A72405

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Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.

Qian Wu et al.

Journal of medicinal chemistry, 48(23), 7243-7252 (2005-11-11)

The X-ray structure of human phenylethanolamine N-methyltransferase (hPNMT) complexed with its product, S-adenosyl-L-homocysteine (4), and the most potent inhibitor reported to date, SK&F 64139 (7), was used to identify the residues involved in inhibitor binding. Four of these residues, Val53

Disulfide-linked dimers of human adrenaline synthesizing enzyme PNMT are catalytically active.

Christine L Gee et al.

Biochimica et biophysica acta, 1750(1), 82-92 (2005-05-17)

The crystal structure of human phenylethanolamine N-methyltransferase (hPNMT) reveals a disulfide-linked dimer, despite the presence of reducing agent in the crystallisation conditions. By removing the reducing agent, hPNMT crystals grow more rapidly and at lower protein concentrations. However, it was

Targeted cytotoxic somatostatin analog AN-162 inhibits growth of human colon carcinomas and increases sensitivity of doxorubicin resistant murine leukemia cells.

Florian Hohla et al.

Cancer letters, 294(1), 35-42 (2010-02-17)

The effect of the targeted cytotoxic somatostatin (SST) analog AN-162, consisting of doxorubicin (DOX) conjugated to SST carrier RC-121, was investigated on the growth of human colorectal cancer (CRC) cell lines HT-29, HCT-15, and HCT-116 and a DOX-resistant mouse leukemia

MMA/MPEOMA/VSA copolymer as a novel blood-compatible material: ex vivo platelet adhesion study.

Jin Ho Lee et al.

Journal of materials science. Materials in medicine, 15(2), 155-159 (2004-08-28)

MMA/MPEOMA/VSA copolymers with both pendant polyethylene oxide (PEO) side chains and negatively chargeable side groups were synthesized by random copolymerization of methyl methacrylate (MMA), methoxy PEO monomethacrylate (MPEOMA; PEO mol. wt, 1000), and vinyl sulfonic acid sodium salt (VSA) monomers

The inhibitory effect of a novel cytotoxic somatostatin analogue AN-162 on experimental glioblastoma.

E Pozsgai et al.

Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme, 42(11), 781-786 (2010-07-29)

Glioblastoma multiforme is the most common and most aggressive type of high grade tumor with a poor prognosis upon discovery. Based on earlier promising results earned with AN-162, a doxorubicin molecule linked to somatostatin (SST) analogue RC-160, it was our

Hypoglycemic effects of a beta-agonist, Ro 16-8714, in streptozotocin-diabetic rats: decreased hepatic glucose production and increased glucose utilization in oxidative muscles.

P Ferré et al.

Metabolism: clinical and experimental, 41(2), 180-183 (1992-02-01)

Streptozotocin (STZ)-induced diabetic rats are glycosuric, hyperglycemic, hyperketonemic, overproduce glucose, and have a decreased glucose utilization in oxidative muscles. Treatment with a beta-agonist, Ro 16-8714, decreases the glycosuria, hyperglycemia, hyperketonemia, and hepatic glucose production. Tissue glucose utilization was unchanged, except

Dispersive liquid-liquid microextraction based on solidification of floating organic drop combined with field-amplified sample injection in capillary electrophoresis for the determination of beta(2)-agonists in bovine urine.

Murat Faruk Us et al.

Electrophoresis, 34(6), 854-861 (2013-01-22)

Dispersive liquid-liquid microextraction based on solidification of floating organic drop (DLLME-SFO) was for the first time combined with field-amplified sample injection (FASI) in CE to determine four β(2)-agonists (cimbuterol, clenbuterol, mabuterol, and mapenterol) in bovine urine. Optimum BGE consisted of

Modulation in vivo of beta-adrenergic-receptor subtypes in rat brown adipose tissue by the thermogenic agonist Ro 16-8714.

J P Revelli et al.

The Biochemical journal, 286 ( Pt 3), 743-746 (1992-09-15)

The number of beta 3-adrenergic receptors (AR) in plasma membranes from interscapular brown adipose tissue (IBAT) was decreased by 62% in lean Zucker rats treated with the thermogenic beta-adrenergic agonist Ro 16-8714 as compared with controls after 72 h of

Role of peripheral versus spinal 5-HT(7) receptors in the modulation of pain undersensitizing conditions.

A Brenchat et al.

European journal of pain (London, England), 16(1), 72-81 (2011-08-17)

Several studies have suggested that 5-HT(7) receptors are involved in nociceptive processing but the exact contribution of peripheral versus central 5-HT(7) receptors still needs to be elucidated. In the present study, the respective roles of peripheral and spinal 5-HT(7) receptors

Drugs that suppress hepatic fat synthesis in starved-refed BHE/cdb rats also have an effect on muscle protein synthesis.

J A Parente et al.

Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.), 204(2), 172-179 (1993-11-01)

Simultaneous lipogenesis and protein synthesis as influenced by LY79771, testosterone, or dehydroepiandrosterone in starved/refed rats were studied. Starved-refed BHE/cdb rats were injected with one of these compounds during the 2-day refeed period. Hepatic de novo fatty acid synthesis using tritium

Catecholamine-synthesizing enzymes in the adult and prenatal human testis.

