Aladan scanning: The structure-activity relationship of dynorphin A

Chen, HeRu; Yang, Yang; Weng, JiangDuo

doi:10.1007/s11426-008-0150-0

Cited by 4 publications

(3 citation statements)

References 16 publications

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“…Furthermore, Aladan has a reasonably large fluorescence QY (ca. 0.29, measured in a protein environment) and, hence, has been used to study various biophysical and biological questions, such as protein solvation dynamics, peptide binding to protein ,,− or membrane, − and protein–protein interactions …”

Section: Fluorescence Probesmentioning

confidence: 99%

Unnatural Amino Acids for Biological Spectroscopy and Microscopy

Feng,

Wang,

Zhang

et al. 2024

Chem. Rev.

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Due to advances in methods for site-specific incorporation of unnatural amino acids (UAAs) into proteins, a large number of UAAs with tailored chemical and/or physical properties have been developed and used in a wide array of biological applications. In particular, UAAs with specific spectroscopic characteristics can be used as external reporters to produce additional signals, hence increasing the information content obtainable in protein spectroscopic and/or imaging measurements. In this Review, we summarize the progress in the past two decades in the development of such UAAs and their applications in biological spectroscopy and microscopy, with a focus on UAAs that can be used as site-specific vibrational, fluorescence, electron paramagnetic resonance (EPR), or nuclear magnetic resonance (NMR) probes. Wherever applicable, we also discuss future directions.

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Section: Fluorescence Probesmentioning

confidence: 99%

Unnatural Amino Acids for Biological Spectroscopy and Microscopy

Feng,

Wang,

Zhang

et al. 2024

Chem. Rev.

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“…The main applications of these steels are related to their high strength and excellent toughness properties as well as their high corrosion resistance [1,2]. Similar studies of the microstructural evolution in 2205 duplex stainless steel aged at high temperatures show that σ phase, precipitates in the interface γ/δ at low aging times [4][5][6][7]. To some degree austenite ensures the toughness of the material and ferrite is responsible for the strength [3].…”

Section: Introductionmentioning

confidence: 99%

Study of Aging Effects in 2205 Duplex Stainless Steel Using Thermoelectric Power Measurement

Lara¹,

Ruíz²,

Carreόn³

et al. 2010

AIP Conference Proceedings

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Articles you may be interested in NDE evaluation of the intergranular corrosion susceptibility of a 2205 duplex stainless steel using thermoelectric power and double loop electrochemical potentiokinetic reactivation methods AIP Conf.ABSTRACT. Thermoelectric power (TEP) measurements have been used as an effective method for evaluating the metallurgical state of various alloys. In the steel industry, some fabrication processes promote phase transformation and second phase precipitations which affect the material properties. Assessment of mechanical properties is critical in order to ensure quality of components. This work was conducted in order to evaluate the influence of the aging state of 2205 duplex stainless steel on TEP values. Commercial 2205 duplex steel was isothermally aged at 650 °C 700 °C and 900 °C at different aging times. TEP measurement technique was applied as a non destructive assessment technique to characterize the aging kinetics of the aged 2205 duplex stainless steel, hardness Rockwell (RC) and Charpy impact test were preformed to observe the effect of aging time on the specimens. Metallographic analysis was used to monitor phase transformation and sigma phase precipitation caused by the spinodal decomposition process of ferrite into secondary austenite and sigma phase. Results indicate that that the TEP is sensitive to gradual microstructural changes produced by the aging treatments..

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“…This series also included analogs in which 3-aminofentanyl is linked to a dynorphin A structure. 15–17 Furthermore, the Tyr and Phe residues in positions 1 and 4 were replaced by a Dmt and Phe(4-Cl), respectively, in 21 to facilitate opioid receptor recognition and enhance metabolic stability. C-side chain modification of the Glu residue was performed using a combination of N α -Fmoc and N α -Boc strategies (Scheme 2, block D).…”

mentioning

confidence: 99%

Effect of anchoring 4-anilidopiperidines to opioid peptides

Petrov

Lee

Vardanyan

et al. 2013

Bioorganic & Medicinal Chemistry Letters

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We report here the design, synthesis, and in vitro characterization of new opioid peptides featuring a 4-anilidopiperidine moiety. Despite the fact that the chemical structures of fentanyl surrogates have been found suboptimal per se for the opioid activity, the corresponding conjugates with opioid peptides displayed potent opioid activity. These studies shed an instructive light on the strategies and potential therapeutic values of anchoring the 4-anilidopiperidine scaffold to different classes of opioid peptides. KeywordsOpioid peptide; Dynorphine analog; Bivalent ligand; Fentanyl; AnalgesicThe increasing need for effective pain management prompts the invention of new strategies and pharmacological tools. Among the three opioid receptor types (μ, δ, and κ, the μ-opioid receptor is considered to be essential for efficient pain suppression. However, μ-opioids do not provide adequate treatment of chronic pain since their long-term use results in multiple side effects (e.g., 1 ). Close examination of the opioid system conferred that a μ-δ opioid receptor heterodimer represents the fundamental signaling unit responsible for opioid tolerance and dependence. 2,3 During the last two decades, our laboratory has carried out extensive research on the synthesis of novel opioid analogs. Within the frame of our works on bivalent opioid ligands there seemed a gap between small-molecule and peptide-based opioids. We have sought to bridge this gap by incorporating the 4-ANDP 4 scaffolds into opioid peptides, and also to optimize their physicochemical properties. [5][6][7] Previously, research efforts to produce bivalent opioid peptides resulted in analogs with exceptional properties. One representative example is biphalin. 8 Despite numerous advantages such as low toxicity, high activity and specificity, opioid peptides are still not being used as painrelieving agents in general anesthetic practice because of main drawbacks such as poor bioavailability after systemic (subcutaneous or oral) administration, limited ability to cross the blood-brain barrier, and rapid degradation in vivo by peptidases. Although the fact that fentanyl 9-12 is a bioavailable drug does not directly suggest that its addition to a peptide structure will yield a bioavailable hybrid, we hypothesized that its incorporation into opioid peptides may positively impact overall bioavailability of the latter. NIH Public Access NIH-PA Author ManuscriptNIH-PA Author Manuscript NIH-PA Author ManuscriptA careful analysis of the literature revealed that in the series of fentanyl analogs there was no general consensus regarding the effect of substitution in the propionyl part of the molecule. We thus set out to prepare the desired compound by using Fmoc-and Phtprotected amino acid chlorides (Scheme 1). This allowed us to synthesize 3-aminofentanyl and analogs 1-6. The synthesis, NMR characterization and binding affinity at the μ and δ opioid receptors of compounds 7-12 have been reported previously by us, 5 but no results of GPI and MVD assays were provided...

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Aladan scanning: The structure-activity relationship of dynorphin A

Cited by 4 publications

References 16 publications

Unnatural Amino Acids for Biological Spectroscopy and Microscopy

Unnatural Amino Acids for Biological Spectroscopy and Microscopy

Study of Aging Effects in 2205 Duplex Stainless Steel Using Thermoelectric Power Measurement

Effect of anchoring 4-anilidopiperidines to opioid peptides

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