• Korean Journal of Microbiology
• /
• v.49 no.2
• /
• pp.211-214
• /
• 2013

Bisphenol A (BPA) is a highly hazardous component to human since it is regarded as one of endocrine disruptors. For the analysis and/or removal of BPA, the searching for the specific ligand with a selective affinity to target BPA is required. In order to find the peptide moiety that specifically binds to BPA, the ultrasound-assisted biopanning was carried out with a phage-displayed peptide library expressing constrained heptamer. After six rounds of positive screening against BPA particles followed by the negative screening against the surface of eppendorf tube, the peptide sequence (CysLysSerLeuGluAsnSerTyrCys) with affinity to BPA was screened based on the order of frequency from the screened phage clones. To further verify the specificity of screened peptide sequence, the cross-binding affinity of the phage peptide toward BPA analogues such as Bisphenol S (BPS) and Bisphenol F (BPF) was also assessed, where the selected phage peptide showed a higher affinity to BPA over BPS and BPF.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.290.3-291
• /
• 2003

To increase detection sensitivity for multi-DDT residues (o,p-/p,p-DDT, o,p-/p,p-DDE, o,o-/o,p-DDD) analysis, a highly selective sample clean-up method was introduced prior to GC/MS analysis using immunoaffinity column. The immunoaffinity matrix was prepared by coupling IgG fraction of DDT antiserum to cyanogens bromide activated Sepharose 4B. Three DDT antisera (DDA-1, DDHP-2, DDCP-3) were test for affinity column ligand that obtained by imunizing respective DDT immunogen to rabbits, and IgG was purified using protein A affinity purification. (omitted)

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.364.1-364.1
• /
• 2002

2-Chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been recognized to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'- and/or 3'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affinity to the receptor. (omitted)

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.365.1-365.1
• /
• 2002

Since adenosine A3 receptor has been cloned from rat brain. a number of compounds have been synthesized and evaluated for the binding affinity to this receptor. Among these. 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been found to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affnity to the receptor. (omitted)

• Journal of the Korean Magnetic Resonance Society
• /
• v.26 no.4
• /
• pp.40-45
• /
• 2022

A small cage-like molecule (2) composed of three aminomethyl pyrroles and two hexa-substituted benzenes has been prepared by reduction of its iminopyrrole analogue (1) using NaBH₄. It was revealed by ¹H NMR spectroscopic analyses that cage molecule 2 strongly binds the fluoride anion in polar DMSO-d₆ relative to CDCl₃. Compared to that of compound 1, the lowered affinity of 2 for the fluoride anion is attributable to its increased electron density resulting from the production of thesecondary amine groups.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1999.04a
• /
• pp.1-4
• /
• 1999

The potential therapeutic benefit of nicotinic ligands in a variety of neurodegenerative pathologies involving the CNS has energized research efforts to develop nicotinic acetylcholine receptor (nAChR) subtype-selective ligands. In particular, there has been a concerted effort to develop nicotinic compounds with selectivity for CNS nAChRs as potential pharmacological tools in the management of these disorders. The characterization of other novel nicotinic ligands such as epibatidine. showing a marked increase in potency at nAChRs, has provided additional support for the development of potent, selective ligands at individual nAChR subtypes. We have developed and studied a number of nicotinic compounds to identify potential candidates exhibiting such selectivity. In the present study, we report the synthesis and biological evaluations of some azabicyclic and azatricyclic nicotine analogs to decipher the relationship among steric requirements of the nicotine's pyrrolidine ring system, binding affinity and subtype-selectivity.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.189.1-189.1
• /
• 2003

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A$_3$ receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A$_3$ receptors. The most potent A$_3$ antagonist of the present series, N-［3-(4-methoxy-phenyl)-［1,2,4］thiadiazol-5-yl］-acetamide exhibiting a K$\_$i/ value of 0.79 nM at human adenosine A$_3$ receptors, showed antagonistic property in functional assay of cAMP biosynthesis involved in one of the signal transduction pathways of adenosine A$_3$ receptors. (omitted)

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.183-185
• /
• 2002

The discovery of new ligands with affinity and selectivity for the dopamine $D_2$ receptor subtypes is an important area in medicinal chemistry. The distribution of the $D_2$ receptors in the limbic areas of brain suggests that these receptors may be particularly an attractive target for the design of potential selective antipsychotic drugs without causing extrapyramidal side effects. (omitted)

• Bulletin of the Korean Chemical Society
• /
• v.23 no.10
• /
• pp.1439-1444
• /
• 2002

6-Nitroquipazine has higher binding affinity for SERT than other selective serotonin reuptake inhibitors. We have prepared 6-nitroquipazine based rhenium complexes which would lead to the development of potential SPECT imaging agents with $^{99m}Tc$ for 5-HT transporter.

• The Korean Journal of Physiology and Pharmacology
• /
• v.7 no.3
• /
• pp.131-142
• /
• 2003

We have studied mutant forms of Kir2.1 in which an aspartate residue (D172), important for gating by intracellular polyamines, is replaced by one of three basic residues (Arg, Lys or His). Such channels are highly selective for $K^+$, but show inward rectification that is a shallow function of voltage compared with that found in wild type. This inward rectification occurs with a reduced affinity for spermine and persists in the absence of polyamines. Though the unitary current-voltage relation shows some inward rectification, it is insufficient to account for that seen under whole cell recording. Channels open and shut under single channel recording, and changes of $P_{open}$ appear to generate inward rectification. In D172H, the reduction in affinity for spermine is greater when His is protonated at low $pH_i$. The effective valency for spermine is reduced from $3.09{\pm}0.07$ in wild type to $1.95{\pm}0.09$ in D172H at $pH_i$ 6.3. In the presence of dual mutants of Kir2.1, where E224 is also replaced, spermine affinity becomes undetectable. However, channels still show inward rectification and open and shut under hyper- and depolarisation, respectively. We suggest that Kir2.1 channel are able to undergo conformation changes; these changes may be important physiologically in generating inward rectification, the normal parameters of which are set by the binding of polyamines such as spermine.