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理性改造光脱羧酶并用于反式脂肪酸选择性脱羧反应 被引量:1
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作者 曾森海 鲍雨妍 +1 位作者 曹奡 黄小强 《大学化学》 CAS 2023年第4期243-252,共10页
立足光酶催化合成和酶的理性改造等研究前沿,设计了一例光酶催化的反式脂肪酸高选择性脱羧去除实验。具体地,本实验借助分子对接技术,理性设计脂肪酸光脱羧酶Cv FAP的突变体V453E-Cv FAP,并实验验证该突变体能够选择性地催化反油酸的脱... 立足光酶催化合成和酶的理性改造等研究前沿,设计了一例光酶催化的反式脂肪酸高选择性脱羧去除实验。具体地,本实验借助分子对接技术,理性设计脂肪酸光脱羧酶Cv FAP的突变体V453E-Cv FAP,并实验验证该突变体能够选择性地催化反油酸的脱羧反应,从而实现顺式脂肪酸的富集。实验涉及培养细胞、诱导酶表达、提取酶液、设计反应以及产物的定性、定量分析等内容,非常适合在化学生物学实验或综合化学实验课程中开设。 展开更多
关键词 酶的理性改造 脂肪酸光脱羧酶Cv FAP 反式脂肪酸 光酶催化 脱羧反应
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工作细菌——胃中的酸碱攻防战
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作者 曾森海 陈芳俊 +1 位作者 陈子涵 陈建成 《大学化学》 CAS 2021年第10期192-196,共5页
讲述了主人公小明感染幽门螺旋杆菌、检测幽门螺旋杆菌到治疗的全过程。介绍了胃壁细胞抵御胃酸伤害的方法,幽门螺旋杆菌在胃酸中的生存方式、检测手段以及治疗幽门螺旋杆菌感染的方法。
关键词 幽门螺旋杆菌 检测手段 治疗方法 化学原理
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Locally unlocks prodrugs by radiopharmaceutical in tumor for cancer therapy
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作者 Changlun Wang Mengxin Xu +6 位作者 Zihang Zhang Senhai Zeng Siyong Shen Zexuan Ding Junyi Chen Xi-Yang Cui Zhibo Liu 《Science Bulletin》 SCIE EI CAS CSCD 2024年第17期2745-2755,共11页
Chemotherapy is the first-line treatment for cancer, but its systemic toxicity can be severe. Tumorselective prodrug activation offers promising opportunities to reduce systemic toxicity. Here, we present a strategy f... Chemotherapy is the first-line treatment for cancer, but its systemic toxicity can be severe. Tumorselective prodrug activation offers promising opportunities to reduce systemic toxicity. Here, we present a strategy for activating prodrugs using radiopharmaceuticals. This strategy enables the targeted release of chemotherapeutic agents due to the high tumor-targeting capability of radiopharmaceuticals. [^(18)F]FDG(2-[^(18)F]-fluoro-2-deoxy-D-glucose), one of the most widely used radiopharmaceuticals in clinics, can trigger Pt(IV) complex for controlled release of axial ligands in tumors, it might be mediated by hydrated electrons generated by water radiolysis resulting from the decay of radionuclide18F. Its application offers the controlled release of fluorogenic probes and prodrugs in living cells and tumor-bearing mice. Of note,an OxaliPt(IV) linker is designed to construct an [^(18)F]FDG-activated antibody-drug conjugate(Pt-ADC).Sequential injection of Pt-ADC and [^(18)F]FDG efficiently releases the toxin in the tumor and remarkably suppresses the tumor growth. Radiotherapy is booming as a perturbing tool for prodrug activation,and we find that [^(18)F]FDG is capable of deprotecting various radiotherapy-removable protecting groups(RPGs). Our results suggest that tumor-selective radiopharmaceutical may function as a trigger, for developing innovative prodrug activation strategies with enhanced tumor selectivity. 展开更多
关键词 Prodrugactivation RADIOPHARMACEUTICAL RADIOCHEMISTRY [^(18)F]FDG Platinum(IV)prodrug
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