Abstract:
:Heat shock protein 90 (Hsp90) plays a vital role in the progress of malignant disease and elevated Hsp90 expression has been reported in pancreatic cancer. In this study, we radiolabeled a dimeric Sansalvamide A derivative (Di-San A1) with 64Cu, and evaluated the feasibility of using 64Cu-Di-San A1 for PET imaging of Hsp90 expression in a mouse model of pancreatic cancer. A macrocyclic chelator NOTA (1,4,7-triazacyclononane-1,4,7-trisacetic acid) was conjugated to Di-San A1. 64Cu-Di-San A1 was successfully prepared in a radiochemical yield > 97% with a radiochemical purity > 98%. 64Cu-Di-San A1 is stable in PBS and mouse serum with > 92% of parent probe intact after 4 h incubation. The cell binding and uptake revealed that 64Cu-Di-San A1 binds to Hsp90-positive PL45 pancreatic cancer cells, and the binding can be effectively blocked by an Hsp90 inhibitor (17AAG). For microPET study, 64Cu-Di-San A1 shows good in vivo performance in terms of tumor uptake in nude mice bearing PL45 tumors. The Hsp90-specific tumor activity accumulation of 64Cu-Di-San A1 was further demonstrated by significant reduction of PL45 tumor uptake with a pre-injected blocking dose of 17AAG. The ex vivo PET imaging and biodistribution results were consistent with the quantitative analysis of PET imaging, demonstrating good tumor-to-muscle ratio (5.35 ± 0.46) of 64Cu-Di-San A1 at 4 h post-injection in PL45 tumor mouse xenografts. 64Cu-Di-San A1 allows PET imaging of Hsp90 expression in PL45 tumors, which may provide a non-invasive method to quantitatively characterize Hsp90 expression in pancreatic cancer.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Wang X,Zhang J,Wu H,Li Y,Conti PS,Chen Kdoi
10.1007/s00726-018-2566-ysubject
Has Abstractpub_date
2018-07-01 00:00:00pages
897-907issue
7eissn
0939-4451issn
1438-2199pii
10.1007/s00726-018-2566-yjournal_volume
50pub_type
杂志文章相关文献
AMINO ACIDS文献大全abstract::Branched Chain Amino Acids (BCAAs) are related to different aspects of diseases like pathogenesis, diagnosis and even prognosis. While in some diseases, levels of all the BCAAs are perturbed; in some cases, perturbation occurs in one or two while the rest remain unaltered. In case of ischemic heart disease, there is a...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-015-1994-1
更新日期:2015-10-01 00:00:00
abstract::The sulfur-containing amino acid, taurine (Tau), regulates glucose and lipid homeostasis under normal, pre- and diabetic conditions. Here, we aimed to verify whether Tau supplementation exerts its beneficial effects against obesity, hyperglycemia and alterations in islet functions, in leptin-deficient obese (ob/ob), o...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2553-3
更新日期:2018-06-01 00:00:00
abstract::In this review, recent studies on the electrophysiological effects of de novo synthesized ("endogenous") kynurenic acid (KYNA) are discussed. Endogenous KYNA is normally formed as a byproduct of tryptophan metabolism. Evidence for a physiological role in neuronal excitability has not been strong, in part because brain...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s007260070060
更新日期:2000-01-01 00:00:00
abstract::Proteins with polybasic clusters bind to negatively charged phosphoinositides at the cell membrane. In this review, I have briefly discussed the types of phosphoinositides naturally found on membrane surfaces and how they recruit protein complexes for carrying out the process of signal transduction. A large number of ...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-013-1512-2
更新日期:2013-10-01 00:00:00
abstract::Glycine is a major amino acid in mammals and other animals. It is synthesized from serine, threonine, choline, and hydroxyproline via inter-organ metabolism involving primarily the liver and kidneys. Under normal feeding conditions, glycine is not adequately synthesized in birds or in other animals, particularly in a ...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-013-1493-1
更新日期:2013-09-01 00:00:00
abstract::Glutamate dehydrogenase (GDH) plays a crucial role in amino acid deamination and has been used as an inductor of nutrients metabolism. In this study, we cloned and analyzed the GDH cDNAs in diploids (red crucian carp), triploids and tetraploids and characterized their expression profiles upon dietary treatments. Resul...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-012-1313-z
更新日期:2012-12-01 00:00:00
abstract::The effect of dietary amino acid taurine on the liver function of chronic hepatitis patients was investigated. The 24 chronic hepatitis patients with 2-5 times over normal activities of alanine aminotransferase (ALT) or aspartate aminotransferase (AST) were selected and equally divided into taurine treatment and contr...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-007-0565-5
更新日期:2008-08-01 00:00:00
