Development of a solid-phase binding assay and identification of nonpeptide ligands for the FynB Src homology 2 domain.

Abstract:

:The nonreceptor tyrosine kinase FynB is known to be required in the induction of long-term potentiation (LTP), a cellular mechanism for learning and memory. Ligands of the FynB SH2 domain as a possible FynB activator are, thus, of great interest. In this study, a solid-phase ligand binding assay was established to meet the screening requirement of high-throughput and ease of use, and in an attempt to find the specific ligands for the FynB SH2 domain. This assay measures the competitive inhibition of the binding of the biotinylated phosphopeptide (GGSETDDY*AEIID), derived from a binding sequence in human focal adhesion kinase, to the SH2 domain of FynB precoated as a glutathione S-transferase fusion protein on a solid-phase. Using this high-throughput screening method for SH2 ligands, a modest size of chemical library was screened, and two non-peptide compounds, 4-acetamidobenzene sulfinic acid and 1-allylpyridinium 3-sulfonate, were identified by their strong binding affinity to the FynB SH2 domain. This result demonstrates the feasibility of the developed assay in high-throughput screening. Further studies on the molecular structures of the identified SH2-binding ligands will allow presentation of specific models for ligand-domain complexes for improving the ligands and will help to develop a potential lead compound for improving LTP.

journal_name

J Pharm Biomed Anal

authors

Kim HJ,Lee HH,Yoo HD,Hwa Lee J,Hong ST

doi

10.1016/s0731-7085(01)00507-6

subject

Has Abstract

pub_date

2002-01-01 00:00:00

pages

51-6

issue

1-2

eissn

0731-7085

issn

1873-264X

pii

S0731708501005076

journal_volume

27

pub_type

杂志文章
  • Preparative isolation and structural elucidation of impurities in fluconazole by LC/MS/MS.

    abstract::Three impurities were detected in the LC/MS analysis of fluconazole bulk drug substance. Two of the impurities were unknowns having not been reported previously. Structural assignment of these impurities was carried out by LC/MS/MS using electrospray ionization source and an ion trap mass analyzer. Structural elucidat...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2006.04.012

    authors: Dongre VG,Karmuse PP,Ghugre PD,Salunke SM,Panda N,Kumar A

    更新日期:2006-09-26 00:00:00

  • Determination of vitamin B6 in pharmaceutical formulations by flow injection-solid phase spectrophotometry.

    abstract::In this work, a new solid phase spectrophotometric method in association with flow injection analysis for Vitamin B6 (pyridoxine) determination has been developed with direct measurement of light-absorption in C18 material. In the developed method, successive passage of the complex, previously formed in the flowing st...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(03)00589-2

    authors: Portela JG,Costa AC,Teixeira LS

    更新日期:2004-02-18 00:00:00

  • Simultaneous quantification and pharmacokinetic investigation of selexipag and its main metabolite ACT-333679 in rat plasma by UPLC-MS/MS method.

    abstract::In the present study, an accurate, simple and fast bioanalytical method based on ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) technique for simultaneous quantification of plasma selexipag and its main metabolite ACT-333679 concentrations in rats was optimized and established. The purpo...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2020.113496

    authors: Xie S,Shi L,Chen J,Xu RA,Ye X

    更新日期:2020-10-25 00:00:00

  • Separation of ribonucleotides, deoxynucleotides, cyclic nucleotides and deoxycyclic nucleotides by reversed-phase high-performance liquid chromatography.

    abstract::A reversed-phase gradient elution system with methanol-triethylammonium phosphate buffer (83.3 mM, pH 6.0) as eluent on C(18)-bonded silica is described for the separation of 38 ribonucleotides, deoxynucleotides, cyclic nucleotides and deoxycyclic nucleotides in less than 33 min. The retention of the nucleotides can b...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(86)80046-2

    authors: Willis CL,Lim CK,Peters TJ

    更新日期:1986-01-01 00:00:00

  • Study of the photolytic and photocatalytic transformation of amiloride in water.

    abstract::The diffusion of drug residues in wastewaters and surface waters as rivers and streams may constitute a problem for the environment, with consequences on the ecosystem and also on the human health. This paper deals with the study of the photo-induced transformation of amiloride, an orally administered diuretic agent, ...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2008.01.014

    authors: Calza P,Massolino C,Monaco G,Medana C,Baiocchi C

    更新日期:2008-09-29 00:00:00

  • Determination of debrisoquine and 4-hydroxydebrisoquine in urine by high-performance liquid chromatography with fluorescence detection after solid-phase extraction.