Michail S Davidoff et al.

Histochemistry and cell biology, 124(3-4), 313-323 (2005-07-30)

Catecholamines play functional roles in the mature and developing mammalian testis but the cell types responsible for their local synthesis are still controversially discussed. Here, we demonstrate that four enzymes involved in the biosynthesis of catecholamines, namely, tyrosine hydroxylase (TH)

Limited potentiation of blood pressure response to oral tyramine by brain-selective monoamine oxidase A-B inhibitor, TV-3326 in conscious rabbits.

M Weinstock et al.

Neuropharmacology, 43(6), 999-1005 (2002-11-09)

TV-3326 is a novel cholinesterase inhibitor that produces irreversible brain-selective inhibition of monoamine oxidase (MAO)-A and B and has antidepressant-like activity in rats after chronic oral administration. This study determined whether TV-3326 would cause less potentiation than other irreversible MAO-inhibitors

Inhibition of human non-small cell lung cancers with a targeted cytotoxic somatostatin analog, AN-162.

Andrea Treszl et al.

Peptides, 30(9), 1643-1650 (2009-06-16)

Human non-small cell lung cancers (NSCLCs) express receptors for somatostatin. The cytotoxic analog of somatostatin AN-162 (AEZS-124), consisting of doxorubicin linked to a somatostatin analog RC-121 binds to receptors for somatostatin and is targeted to tumors expressing these receptors. The

Dissection of peripheral and central endogenous opioid modulation of systemic interleukin-1beta responses using c-fos expression in the rat brain.

K M Buller et al.

Neuropharmacology, 49(2), 230-242 (2005-07-05)

In opiate addicts or patients receiving morphine treatment, it has been reported that the immune system is often compromised. The mechanisms responsible for the adverse effects of opioids on responses to infection are not clear but it is possible that

Selective synthesis of racemic 1-11C-labelled norepinephrine, octopamine, norphenylephrine and phenylethanolamine using [11C]nitromethane.

K Någren et al.

Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine, 45(4), 515-521 (1994-04-01)

A new and simple method for the selective condensation of no-carrier-added [11C]nitromethane (1) with various substituted (protected) benzaldehydes to [beta-11C]beta-nitrophenethyl alcohols was developed. This method which utilizes tetrabutylammonium fluoride in THF as a catalyst gave a condensation yield of 80-90%

Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.

Masashi Imanishi et al.

Journal of medicinal chemistry, 51(15), 4804-4822 (2008-07-25)

We designed a series of benzoic acid derivatives containing the biphenyl ether or biphenyl template on the RHS and a phenylethanolaminotetraline (PEAT) skeleton, which was prepared by highly stereoselective synthesis, to generate two structurally different lead compounds ( 10c, 10m)

[Studies on the chemical constituents of Epimedium brevicornum].

Yun Yang et al.

Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials, 32(7), 1051-1053 (2009-10-31)

To study the chemical constituents of Epimedium breviconum. Compounds were purificated with various chromatographic techniques such as silica vacuum liquid chromatography and Sephadex LH-20 column chromatography. Their structures were elucidated by physico-chemical methods and spectral analysis. Ten compounds were obtained

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.

Panayiotis A Procopiou et al.

Journal of medicinal chemistry, 52(8), 2280-2288 (2009-03-26)

A series of saligenin alkoxyalkylphenylsulfonamide beta(2) adrenoceptor agonists were prepared by reacting a protected saligenin oxazolidinone with alkynyloxyalkyl bromides, followed by Sonogashira reaction, hydrogenation, and deprotection. The meta-substituted primary sulfonamide was more potent than the para- and the ortho-analogues. Primary

Phe310 in transmembrane VI of the alpha1B-adrenergic receptor is a key switch residue involved in activation and catecholamine ring aromatic bonding.

S Chen et al.

The Journal of biological chemistry, 274(23), 16320-16330 (1999-05-29)

Pharmacophore mapping of adrenergic receptors indicates that the phenyl ring of catecholamine agonists is involved in receptor binding and activation. Here we evaluated Phe310, Phe311, and Phe303 in transmembrane VI (TMVI), as well as Tyr348 in TMVII of the alpha1B-adrenergic

Effect of a beta-adrenergic agonist on glucose transport and insulin-responsive glucose transporters (GLUT4) in brown adipose tissue of control and obese fa/fa rats.

F Assimacopoulos-Jeannet et al.

Pflugers Archiv : European journal of physiology, 421(1), 52-58 (1992-05-01)

A beta-adrenergic agonist specific for brown adipose tissue, Ro 16-8714, was administered to control and obese insulin-resistant fa/fa rats and glucose utilisation measured in brown adipose tissue using the euglycaemic hyperinsulinaemic clamp combined with the injection of 2-deoxyglucose. Treatment with

Expression of neuropeptide hormone receptors in human adrenal tumors and cell lines: antiproliferative effects of peptide analogues.

C G Ziegler et al.

