Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment

Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment

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Tumor-homing peptides with tissue-penetrating properties increase the efficacy of targeted cancer therapy by delivering an anticancer agent to the tumor interior. LyP-1 (CGNKRTRGC) and iRGD (CRGDKGPDC) are founding members of this class of peptides. The presence of the cysteines forming the cyclizin...

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Main Authors: Venkata Ramana Kotamraju, Shweta Sharma, Poornima Kolhar, Lilach Agemy, James Pavlovich, Erkki Ruoslahti
Format: Article
Language:English
Published: SAGE Publishing 2015-01-01
Series:Breast Cancer: Basic and Clinical Research
Online Access:https://doi.org/10.4137/BCBCR.S29426
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spelling doaj-7d54d071be0143e8b75bd21e818a5c972020-11-25T02:59:01ZengSAGE PublishingBreast Cancer: Basic and Clinical Research1178-22342015-01-019s210.4137/BCBCR.S29426Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and TreatmentVenkata Ramana Kotamraju0Shweta Sharma1Poornima Kolhar2Lilach Agemy3James Pavlovich4Erkki Ruoslahti5Department of Molecular, Cellular, and Developmental Biology, Center for Nanomedicine, University of California, Santa Barbara, Santa Barbara, CA, USA.Cancer Research Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA.Department of Biomolecular Science and Engineering, University of California, Santa Barbara, Santa Barbara, CA, USA.Department of Plant Sciences, Weizmann Institute of Science, Rehovot, Israel.Department of Chemistry and Biochemistry, University of California, Santa Barbara, Santa Barbara, CA, USA.Department of Molecular, Cellular, and Developmental Biology, Center for Nanomedicine, University of California, Santa Barbara, Santa Barbara, CA, USA.Tumor-homing peptides with tissue-penetrating properties increase the efficacy of targeted cancer therapy by delivering an anticancer agent to the tumor interior. LyP-1 (CGNKRTRGC) and iRGD (CRGDKGPDC) are founding members of this class of peptides. The presence of the cysteines forming the cyclizing disulfide bond complicates conjugation of these peptides with other molecules, such as drugs. Here, we report the synthesis of conjugatable disulfide-bridged peptides and their conjugation to biologically important molecules. We have synthesized the LyP-1, iRGD, and CRGDC (GACRGDCLGA) peptides with a cysteine or maleimidohexanoic acid added externally at N-terminus of the sequences. Subsequent conjugation to payloads yielded stable compounds in which the tumor-homing properties of the peptide and the biological activity of the payload were retained.https://doi.org/10.4137/BCBCR.S29426
collection DOAJ
language English
format Article
sources DOAJ
author Venkata Ramana Kotamraju
Shweta Sharma
Poornima Kolhar
Lilach Agemy
James Pavlovich
Erkki Ruoslahti
spellingShingle Venkata Ramana Kotamraju
Shweta Sharma
Poornima Kolhar
Lilach Agemy
James Pavlovich
Erkki Ruoslahti
Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
Breast Cancer: Basic and Clinical Research
author_facet Venkata Ramana Kotamraju
Shweta Sharma
Poornima Kolhar
Lilach Agemy
James Pavlovich
Erkki Ruoslahti
author_sort Venkata Ramana Kotamraju
title Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
title_short Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
title_full Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
title_fullStr Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
title_full_unstemmed Increasing Tumor Accessibility with Conjugatable Disulfide-Bridged Tumor-Penetrating Peptides for Cancer Diagnosis and Treatment
title_sort increasing tumor accessibility with conjugatable disulfide-bridged tumor-penetrating peptides for cancer diagnosis and treatment
publisher SAGE Publishing
series Breast Cancer: Basic and Clinical Research
issn 1178-2234
publishDate 2015-01-01
description Tumor-homing peptides with tissue-penetrating properties increase the efficacy of targeted cancer therapy by delivering an anticancer agent to the tumor interior. LyP-1 (CGNKRTRGC) and iRGD (CRGDKGPDC) are founding members of this class of peptides. The presence of the cysteines forming the cyclizing disulfide bond complicates conjugation of these peptides with other molecules, such as drugs. Here, we report the synthesis of conjugatable disulfide-bridged peptides and their conjugation to biologically important molecules. We have synthesized the LyP-1, iRGD, and CRGDC (GACRGDCLGA) peptides with a cysteine or maleimidohexanoic acid added externally at N-terminus of the sequences. Subsequent conjugation to payloads yielded stable compounds in which the tumor-homing properties of the peptide and the biological activity of the payload were retained.
url https://doi.org/10.4137/BCBCR.S29426
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