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Design, Synthesis, and Bioevaluation of Novel Enzyme-Triggerable Cell Penetrating Peptide-Based Dendrimers for Targeted Delivery of Camptothecin and Cancer Therapy.
Mai, Ruiyao; Deng, Bulian; Zhao, Huiting; Li, Ling; Fang, Yuyu; Li, Siming; Deng, Xin; Chen, Jianjun.
Afiliación
  • Mai R; School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, China.
  • Deng B; School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, China.
  • Zhao H; School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, China.
  • Li L; School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, China.
  • Fang Y; Department of Nephrology, First People's Hospital of Pingjiang County, Yueyang 414500, China.
  • Li S; Analytical Applications Center, Shimadzu (China) Co., Ltd. Guangzhou Branch, 230 Gaotang Road, Guangzhou 510656, China.
  • Deng X; Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target and Clinical Pharmacology, the NMPA and State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
  • Chen J; School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, China.
J Med Chem ; 65(7): 5850-5865, 2022 04 14.
Article en En | MEDLINE | ID: mdl-35380045
Novel enzyme-triggerable cell penetrating peptide (ETCPP) dendrimers with a camptothecin (CPT) warhead were designed and synthesized based on an amphiphilic penetrating peptide (FKKFFRKLL, discovered by us before). Among the newly synthesized ETCPP dendrimer conjugates, BL_Oc-SS-CPT (a high-generation dendrimer) exhibited the highest activity with IC50s in the nanomolar range (31-747 nM) against a panel of cancer cells, which is 3-10 times better than that of CPT. BL_Oc-SS-CPT remained intact during transit to target cells and in normal tissues with a plasma half-life of 4.2 h, 2.3-fold longer than that of the monomer (1.8 h). Once reaching the tumor site, BL_Oc-SS-CPT gradually released CPT in the presence of excessive matrix metalloproteinase-2/9 and GSH in cancer cells. Importantly, BL_Oc-SS-CPT exhibited excellent in vivo tumor targeting capability and antitumor efficacy with benign toxicity profiles. Thus, the novel ETCPP dendrimer-based drug delivery system (e.g., BL_Oc-SS-CPT) represents a safe and effective strategy for targeted cancer therapy.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Camptotecina / Sistemas de Liberación de Medicamentos / Dendrímeros / Péptidos de Penetración Celular / Neoplasias Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Camptotecina / Sistemas de Liberación de Medicamentos / Dendrímeros / Péptidos de Penetración Celular / Neoplasias Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos