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Armin Arabanian Mahdieh Mohammadnejad Saeed Balalaie Jürgen H. Gross 《Bioorganic & medicinal chemistry letters》2009,19(3):887-890
An efficient method for the synthesis of some Gn-RH analogues based on Ugi reaction has been developed. Four-component reaction of N- and C-terminus peptides, aromatic aldehydes and isocyanides affords novel Gn-RH analogues derived from triptorelin and gonadorelin. All of the products were purified using preparative HPLC and the structures were assigned according to MALDI-mass spectrometry data. 相似文献
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Ghodrati Atefe Firoozpour Loghman Balalaie Saeed Hosseini Faezeh Sadat Ramezanpour Sorour Edraki Najme Mohtavinejad Naser Amanlou Massoud 《International journal of peptide research and therapeutics》2020,26(4):2169-2177
International Journal of Peptide Research and Therapeutics - β-secretase 1 (BACE1) plays a pivotal role in the pathology of Alzheimer?s disease via accumulation beta amyloid in the... 相似文献
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Razieh Salehi Ashani Homa Azizian Nahid Sadeghi Alavijeh Vaezeh Fathi Vavsari Shabnam Mahernia Niloofar Sheysi Mahmood Biglar Massoud Amanlou Saeed Balalaie 《化学与生物多样性》2020,17(5)
A series of new deferasirox derivatives were synthesized through the reaction of monosubstituted hydrazides with 2‐(2‐hydroxyphenyl)‐4H‐benzo[e][1,3]oxazin‐4‐one. For the first time, deferasirox and some of its derivatives were evaluated for their in vitro inhibitory activity against Jack bean urease. The potencies of the members of this class of compounds are higher than that of acetohydroxamic acid. Two compounds, bearing tetrazole and hydrazine derivatives (bioisoester of carboxylate group), represented the most potent urease inhibitory activity with IC50 values of 1.268 and 3.254 μm , respectively. In silico docking studies were performed to delineate possible binding modes of the compounds with the enzyme, urease. Docking analysis suggests that the synthesized compounds were anchored well in the catalytic site and extending to the entrance of binding pocket and thus restrict the mobility of the flap by interacting with its crucial amino acid residues, CME592 and His593. The overall results of urease inhibition have shown that these target compounds can be further optimized and developed as a lead skeleton for the discovery of novel urease inhibitors 相似文献
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Zahra Rezaee Seyed Abbas Arabanian Saeed Balalaie Abolhassan Ahmadiani Leila Khalaj Sanaz Nasoohi 《Journal of peptide science》2012,18(2):92-96
Dipeptidyl carboxypeptidase‐I is an enzyme involved in the biological degradation of enkephalins. It has been suggested that C‐terminal amidation of enkephalins enhances their resistance to dipeptidyl carboxypeptidase‐I‐mediated biodegradation. In this study, a novel [Met5]enkephalin amide (MEA) analogue [Met5]enkephalin (ME)‐semicarbazide synthesized by another laboratory in our group was assessed for its antinociceptive effects compared with ME‐ethylamide, MEA and ME, using tail flick test. To protect the administered drugs from biodegradation, rats were pretreated with peptidase inhibitors including amastatin, phosphoramidon and captopril. Then captopril (dipeptidyl carboxypeptidase‐I inhibitor) was deleted from the peptidase inhibitors' combination for evaluating in vivo resistance of the synthetic drugs to dipeptidyl carboxypeptidase‐I. According to the results, ME‐semicarbazide and MEA were resistant enough to dipeptidyl carboxypeptidase‐I to exert their strong antinociception following intrathecal administration even in the absence of captopril, whereas the antinociceptive effects produced by ME‐ethylamide (10 nmol) were abolished in rats not pretreated with captopril, indicating that significant amounts of the ME‐ethylamide were degraded by dipeptidyl carboxypeptidase‐I. Replacement of the amide moiety of MEA with semicarbazide provides a new ME derivative, with high analgesic effects as well as more resistance to dipeptidyl carboxypeptidase‐I‐mediated biodegradation. Copyright © 2011 European Peptide Society and John Wiley & Sons, Ltd. 相似文献
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Zahra Rezaee Armin Arabanian Saeed Balalaie Abolhassan Ahmadiani Sanaz Nasoohi 《International journal of peptide research and therapeutics》2012,18(4):305-309
In our previous study on [Met5]-enkephalin analogues, [Met5]-enkephalin semicarbazide was found as a new enkephalin amide that produces antinociception even in ACE (Angiotensin Converting Enzyme) exposure in vivo. In the present work we examined the corresponding [Leu5]-enkephalin derivatives to confirm the influence of semicarbazide substitution. To prevent the enkephalins biodegradation animals were pretreated with a mixture of peptidase inhibitors. As assessed by tail-flick test no significant difference was detected between the produced antinociception by the [Leu5]-enkephalin derivatives. Based on our results both semicarbazide and ethylamide groups could preserve the provided analgesia after captopril (ACE inhibitor) omission from the peptidase inhibitors mixture. This work confirms that semicarbazide substitution on enkephalins yields ACE resistance antinociceptive peptides, nevertheless it may necessarily not enhance the peptides analgesic potencies. 相似文献
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Fereshteh Shamsipour Saeeideh Hosseinzadeh Seyed Shahriar Arab Sedigheh Vafaei Samira Farid Mahmood Jeddi-Tehrani Saeed Balalaie 《Journal of chemical biology》2014,7(3):85-91
Hesperadin is one of the indolinones that was designed against the ATP-binding site of Aurora kinase. This molecule inhibits Aurora B kinase by phosphorylation of histone H3. In this study, new derivatives of Hesperadin containing an amide group in their structures were synthesized through sequential Ugi/palladium-catalyzed approach and in vitro antitumor activity of new compounds were evaluated by cell proliferation assay. The results show that compounds 6f, 6i, 6l, and 6o were dose-dependently inhibited in different concentrations, and IC50 values were between 35 and 43 nM. It seems that lipophilic substitution on the indolinone core with the ability to form additional hydrogen bond might lead to increased stability of structure and activity of new Hesperadin analogues. 相似文献
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Meghdad Abdollahpour-Alitappeh Majid Lotfinia Nader Bagheri Koushan Sineh Sepehr Mahdi Habibi-Anbouhi Farzad Kobarfard Saeed Balalaie Alireza Foroumadi Ghasem Abbaszadeh-Goudarzi Kazem Abbaszadeh-Goudarzi Mohsen Abolhassani 《Journal of cellular physiology》2019,234(3):2693-2704
Targeted therapy using specific monoclonal antibodies (mAbs) conjugated to chemotherapeutic agents or toxins has become one of the top priorities in cancer therapy. Antibody–drug conjugates (ADCs) are emerging as a promising strategy for cancer-targeted therapy. In this study, trastuzumab, a humanized monoclonal anti-HER2 antibody, was reduced by dithiothreitol and conjugated to the microtubule-disrupting agent monomethyl auristatin E (MMAE) through a valine-citrulline peptide linker (trastuzumab-MC-Val-Cit-PABC-MMAE [trastuzumab-vcMMAE]). After conjugation, ADCs were characterized by using UV–vis, sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE), and flow cytometry. The antitumor activity of the ADC was evaluated in breast cancer cells in vitro. In addition, ADCs were further characterized using purification by the protein A chromatography, followed by assessment using apoptosis and MTT (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assays. Hydrophobic interaction chromatography was used to determine drug-to-antibody ratio species of ADCs produced. Our finding showed that approximately 5.12 drug molecules were conjugated to each mAb. H2L2, H2L, HL, H2, H, and L forms of ADCs were detected in nonreducing SDS-PAGE. The binding of trastuzumab-vcMMAE to HER2-positive cells was comparable with that of the parental mAb. The MTT assay showed that our ADCs induced significant cell death in HER2-positive cells, but not in HER2-negative cells. The ADCs produced was a mixture of species, unconjugated trastuzumab (14.147%), as well as trastuzumab conjugated with two (44.868%), four (16.886%), six (13.238%), and eight (10.861%) molecules of MMAE. These results indicated that MMAE-conjugated trastuzumab significantly increases the cytotoxic activity of trastuzumab, demonstrating high affinity, specificity, and antitumor activity in vitro. Trastuzumab-vcMMAE is an effective and selective agent for the treatment of HER2-positive breast tumors. 相似文献
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AbdolMajid Valipour Behrooz Heidari S. Mohsen Asghari Saeed Balalaie Hanieh Rabouti Navid Omidian 《Journal of fish biology》2021,98(4):1137-1143
Despite several studies on fish hormone therapy, finding new candidates may provide more reproductive efficiency in artificial propagation. Kisspeptins, being upstream of the hypothalamic–pituitary-gonadal axis, appear to play a key role in the reproduction process. In the present study, the effect of different variants of kisspeptide, including goldfish (Carassius auratus) kiss1 kisspeptin (Kiss1), human kisspeptin (Hkiss), and their combination (Kiss1 + H), on the reproductive indices of goldfish broodstock in comparison to Ovaprim (a typical synthetic Gnrh hormone) was investigated. Peptides (Kiss1 and Hkiss) were synthesized using a solid-phase synthesis approach. Kiss1 and Hkiss were injected at a dose of 100 μg kg−1 body weight, blood samples were taken 6 h after injection and sex hormones (E2, Dhp, and 11-Kt), gonadotropins (Lh and Fsh), cortisol and reproductive indices (fecundity, fertilization and hatching percentage) were measured. The results showed a significant increase of plasma sex hormones and gonadotropins in fish treated with kisspeptins. In addition, the cortisol and lipoprotein lipase in Kiss1, Hkiss and Kiss1 + H were remarkably increased compared to Ovaprim. In conclusion, kisspeptins could be a more suitable candidate than Ovaprim for accelerating and synchronizing oocyte maturation in the fisheries industry. 相似文献
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