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Rose Bengal-Amphiphilic Peptide Conjugate for Enhanced Photodynamic Therapy of Malignant Melanoma.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-01-15 , DOI: 10.1021/acs.jmedchem.9b01802 Simanpreet Kaur Dhillon 1 , Simon L Porter 1 , Nermeen Rizk 1 , Yingjie Sheng 1 , Thomas McKaig 1 , Kathyrn Burnett 1 , Bronagh White 1 , Heather Nesbitt 1 , Rubeta N Matin 2 , Anthony P McHale 1 , Bridgeen Callan 1 , John F Callan 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-01-15 , DOI: 10.1021/acs.jmedchem.9b01802 Simanpreet Kaur Dhillon 1 , Simon L Porter 1 , Nermeen Rizk 1 , Yingjie Sheng 1 , Thomas McKaig 1 , Kathyrn Burnett 1 , Bronagh White 1 , Heather Nesbitt 1 , Rubeta N Matin 2 , Anthony P McHale 1 , Bridgeen Callan 1 , John F Callan 1
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Malignant melanoma is an aggressive skin cancer with poor survival outcomes for patients diagnosed at an advanced stage. While targeted serine/threonine-protein kinase B-Raf (BRAF) and immune checkpoint inhibitors have improved survival outcomes for a proportion of these patients, response rates remain variable. There is a need, therefore, for more effective treatments to bolster the options available for melanoma patients. In this manuscript, we covalently attached Rose Bengal (RB) to the amphipathic peptide (AMP) C(KLAKLAK)2 and determined the effectiveness of the resulting RB-C(KLAKLAK)2 conjugate as a photodynamic therapy (PDT) sensitizer. RB-C(KLAKLAK)2-mediated PDT treatment of subcutaneous B16-F10-Luc2 tumors in C57 mice resulted in lesions that were 479% smaller at the end of the study than animals treated with RB-mediated PDT. The synergistic effect between RB and C(KLAKLAK)2 has been attributed to the AMP sensitizing cells to reactive oxygen species (ROS), making them more susceptible to ROS-induced oxidative stress.
中文翻译：
玫瑰孟加拉-两亲性肽结合物可增强恶性黑色素瘤的光动力治疗。
恶性黑色素瘤是一种侵袭性皮肤癌，对于晚期诊断的患者，其生存结果较差。尽管靶向丝氨酸/苏氨酸蛋白激酶B-Raf（BRAF）和免疫检查点抑制剂可改善部分患者的生存结局，但应答率仍存在差异。因此，需要一种更有效的治疗方法来支持黑色素瘤患者的可用选择。在此手稿中，我们将玫瑰孟加拉（RB）共价连接到两亲性肽（AMP）C（KLAKLAK）2上，并确定了所得RB-C（KLAKLAK）2偶联物作为光动力疗法（PDT）敏化剂的有效性。RB-C（KLAKLAK）2介导的PDT对C57小鼠皮下B16-F10-Luc2肿瘤的治疗导致的损伤在研究结束时比RB介导的PDT治疗的动物小479％。
更新日期：2020-01-27
中文翻译：
玫瑰孟加拉-两亲性肽结合物可增强恶性黑色素瘤的光动力治疗。
恶性黑色素瘤是一种侵袭性皮肤癌，对于晚期诊断的患者，其生存结果较差。尽管靶向丝氨酸/苏氨酸蛋白激酶B-Raf（BRAF）和免疫检查点抑制剂可改善部分患者的生存结局，但应答率仍存在差异。因此，需要一种更有效的治疗方法来支持黑色素瘤患者的可用选择。在此手稿中，我们将玫瑰孟加拉（RB）共价连接到两亲性肽（AMP）C（KLAKLAK）2上，并确定了所得RB-C（KLAKLAK）2偶联物作为光动力疗法（PDT）敏化剂的有效性。RB-C（KLAKLAK）2介导的PDT对C57小鼠皮下B16-F10-Luc2肿瘤的治疗导致的损伤在研究结束时比RB介导的PDT治疗的动物小479％。
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