abstract::3-Hydroxyaspartic acid and its derivatives are found both in the free form and as peptide constituents in various microorganisms and fungi. Considering the biological importance of this amino acid and its potential utility as a multifunctional building block in organic syntheses, we have developed a short-step, asymme...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-007-0595-z
更新日期:2008-08-01 00:00:00
abstract::Germination ofBacillus subtilis spores was initiated by L-Ala and competitively inhibited by D-Ala, suggesting the presence of an alanine receptor. The spores showed alanine racemase activity in the spore coat. To investigate the role of alanine racemase (L → D) on germination, net racemase activity was determined usi...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00805804
更新日期:1993-02-01 00:00:00
abstract::The transient receptor potential channels TRPV2 and TRPV5 belong to the vanilloid TRP subfamily. TRPV2 is highly similar to TRPV1 and shares many common properties with it. TRPV5 (and also its homolog TRPV6) is a rather distinct member of the TRPV subfamily. It is distant for being strictly Ca(2+)-selective and featur...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-010-0712-2
更新日期:2011-02-01 00:00:00
abstract::Effects of taurine on the delayed rectifier K(+) channel in isolated 10-day-old embryonic chick ventricular cardiomyocytes were examined at different intracellular Ca(2+) concentrations ([Ca]i), using whole-cell voltage and current clamp techniques. Experiments were performed at room temperature (22°C). Test pulses we...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00805955
更新日期:1995-09-01 00:00:00
abstract::The cyclization of N-Boc-α-alkylserines to corresponding β-lactones under Mitsunobu reaction conditions and the ring opening with heterocyclic amines (pyrrolidine, piperidine, morpholine and thiomorpholine) produced N-Boc-α-alkyl-β-(sec-amino)alanines. The removal of the Boc group gives di-hydrochlorides of non-protei...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-011-1055-3
更新日期:2012-06-01 00:00:00
abstract::Lateral diffusion of membrane-integral receptors within the plane of the membrane has been postulated to be mechanistically important for signal transduction. Direct measurement of polypeptide hormone receptor lateral mobility using fluorescence photobleaching recovery techniques indicates that tyrosine kinase recepto...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00805831
更新日期:1995-06-01 00:00:00
abstract::The putative translation factor eIF5A is essential for cell viability and is highly conserved from archaebacteria to mammals. This factor is the only cellular protein that undergoes an essential posttranslational modification dependent on the polyamine spermidine, called hypusination. This review focuses on the functi...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-007-0533-0
更新日期:2007-08-01 00:00:00
abstract::Agmatine, a metabolite generated by arginine decarboxylation, has been reported as neuromodulator and neuroactive substance. Several findings suggest that agmatine displays neuroprotective effects in several models of neurodegenerative disorders, such as Parkinson's disease (PD). It has been hypothesized that biogenic...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-019-02759-6
更新日期:2020-02-01 00:00:00
abstract::The study of nanomaterial/biomolecule interface is an important emerging field in bionanoscience, and additionally in many biological processes such as hard-tissue growth and cell-surface adhesion. To have a deeper understanding of the amino acids/gold nanoparticle assemblies, the adsorption of these amino acids on th...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-013-1642-6
更新日期:2014-04-01 00:00:00
abstract::The efficient synthesis ofδ-hydroxy-β,γ-dehydroα-amino acids (1) was achieved by the hybrid process, in which the Pd(II)-assisted rear-rangement ofβ-acetoxyallylglycine ester (6) afforded the corresponding (E)-δ-acetoxyvinylglycine derivatives (7) in a moderate yield. The chemo- and stereo-selective hydrolysis of7 was...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00807269
更新日期:1995-12-01 00:00:00
abstract::The TES ether of the C6-hydroxy derivative of naturally occurring epi-jasmonic acid (epi-JA) was designed as epimerization-free equivalent of epi-JA. The TES ether was synthesized from (1R,4S)-4-hydroxycyclopent-2-enyl acetate in 13 steps. The acid part of the ether was activated with ClCO2Bui and subjected to condens...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-011-0925-z
更新日期:2012-05-01 00:00:00
abstract::Reports on nucleobase-containing chiral peptides (both natural and artificial) and achiral pseudopeptides are reviewed. Their synthesis, structural features, DNA and RNA-binding ability, as well as some other interesting applications which make them promising diagnostic/therapeutic agents of great importance in many a...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-010-0567-6
