title: Gold nanoparticles functionalized with therapeutic and targeted peptides for cancer treatment.
abstract: Functionalization of nanostructures such as gold nanoparticles (AuNPs) with different biological molecules has many applications in biomedical imaging, clinical diagnosis and therapy. Researchers mostly employed AuNPs larger than 10 nm for different biological and medicinal applications in previous studies. Herein, we synthesized a novel small (2 nm) AuNPs, which were functionalized with the therapeutic peptide, PMI (p12), and a targeted peptide, CRGDK for selective binding to neuropilin-1(Nrp-1) receptors which overexpressed on the cancer cells and regulated the process of membrane receptor-mediated internalization. It was found that CRGDK peptides increased intracellular uptake of AuNPs compared to other surface conjugations quantified by ICP-MS. Interestingly, CRGDK functionalized AuNPs resulted in maximal binding interaction between the CRGDK peptide and targeted Nrp-1 receptor overexpressed on MDA-MB-321 cell surface, which improved the delivery of therapeutic P12 peptide inside targeted cells. Au@p12 + CRGDK nanoparticles indicated with highly effective cancer treatment by increasing p53 expression upregulated with intracellular enhanced p12 therapeutic peptide. These results have implications to design and functionalize different molecules onto AuNPs surfaces to make hybrid model system for selective target binding as well as therapeutic effects for cancer treatment.
authors: CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Chinese Academy of Sciences, Beijing 100190, PR China.
authors: Anil
authors: A
authors: Kumar
authors: Huili
authors: H
authors: Ma
authors: Xu
authors: X
authors: Zhang
authors: Keyang
authors: K
authors: Huang
authors: Shubin
authors: S
authors: Jin
authors: Juan
authors: J
authors: Liu
authors: Tuo
authors: T
authors: Wei
authors: Weipeng
authors: W
authors: Cao
authors: Guozhang
authors: G
authors: Zou
authors: Xing-Jie
authors: XJ
authors: Liang
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000378:metabolism; D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D005260:Female; D006046:Gold / Q000737:chemistry; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D039942:Neuropilin-1 / Q000378:metabolism; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides; D010455:Peptides; D016159:Tumor Suppressor Protein p53; C549069:threonyl-seryl-phenylalanyl-alanyl-glutamyl-tyrosyl-tryptophyl-asparagyl-leucyl-leucyl-seryl-proline; D039942:Neuropilin-1; D006046:Gold