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Synthesis and in vitro anti-cancer evaluation of luteinizing hormone-releasing hormone-conjugated peptide

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Abstract

Luteinizing hormone-releasing hormone (LHRH) is a decapeptide hormone released from the hypothalamus and shows high affinity binding to the LHRH receptors. It is reported that several cancer cells also express LHRH receptors such as breast, ovarian, prostatic, bladder and others. In this study, we linked B1, an anti-cancer peptide, to LHRH and its analogs to improve the activity against cancer cells with LHRH receptor. Biological evaluation revealed that TB1, the peptide contains triptorelin sequence, present favorable anti-cancer activity as well as plasma stability. Further investigations disclosed that TB1 trigger apoptosis by activating the mitochondria–cytochrome c–caspase apoptotic pathway, it also exhibited the anti-migratory effect on cancer cells.

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Acknowledgments

The work was supported by the National Natural Science Foundation of China (No. 81172932 and 81273376), the Natural Science Foundation of Jiangsu Province (No. BK2012356).

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The authors have no conflicts of interest to declare.

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    Authors and Affiliations

    1. State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, Jiangsu, China

      Xin Deng, Qianqian Qiu, Wenlong Huang & Hai Qian

    2. Key Laboratory of Cardiovascular Disease and Molecular Intervention, Atherosclerosis Research Center, Nanjing Medical University, Nanjing, 210029, Jiangsu, China

      Ke Ma

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    1. Xin Deng
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    2. Qianqian Qiu
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    3. Ke Ma
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    4. Wenlong Huang
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    Correspondence to Wenlong Huang or Hai Qian.

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    Handling Editor: G. J. Peters.

    X. Deng and Q. Qiu contributed equally to this work.

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    Deng, X., Qiu, Q., Ma, K. et al. Synthesis and in vitro anti-cancer evaluation of luteinizing hormone-releasing hormone-conjugated peptide. Amino Acids 47, 2359–2366 (2015). https://doi.org/10.1007/s00726-015-2021-2

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    • DOI: https://doi.org/10.1007/s00726-015-2021-2

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