| Design of Acid-activated Cell Penetrating Peptide for Delivery of Active Molecules into Cancer Cells. | |
| | |
MedLine Citation:
|
PMID: 21663318 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
TP10-5 (TK) was screened as the most promising candidate among the designed analogs of transportan 10 (TP10), a cell penetrating peptide (CPP) with remarkable capacity for membrane translocation. However, low levels of specificity and high toxicity limit its successful use for drug delivery applications. Here, we developed a new type of acid-activated CPP (TH) by replacement of all lysines of TK with histidines. As expected, histidine-containing TH can be activated and subsequently enter cells at pH 6.0, whereas it is less active at pH 7.4. In contrast, the uptake of TK has no significant difference for both pH values. Importantly, the toxicity of TH was significantly lower than that of TK under physiological conditions. After attachment of camptothecin (CPT) to TH, this conjugate inhibited the proliferation of cancer cells in a pH-dependent manner compared with free CPT and TK-CPT. This study opens a new avenue to design CPPs that preferentially enter cells in acidic solid tumors, with minimal cellular uptake in normal tissues. |
| | |
Authors:
|
Rui Wang; Wei Zhang; Jingjing Song; Bangzhi Zhang; Liwei Liu; Kairong Wang |
Related Documents
:
|
21795398 - Caldesmon regulates actin dynamics to influence cranial neural crest migration in xenopus. 21601508 - Contact lens wear and the goblet cells of the human conjunctiva-a review. 22042758 - Effect of 25-hydroxyvitamin d(3) and 1 α,25 dihydroxyvitamin d(3) on differentiation... 21831548 - Diamond cell fourier transform infrared spectroscopy transmittance analysis of black to... 19050678 - Chimeric molecules facilitate the degradation of androgen receptors and repress the gro... 7588398 - Adrenal-specific transgene expression and derivation of conditionally immortal rat adre... |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2011-6-13 |
Journal Detail:
|
Title: Bioconjugate chemistry Volume: - ISSN: 1520-4812 ISO Abbreviation: - Publication Date: 2011 Jun |
Date Detail:
|
Created Date: 2011-6-13 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Pd-Catalyzed Asymmetric Allylic Etherizations with Oximes by Chiral Alkene-Phosphine Ligands.
Next Document: Convergent Synthesis and Biological Evaluation of 2-Amino-4-(3',4',5'-trimethoxyphenyl)-5-Aryl Thiaz...