, as well as preclinical and clinical outcomes of SMs in solid tumor treatment, and we analyze their strengths, weaknesses, opportunities, and threats from our point of view. We also highlight several questions in need of further investigation. View Full-Text
Keywords: inhibitor of apoptosis protein (IAP); second mitochondria-derived activator of caspase (SMAC); direct IAP-binding protein with low pI (DIABLO); SMAC mimetics (SMs); clinical trial; therapy; solid tumor inhibitor of apoptosis protein (IAP); second mitochondria-derived activator of caspase (SMAC); direct IAP-binding protein with low pI (DIABLO); SMAC mimetics (SMs); clinical trial; therapy; solid tumor
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MDPI and ACS Style

Zhao, X.-Y.; Wang, X.-Y.; Wei, Q.-Y.; Xu, Y.-M.; Lau, A.T.Y. Potency and Selectivity of SMAC/DIABLO Mimetics in Solid Tumor Therapy. Cells 2020, 9, 1012. https://doi.org/10.3390/cells9041012

AMA Style

Zhao X-Y, Wang X-Y, Wei Q-Y, Xu Y-M, Lau ATY. Potency and Selectivity of SMAC/DIABLO Mimetics in Solid Tumor Therapy. Cells. 2020; 9(4):1012. https://doi.org/10.3390/cells9041012

Chicago/Turabian Style

Zhao, Xiao-Yun, Xiu-Yun Wang, Qi-Yao Wei, Yan-Ming Xu, and Andy T.Y. Lau. 2020. "Potency and Selectivity of SMAC/DIABLO Mimetics in Solid Tumor Therapy" Cells 9, no. 4: 1012. https://doi.org/10.3390/cells9041012

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