更新日期:2010-06-01 00:00:00
abstract::Depending on the amount of alimentary proteins, between 6 and 18 g nitrogenous material per day enter the large intestine lumen through the ileocaecal junction. This material is used as substrates by the flora resulting eventually in the presence of a complex mixture of metabolites including ammonia, hydrogen sulfide,...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-006-0477-9
更新日期:2007-11-01 00:00:00
abstract::A large series of plasma albumin (ALB, g/dl) and simultaneous blood and clinical measurements were prospectively performed on 92 liver resection patients, and processed to assess the correlations between ALB, other plasma proteins, additional variables and clinical events. The measurements were performed preoperativel...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-005-0287-5
更新日期:2006-11-01 00:00:00
abstract::Based on ubiquitous presence of large ionic motifs and clusters in proteins involved in gene transcription and protein synthesis, we analyzed the distribution of ionizable sidechains in a broad selection of proteins with regulatory, metabolic, structural and adhesive functions, in agonist, antagonist, toxin and antimi...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-012-1418-4
更新日期:2012-12-01 00:00:00
abstract::Taurine can protect against cardiovascular diseases, whereas elevated levels of plasma homocysteine are associated with atherosclerotic and thromboembolic cardiovascular diseases. To illustrate the effects of taurine on hyperhomocysteinemia, we observed the myocardial mitochondria dysfunction in the rats with hyperhom...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-004-0096-2
更新日期:2004-08-01 00:00:00
abstract::Nitric oxide synthase (NOS) activities are responsible for the enzymatic conversion of L-arginine into NO and L-citrulline. Relatively low amounts of NO are produced in intestinal epithelial cells or are released from nerve endings. The effects of NO production are related to the maintenance of epithelial integrity an...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s007260050020
更新日期:2000-01-01 00:00:00
abstract::A growing body of evidence implicates endoplasmic reticulum (ER)-induced cellular dysfunction and apoptosis as important factors to a variety of diseases. In endothelial cells (ECs), the sulfur-containing amino acid homocysteine (Hcy) causes EC apoptosis and reactive oxygen species (ROS) generation through induction o...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-016-2375-0
更新日期:2017-04-01 00:00:00
abstract::Delta-amino acids are very attractive in drug discovery, especially in the peptidomimetic area, because of their capability to act as dipeptide isosteres and reverse turn mimetics. Herein we report the synthesis of a rigid delta-amino acid constrained by a 3-aza-6,8-dioxabicyclo[3.2.1]octane-based scaffold, which can ...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-007-0636-7
更新日期:2008-06-01 00:00:00
abstract::In this study, we investigated the activating role of Mcm1p at ARG1 during arginine starvation. Our results showed that two Mcm1p binding sites positively contribute to ARG1 transcription and cell growth. Especially, we provide strong evidence that the Mcm1p binding sites play a positive role in ARG1 transcription to ...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-010-0687-z
更新日期:2011-02-01 00:00:00
abstract::Green tea which is widely consumed in China, Japan and India, contains polyphenolic compounds, which account for 30% of the dry weight of the leaves. Most of the polyphenols are flavanols, of which (-)-epigallocatechin-3-gallate (EGCG) is most abundant. Epidemiological studies revealed that the incidences of stomach a...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s726-002-8197-9
更新日期:2002-01-01 00:00:00
abstract::Emerging evidence from laboratory researches has highlighted the bioactivity of food melanoidins and melanoproteins. Whilst such studies have been carried out with different in vitro systems, information about melanoidins absorption and bio-availability are scarce. However, they are generally considered as poorly abso...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-015-1951-z
更新日期:2015-06-01 00:00:00
abstract::D: -Amino acid oxidase (DAAO) in mammal kidney regulates the renal reactive oxygen species (ROS) levels directly and plays a leading role in the development of ROS-mediated renal pathologic damages based on its crucial role in the oxidative deamination of D: -amino acids and the consequent generation of H(2)O(2). Quan...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-010-0811-0
更新日期:2012-01-01 00:00:00