    abstract::A simple, selective and sensitive method has been developed to determine debrisoquine and 4-hydroxydebrisoquine in human urine. Separation of the analytes was obtained using a mobile phase of 0.1 M sodium dihydrogen phosphate-acetonitrile (87:13, v/v) and a muBondapak C18 column. The column effluent was monitored with...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(93)80184-3

    authors: Bozkurt A,Basci NE,Isimer A,Kayaalp SO

    更新日期:1993-08-01 00:00:00

  • Chemical and physicochemical properties of the high cohesive silicone gel from Poly Implant Prothèse (PIP) breast prostheses after explantation: a preliminary, comparative analytical investigation.

    abstract::Aim of this work was to gain a deeper insight into the analytical profile of the macromolecular and LMW fractions of polymeric silicones present in breast implants. The study was conducted on silicone gel samples from (i) breast prostheses (Poly Implant Prothèse, PIP) explanted from a patient that needed their therape...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2013.01.040

    authors: Beretta G,Malacco M

    更新日期:2013-05-05 00:00:00

  • Determination of residual 4-nitrobenzaldehyde in chloramphenicol and its pharmaceutical formulation by HPLC with UV/Vis detection after derivatization with 3-nitrophenylhydrazine.

    abstract::4-Nitrobenzaldehyde is the synthetic raw material and an important photodegradation product of chloramphenicol. With a structural "alert" of human genotoxic potential and reported mutagenicity, this compound should be controlled in drug substances as a potential genotoxic impurity. However, current analysis methods re...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2018.04.024

    authors: Luo L,Gu C,Li M,Zheng X,Zheng F

    更新日期:2018-07-15 00:00:00

  • Photochemical stability of nimesulide.

    abstract::HPLC and TLC methods for monitoring of the photochemical stability of nimesulide are presented. Solution of nimesulide sodium salt was exposed to the light of wavelengths 254 nm. The presence of degradation products (2-phenoxy4-nitroaniline and methanesulfonic acid) was observed. In the exposed sample, 2-phenoxy4-nitr...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(02)00659-3

    authors: Kovaríková P,Mokrý M,Klimes J

    更新日期:2003-03-26 00:00:00

  • Spectrophotometric determination of fluoride in dosage forms and dental preparations.

    abstract::The method is based upon the reaction between fluoride ions and the coloured complex of Fe(III) with methyl salicylate to form the stable, colourless hexaflouride complex of iron. The conditions of the method (pH, time and combination ratio) were studied and a standard curve was obtained for 0.01-0.08 mg NaF ml-1, at ...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(96)01745-1

    authors: Săndulescu R,Florean E,Roman L,Mirel S,Oprean R,Suciu P

    更新日期:1996-06-01 00:00:00

  • Quantification of gliclazide by semi-micro high-performance liquid chromatography: application to a bioequivalence study of two formulations in healthy subjects.

    abstract::The objective of the present study was to evaluate the bioequivalence of two formulations of gliclazide in healthy human volunteers. Bioequivalence of the two formulations was determined in 20 healthy subjects with a single-dose, two-period, crossover study. A new high-performance liquid chromatographic method for the...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/j.jpba.2004.02.025

    authors: Park JY,Kim KA,Kim SL,Park PW

    更新日期:2004-06-29 00:00:00

  • Enantioselective determination of felodipine in human plasma by chiral normal-phase liquid chromatography and electrospray ionisation mass spectrometry.

    abstract::An analytical method was developed for the determination of the enantiomers of felodipine, a dihydropyridine-type calcium antagonist, in human blood plasma. Felodipine was extracted from plasma using toluene as extraction solvent. The enantiomers were separated on a cellulose tris(4-methyl benzoate) stationary phase (...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(01)00582-9

    authors: Lindmark B,Ahnoff M,Persson BA

    更新日期:2002-01-15 00:00:00

  • A comparative study of the reversed-phase HPLC retention behaviour of S-adenosyl-L-methionine and its related metabolites on Hypersil ODS and Supelcosil LC-ABZ stationary phases.

    abstract::S-Adenosyl-L-methionine (SAM) and its metabolites S-adenosyl-L-homocysteine (SAH) and methyl-thioadenosine (MTA) are endogenous compounds that are heavily involved in a variety of biochemical processes, and have therefore been the target for several assays in body fluids and tissues. Reversed-phase chromatographic beh...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(93)80029-z

    authors: Valkó K,Hamedani MP,Ascah TL,Gibbons WA

    更新日期:1993-04-01 00:00:00

  • A preliminary study of beta-cyclodextrin/metoprolol tartrate inclusion complex for potential enantiomeric separation.

