Radionuclide–Peptide Nucleic Acid in Diagnosis and Treatment of Pancreatic Cancer

Wickstrom, Eric; Tian, Xiaofeng; Амирханов, Н. В.; Chakrabarti, Abhijit; Aruva, Mohan R.; Rao, P. S.; Qin, Wenyi; Zhu, Weizhu; Sauter, Edward R.; Thakur, Mathew L.

doi:10.1385/1-59259-854-4:135

Cited by 6 publications

(7 citation statements)

References 121 publications

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“…19,31,[40][41][42][43][44] For the purpose of this work, we decided to use a di-(2-picolyl)amide (Dpam) derivative (3, Figure 1) as a coordination entity for Re/ 99m…”

Section: Mmentioning

confidence: 99%

Towards the Preparation of Novel Re/99mTc Tricarbonyl-Containing Peptide Nucleic Acid Bioconjugates

et al. 2011

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A novel azido derivative of the di-(2-picolyl)amide (Dpam) ligand, namely 3-azido-N,N-bispyridin-2-ylmethyl-propionamide (3), was prepared from 3-bromo-N,N-bis(pyridin-2-ylmethyl)propanamide (2) with an excess of sodium azide in DMSO. 3 was then reacted, by CuI-catalyzed [3 + 2] cycloaddition (often referred to as 'Click Chemistry'), with the previously reported alkyne-containing peptide nucleic acid (PNA) monomer Fmoc-1-OtBu to give the Dpam-containing PNA monomer

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“…19,31,[40][41][42][43][44] For the purpose of this work, we decided to use a di-(2-picolyl)amide (Dpam) derivative (3, Figure 1) as a coordination entity for Re/ 99m…”

Section: Mmentioning

confidence: 99%

Towards the Preparation of Novel Re/99mTc Tricarbonyl-Containing Peptide Nucleic Acid Bioconjugates

et al. 2011

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“…Nevertheless, we among a few others, have designed, synthesized and evaluated Tc-99m and Cu-64 labeled specific probes that target specific oncogene mRNAs for SPECT or PET imaging of breast, pancreatic and colorectal cancers (34-42). Our probes consist of a short 12 mer peptide nucleic acid (PNA) to which is attached tetramer cyclic peptide (Cys-Ser-Lys-Cys-CONH2) specific for IGFR-1 receptors at one end a chelating agent such as DOTA (1,4,7,10-tetraazacyclododecane-N 1 ,-N 11 , N 111, N 1111 -tetraacetic acid) at the other, for strong chelation of a radionuclide.…”

Section: B Diagnostic Applicationsmentioning

confidence: 99%

“…It is estimated that more than 10 6 IGFR1 receptors are expressed on certain human breast cancer cells, as compared only to a few on normal cells. This provides high specificity for the probe to bind and internalize in malignant cells (34-42). Similarly, approximately 6 × 10 3 cyclinD1 mRNA copies are expressed per MCF7 human breast cancer cell that provide up to 10 12 targets per gram of a tumor.…”

Section: B Diagnostic Applicationsmentioning

confidence: 99%

Genomic Biomarkers for Molecular Imaging: Predicting the Future

Thakur

2009

Seminars in Nuclear Medicine

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Over the past few decades great strides have been made in anatomical imaging of disease that has lead to their diagnosis with minimal invasion. Despite these advances, disease like cancer continues to take one human life every minute in the USA alone. Complimentary approaches that pertain directly to the genesis of the disease might contribute to its early diagnosis and subsequent management. In cancer, an array of molecular abnormalities leading to the modulations in expression of key proteins important in the cellular signaling pathways and cell proliferation has been identified. These specific disease fingerprints, biomarkers, are over expressed on malignant cell surfaces or within the cytoplasm and provide unique targets and promise to improve cancer diagnosis and therapy.We, among others, have designed, synthesized, and evaluated some novel probes specific for those oncogenes and oncogene product biomarkers for PET and SPECT molecular imaging of certain types of cancers.This article briefly describes this approach and gives specific examples which depict the ability of molecular imaging to detect occult lesions not detectable by current scintigraphic approaches. The article also outlines a few examples predicting other possible applications of targeting such specific probes not yet utilized."Our nation always has been about the urge to dream and the will to accomplish them" N. Tyson.

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“…In a similar approach, Wickstrom and colleagues prepared novel DOTA-polydiaminopropanoate (DOTA-PDAP) dendrimers, which were conjugated to PNA-peptide chimeras designed to target the mRNA of the mutant K-ras oncogene [105]. The synthesis started with assembly of the delivery peptide on solid phase, followed by inline coupling of the PNA monomers.…”

Section: Pna-metal Complex Derivatives and Pna-minor Groove Binder Comentioning

confidence: 99%

Peptide Nucleic Acid Conjugates: Synthesis, Properties and Applications

Zhilina¹,

Ziemba²,

Ebbinghaus³

2005

CTMC

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Artificial control of gene expression has great potential in the treatment of many human diseases, and peptide nucleic acids (PNAs) offer several potential advantages for silencing gene expression in mammalian cells. The pseudopeptide backbone of the PNA makes it resistant to enzymatic degradation, and PNAs bind complementary DNA and RNA with high affinity and specificity. PNAs are potentially leading agents for antigene and antisense therapeutics, but the application of PNAs in the in vivo setting is hampered by their poor intracellular delivery. This problem has been addressed by PNA conjugation to lipophilic moieties, peptides, and cell-specific receptor ligands. The biological activity of PNAs can also benefit from conjugation to DNA interactive compounds like intercalators and alkylators. Here we review the most interesting literature concerning PNA conjugation with small molecules, emphasizing synthetic approaches, properties and applications of the PNA conjugates.

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Radionuclide–Peptide Nucleic Acid in Diagnosis and Treatment of Pancreatic Cancer

Cited by 6 publications

References 121 publications

Towards the Preparation of Novel Re/99mTc Tricarbonyl-Containing Peptide Nucleic Acid Bioconjugates

Towards the Preparation of Novel Re/99mTc Tricarbonyl-Containing Peptide Nucleic Acid Bioconjugates

Genomic Biomarkers for Molecular Imaging: Predicting the Future

Peptide Nucleic Acid Conjugates: Synthesis, Properties and Applications

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