Proceedings of the National Academy of Sciences of the United States of America, 106(37), 15879-15884 (2009-09-01)

Peptide analogues targeting various neuropeptide receptors have been used effectively in cancer therapy. A hallmark of adrenocortical tumor formation is the aberrant expression of peptide receptors relating to uncontrolled cell proliferation and hormone overproduction. Our microarray results have also demonstrated

Targeting triple-negative breast cancer through the somatostatin receptor with the new cytotoxic somatostatin analogue AN-162 [AEZS-124].

Stephan Seitz et al.

Anti-cancer drugs, 24(2), 150-157 (2012-10-20)

Previously, we have shown that the targeted cytotoxic somatostatin (sst) analogue AN-162 [AZSE-124] inhibits the growth of MDA-MB-231 human breast cancers xenografted into nude mice. In this study, we examined the trafficking of AN-162 into the cell, the expression of

Phenylethanolaminotetralines compete with [3H]dihydroalprenolol binding to rat colon membranes without evidencing atypical beta-adrenergic sites.

M Landi et al.

Biochemical pharmacology, 44(4), 665-672 (1992-08-18)

[3H]Dihydroalprenolol ([3H]DHA) specific binding (determined by the difference in the presence and absence of 20 microM (-)isoprenaline) to rat colon membranes was saturable (Bmax = 39.6 fmol/mg protein), of high affinity (Kd = 0.87 nM) and stereospecific (IC50 330 and

Combinations of growth promoters in veal calves: consequences for screening and confirmation methods.

M J Groot et al.

Zentralblatt fur Veterinarmedizin. Reihe A, 45(6-7), 425-440 (1998-10-30)

This study investigates the influence of low dosages of beta-agonists combined with other growth promoters on screening and confirmation methods in male veal calves. Five groups of four calves were treated for 6 weeks with combinations of low dosages of

A phase I/II trial of epirubicin and docetaxel in locally advanced breast cancer (LABC) on 2-weekly or 3-weekly schedules: NCIC CTG MA.22.

Maureen Elizabeth Trudeau et al.

SpringerPlus, 4, 631-631 (2015-11-07)

This phase I/II neoadjuvant trial (ClinicalTrials.gov identifier NCT00066443) determined maximally-tolerated doses (MTD), dose-limiting toxicities, response-to-therapy, and explored the role of novel response biomarkers. MA.22 accrued T3N0, any N2 or N3, and T4 breast cancer patients. Treatment was 6 cycles of

A quantum dot based electrochemiluminescent immunosensor for the detection of pg level phenylethanolamine A using gold nanoparticles as substrates and electron transfer accelerators.

Panpan Yan et al.

The Analyst, 139(17), 4365-4372 (2014-07-12)

This study reports the development of an electrochemiluminescent (ECL) immunosensor for ultrasensitive detection of phenylethanolamine A (PA) based on CdSe quantum dots (QDs) and gold nanoparticles (GNPs). The GNPs/ovalbumin-PA/anti-PA-QD immunosensor was fabricated layer by layer using GNPs as substrates and

[Studies on asymmetric synthesis of R-phenylethanolamine by whole cells of Arachnia sp. P163].

J L Wang et al.

Sheng wu gong cheng xue bao = Chinese journal of biotechnology, 17(4), 467-470 (2001-11-13)

Effects of various factors on asymmetric synthesis of R-phenylaminoethanol from aminoacetophenone by the whole cells of Arachnia sp. P163 producing alcohol dehydrogenase for phenylethanol amine was investigated. It found that, although the reduction was inhibited by the substrate and the

Subunit arrangement and phenylethanolamine binding in GluN1/GluN2B NMDA receptors.

Erkan Karakas et al.

Nature, 475(7355), 249-253 (2011-06-17)

Since it was discovered that the anti-hypertensive agent ifenprodil has neuroprotective activity through its effects on NMDA (N-methyl-D-aspartate) receptors, a determined effort has been made to understand the mechanism of action and to develop improved therapeutic compounds on the basis

Development and validation of a sensitive method for simultaneous determination of eight β₂-agonists in pork by ultrasonic-assisted extraction and liquid chromatography/tandem mass spectrometry.

Shengdong Pan et al.

Journal of chromatographic science, 53(1), 104-111 (2014-04-29)

A simple and sensitive ultrasonic-assisted extraction coupled with liquid chromatography-tandem quadrupole mass spectrometry was developed for the simultaneous determination of eight β2-agonists (i.e., phenylethanolamine, fenoterol, formoterol, clenbuterol, ractopamine, salbutamol, terbutaline and tulobuterol) in pork. The recovery rate of ultrasonic-assisted extraction

Nicotine stimulates expression of the PNMT gene through a novel promoter sequence.

Marian J Evinger et al.

Journal of molecular neuroscience : MN, 26(1), 39-55 (2005-06-22)

Transcription of the gene encoding the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase (PNMT, E.C. 2.1.1.28) accelerates in response to hormonal and neural stimuli. Cholinergic stimulation through neuronal nicotinic receptors constitutes the primary means for neural regulation of PNMT expression in the adrenal

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