    abstract::The inclusion complex formation between Metoprolol tartarata (MeT) and beta-cyclodextrin (beta-CD) has been investigated using hyperchromic shift at lambda(max) 274.4 nm of MeT. Different parameters such as stirring time, solvent composition (aqueous and aqueous/methanol solutions with methanol content up to 50%), pH ...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(00)00555-0

    authors: Radulovic DM,Karljikovic-Rajic KD,Lucic BM,Vujic ZB

    更新日期:2001-03-01 00:00:00

  • Simultaneous stereoselective analysis of venlafaxine and O-desmethylvenlafaxine enantiomers in clinical samples by capillary electrophoresis using charged cyclodextrins.

    abstract::Capillary electrophoresis (CE) was used for the simultaneous chiral determination of venlafaxine (Vx), a new antidepressant drug and its main active metabolite. O-desmethyl venlafaxine (ODV). Among the charged cyclodextrins (CD) tested, phosphated gamma-CD was the most appropriate. Resolution of Vx and ODV was obtaine...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(00)00280-6

    authors: Rudaz S,Stella C,Balant-Gorgia AE,Fanali S,Veuthey JL

    更新日期:2000-08-01 00:00:00

  • 600 MHz 1H-NMR spectroscopy of human cerebrospinal fluid: effects of sample manipulation and assignment of resonances.

    abstract::Extensive assignments of resonances in the 600 MHz 1H-NMR spectra of cerebrospinal fluid are reported. These have been achieved by the measurement of a combination of two-dimensional experiments comprising homonuclear J-resolved, COSY45, and double-quantum filtered COSY (DQCOSY) spectra. By these means the previous to...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(93)80171-v

    authors: Sweatman BC,Farrant RD,Holmes E,Ghauri FY,Nicholson JK,Lindon JC

    更新日期:1993-08-01 00:00:00

  • Evaluation of mobile phase gradient supercritical fluid chromatography for impurity profiling of pharmaceutical compounds.

    abstract::The use of gradient supercritical fluid chromatography (SFC) for the impurity profiling of pharmaceutical products is not widely practiced. Historically, the limited advancement in SFC instrumentation and the lag in column development have resulted in marginal sensitivity, selectivity and reproducibility when compared...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2012.05.025

    authors: Alexander AJ,Hooker TF,Tomasella FP

    更新日期:2012-11-01 00:00:00

  • Determination of a process intermediate of celiprolol and its potential impurities by gradient high-performance liquid chromatography--application of high-low chromatography.

    abstract::3-(3-acetyl-4-hydroxyphenyl)-1,1-diethylurea (A-1354), is a synthetic intermediate of the beta-adrenergic blocker, celiprolol hydrochloride. A liquid chromatographic method has been developed and validated for the determination of bulk A-1354 and its potential impurities. High-low chromatography was used to improve th...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(91)80008-w

    authors: Difeo TJ,Shuster JE

    更新日期:1991-01-01 00:00:00

  • Direct quantitation of free, encapsulated, total doxorubicin and doxorubicinol in stabilized frozen human plasma to support a BE study of liposomal doxorubicin.

    abstract::Regulatory guidance requires the quantification of encapsulated and free doxorubicin for a liposomal doxorubicin injection bioequivalence study. Due to the instability of liposome formulations in plasma samples, the release of free drug from the liposomal encapsulated doxorubicin during sample handling would result in...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2020.113388

    authors: Ji Y,Zhang X,Liu J,Chen Y,Meng M,Li C,Wang L

    更新日期:2020-09-10 00:00:00

  • LC separation of calcipotriol from its photodegradation products and protection possibilities using adjuvants.

    abstract::Mobile phase optimization and reversed-phase column characteristics were used to separate photodegradation products from the parent compound, 24-cyclopropyl-9-,10-secochola-5,7,10(19),22-tetraene-1alpha,3beta,24-triol (calcipotriol). Separation between calcipotriol and its degradation products was obtained with an ace...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(01)00390-9

    authors: Cirunay JJ,Vander Heyden Y,Plaizier-Vercammen J

    更新日期:2001-08-01 00:00:00

  • Characterization of interaction and the effect of carbamazepine on the structure of human serum albumin.

    abstract::The binding of carbamazepine (CBZ) to human serum albumin (HSA) was investigated under simulative physiological conditions. In this study, intrinsic fluorescence of tryptophan-214 in HSA was monitored upon the addition of CBZ. Binding constant of CBZ-HSA was calculated by the remarkable static quenching effect of CBZ ...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2010.05.025

    authors: Kalanur SS,Seetharamappa J,Kalalbandi VK

    更新日期:2010-11-02 00:00:00

  • A comparison of matrix resolution method, ratio spectra derivative spectrophotometry and HPLC method for the determination of thiamine HCl and pyridoxine HCl in pharmaceutical preparation.

    abstract::A comparison of two spectrophotometric methods and a HPLC method were described in this work for the analysis of pyridoxine hydrochloride and thiamine hydrochloride in a vitamin combination. In the first method, A(1)1 (1%, 1 cm) values of these two compounds were calculated using absorbances measured at 246.8 and 290....

