139338-72-0Relevant articles and documents
Synthesis and evaluation of diastereoisomers of 1,4,7-triazacyclononane-1, 4,7-tris-(glutaric acid) (NOTGA) for multimeric radiopharmaceuticals of gallium
Gomez, Francisco L. Guerra,Uehara, Tomoya,Rokugawa, Takemi,Higaki, Yusuke,Suzuki, Hiroyuki,Hanaoka, Hirofumi,Akizawa, Hiromichi,Arano, Yasushi
, p. 2229 - 2238 (2012)
In the conventional synthesis of 1,4,7-tris-(glutaric acid)-1,4,7- triazacyclononane (NOTGA), four isomeric species are usually generated by the alkylation of 1,4,7-triazacyclononane with α-bromoglutaric acid diester. To estimate their biological efficaci
Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming
Sheng, Yuwen,Chen, Yuwen,Zeng, Zhongqiu,Wu, Wenbi,Wang, Jing,Ma, Yuling,Lin, Yuan,Zhang, Jichao,Huang, Yulan,Li, Wenhua,Zhu, Qiyu,Wei, Xiao,Li, Suiyan,Wisanwattana, Wisanee,Li, Fu,Liu, Wanli,Suksamrarn, Apichart,Zhang, Guolin,Jiao, Wei,Wang, Fei
, p. 460 - 484 (2022/01/03)
Cancer cell proliferation in some organs often depends on conversion of pyruvate to oxaloacetate via pyruvate carboxylase (PC) for replenishing the tricarboxylic acid cycle to support biomass production. In this study, PC was identified as the cellular target of erianin using the photoaffinity labeling-click chemistry-based probe strategy. Erianin potently inhibited the enzymatic activity of PC, which mediated the anticancer effect of erianin in human hepatocellular carcinoma (HCC). Erianin modulated cancer-related gene expression and induced changes in metabolic intermediates. Moreover, erianin promotes mitochondrial oxidative stress and inhibits glycolysis, leading to insufficient energy required for cell proliferation. Analysis of 14 natural analogs of erianin showed that some compounds exhibited potent inhibitory effects on PC. These results suggest that PC is a cellular target of erianin and reveal the unrecognized function of PC in HCC tumorigenesis; erianin along with its analogs warrants further development as a novel therapeutic strategy for the treatment of HCC.
EXENATIDE MODIFIER AND USE THEREOF
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Paragraph 0083, (2018/05/24)
Disclosed are an exenatide modifier for connecting the exenatide to a fatty chain with a carboxy in the terminus thereof by means of a hydrophilic connecting arm, and a use thereof in preparing drugs serving as a GLP-1 receptor agonist; a use in preparing drugs for preventing and/or treating diseases and/or symptoms associated with a low GLP-1 receptor activity; a use in preparing drugs for diseases and/or symptoms associated with glycometabolism; a use in preparing drugs for diabetes; a use in preparing drugs for fatty liver disease, and a use in preparing drugs for losing weight.
Zinc(II)cyclen-peptide conjugates interacting with the weak effector binding state of Ras
Schmidt, Florian,Rosnizeck, Ina C.,Spoerner, Michael,Kalbitzer, Hans Robert,K?nig, Burkhard
, p. 38 - 48 (2011/03/22)
Zinc(II)cyclen-peptide hybrid compounds and bis-zinc(II)cyclen complexes are prepared as potential binders of the guanine nucleotide binding protein Ras, an important molecular switch in cellular signal transduction. The design of the compounds is based on the previous observation that zinc(II)cyclen complexes could serve as lead compounds for inhibitors of Ras-effector interaction and thus be able to interrupt Ras induced signal transduction. Zinc(II)cyclen selectively stabilizes conformational state 1 of active Ras, a conformational state with drastically decreased affinity to effector proteins like Raf-kinase. To achieve higher binding affinities of such Ras-Raf interaction inhibitors, zinc(II)cyclen conjugates with short peptides, derived from the sequence of the Ras-activator SOS, were prepared by solid phase synthesis protocols. Dinuclear bis-zinc(II)cyclen complexes were obtained from alkyne-azide cycloaddition reactions. NMR investigations of the prepared compounds revealed that the peptide conjugates do not lead to an increase in Ras binding affinity of the metal complex-peptide conjugates. The dinuclear zinc complexes lead to an immediate precipitation of the protein prohibiting spectroscopic investigations of their binding.
Synthesis of bifunctional integrin-binding peptides containing PEG spacers of defined length for non-viral gene delivery
Pilkington-Miksa, Michael A.,Sarkar, Supti,Writer, Michele J.,Barker, Susie E.,Shamlou, Parviz Ayazi,Hart, Stephen L.,Hailes, Helen C.,Tabor, Alethea B.
experimental part, p. 2900 - 2914 (2009/04/11)
Improving the buffer and serum stability of non-viral gene delivery vectors, and increasing their circulation time in vivo, is an important focus of current research in gene therapy. The most successful strategies to date have involved shielding the complexes with large polydisperse PEG adducts. However, this approach is accompanied by a fall in transfection efficiency. In this paper we describe the solid-phase synthesis of a series of bifunctional peptides bearing short PEG spacers of defined structure as components of lipopolyplex gene delivery vectors. Short, high-yielding routes to a series of PEG-amino acids are described: these PEG-amino acids can be used in varying combinations to afford bifunctional peptides with varying lengths of PEG spacers by using standard solid-phase synthesis techniques. A series of lipopolyplexes were formulated using these bifunctional peptides, and their transfection properties assessed. Dynamic light scattering measurements on the complex with the best transfection properties showed that in phosphate-buffered saline this complex was considerably more stable, and aggregated more slowly, than a complex formulated using a similar peptide lacking the short PEG spacer. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Spacer molecules in peptide sequences: Incorporation into analogues of atrial natriuretic factor
Boumrah, Derradji,Campbell, Malcolm M.,Fenner, Simon,Kinsman, Richard G.
, p. 6977 - 6992 (2007/10/03)
In the present study, 10 modified human atrial natriuretic factor (hANF) analogues were designed using solid phase synthesis. This was carried out by replacing 'alkyl or glycol' spacer with octapeptide sequence within die cyclic portion of hANF in each annlogue synthesised. The unnatural amino acid spacers (1b) and (2d) have been synthesised using solution chemistry. The latter spacers were successfully incorporated into the peptide structure, using solid phase synthesis assembly. Amongst the ten analogues, thus prepared, two in which the alkyl spacer was used to substitute amino acid residues Gly15 to Gly21 and Arg14 to Leu21 to give 4a and 4b, successively. In the purification process of the latter analogues (4a, 4b), problems of their severe solubility were encountered. The eight glycol-spaced analogues (5a-5h) were successfully synthesised and purified using HPLC. The structure of (5a-5h) was confirmed by the presence of mass ion peaks in the atom bombardment mass spectroscopy (FAB MS) and by NMR. The latter analogues were tested, in vivo, for their ability to bind to specific hANF receptors, as agonists or antagonists. The biological results have showed that none of these analogues (5a-5h) were active.