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(00)00308-3

    authors: Din E,Kökdil G,Onur F

    更新日期:2000-07-01 00:00:00

  • Simultaneous determination of benazepril hydrochloride and hydrochlorothiazide in tablets by second-order derivative spectrophotometry.

    abstract::A second-order derivative spectrophotometric method for the simultaneous determination of benazepril hydrochloride and hydrochlorothiazide in pharmaceutical dosage forms is described. The determination of benazepril hydrochloride in the presence of hydrochlorothiazide was achieved by measuring the second-order derivat...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(99)00134-x

    authors: Panderi IE

    更新日期:1999-11-01 00:00:00

  • Pharmacokinetic study of matrine, oxymatrine and oxysophocarpine in rat plasma after oral administration of Sophora flavescens Ait. extract by liquid chromatography tandem mass spectrometry.

    abstract::A rapid, sensitive and selective high-performance liquid chromatography tandem mass spectrometric method (HPLC-MS) has been developed and validated for the simultaneous determination of matrine (MT), oxymatrine (OMT) and oxysophocarpine (OSP) in rat plasma after oral administration of Sophora flavescens Ait. extract u...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2008.03.019

    authors: Zhang L,Liu W,Zhang R,Wang Z,Shen Z,Chen X,Bi K

    更新日期:2008-08-05 00:00:00

  • Quantitative risk assessment in classification of drugs with identical API content.

    abstract::When combating counterfeits it is equally important to recognize fakes and to avoid misclassification of genuine samples. This study presents a general approach to the problem using a newly-developed method called Data Driven Soft Independent Modeling of Class Analogy. The possibility to collect representative data fo...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2014.05.033

    authors: Rodionova OY,Balyklova KS,Titova AV,Pomerantsev AL

    更新日期:2014-09-01 00:00:00

  • Direct chemical ionization-mass spectrometric profiling of urine in premenstrual syndrome.

    abstract::In search of the pathophysiological background of premenstrual syndrome, direct chemical ionization-mass spectrometric profiling was applied to urine samples from 17 patients and 18 control subjects, collected on days 11 and 25 of the menstrual cycle. Oestrogenic compounds and hippuric acid were found to be involved i...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(89)80127-x

    authors: Tas AC,van den Berg H,Odink J,Korthals H,Thissen JT,van der Greef J

    更新日期:1989-01-01 00:00:00

  • Development of a simple method for quantitation of methanesulfonic acid at low ppm level using hydrophilic interaction chromatography coupled with ESI-MS.

    abstract::A simple, sensitive and robust method using HILIC-ESI-MS has been developed for the determination of methane sulfonic acid (MSA) at low ppm level in order to verify the effectiveness of controlling the formation of genotoxic sulfonate esters in the downstream synthetic step, by which produces active pharmaceutical ing...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2014.08.019

    authors: Huang Z,Francis R,Zha Y,Ruan J

    更新日期:2015-01-01 00:00:00

  • UPLC-MS/MS method for the determination of talazoparib in rat plasma and its pharmacokinetic study.

    abstract::In the present study, an accurate and sensitive ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the determination of plasma talazoparib concentration in rats was developed and established. The purpose of chromatographic separation of talazoparib and the internal standard (bosut...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/j.jpba.2019.112850

    authors: Ye L,Chen J,Li SL,Zhu YL,Xie S,Du X

    更新日期:2020-01-05 00:00:00

  • Determination of ambroxol in human plasma using LC-MS/MS.

    abstract::A sensitive and selective liquid chromatographic method coupled with tandem mass spectrometry (LC-MS/MS) was developed for the quantification of ambroxol in human plasma. Domperidone was used as internal standard, with plasma samples extracted using diethyl ether under basic condition. A centrifuged upper layer was th...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/s0731-7085(03)00059-1

    authors: Kim H,Yoo JY,Han SB,Lee HJ,Lee KR

    更新日期:2003-06-01 00:00:00

  • Spectrophotometric determination of cimetidine in the presence of its acid-induced degradation products.

    abstract::Cimetidine has been determined in the presence of its acid-induced degradation products using a second derivative (D2-) spectrophotometric method (method I) or a colorimetric method (method II). The former is based on D2-value measurement at 216 nm, whilst the latter depends on charge-transfer complexation with dichlo...

    journal_title:Journal of pharmaceutical and biomedical analysis

    pub_type: 杂志文章

    doi:10.1016/0731-7085(91)80196-g

    authors: Bedair MM,Elsayed MA,Korany MA,Fahmy OT

    更新日期:1991-01-01 00:00:00