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The Natural History of Teneurins: A Billion Years of Evolution in Three Key Steps.

Ron Wides

Front Neurosci 2019 15;13:109. Epub 2019 Mar 15.

The Mina and Everard Goodman Faculty of Life Sciences, Bar-Ilan University, Ramat Gan, Israel.

The entire evolutionary history of the animal gene family, Teneurin, can be summed up in three key steps, plus three salient footnotes. In a shared ancestor of all bilaterians, the first step began with gene fusions that created a protein with an amino-terminal intracellular domain bridged via a single transmembrane helix to extracellular EGF-like domains. This first step was completed with a further gene fusion: an additional carboxy-terminal stretch of about 2000 amino acids (aa) was adopted, as-a-whole, from bacteria. Read More

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Dihydroartemisinin and its Analogs: A New Class of Antitubercular Agents.

Curr Top Med Chem 2019 ;19(8):594-599

Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, India.

Background: Tuberculosis is one of the leading causes of mortality worldwide. Resistance against the frontline anti-tubercular drugs has worsened the already alarming situation, which requires intensive drug discovery to develop new, more effective, affordable and accessible anti-tubercular agents possessing novel modes of action.

Objective: Chemical transformation of dihydroartemisinin for anti-tubercular lead optimization. Read More

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STARTING-SICH Nomogram to Predict Symptomatic Intracerebral Hemorrhage After Intravenous Thrombolysis for Stroke.

Stroke 2018 02 8;49(2):397-404. Epub 2018 Jan 8.

From the DAI di Neuroscienze, Azienda Ospedaliera Universitaria Integrata, Verona, Italy (M.C., S.F., C.Z., P.B., B.B.); Emergency Department, Girolamo Fracastoro Hospital San Bonifacio (Verona), Italy (G.T.); and Dipartimento di Neurologia e Psichiatria, Università degli Studi di Roma "La Sapienza," Italy (D.T.).

Background And Purpose: Symptomatic intracerebral hemorrhage (sICH) is a rare but the most feared complication of intravenous thrombolysis for ischemic stroke. We aimed to develop and validate a nomogram for individualized prediction of sICH in intravenous thrombolysis-treated stroke patients included in the multicenter SITS-ISTR (Safe Implementation of Thrombolysis in Stroke-International Stroke Thrombolysis Register).

Methods: All patients registered in the SITS-ISTR by 179 Italian centers between May 2001 and March 2016 were originally included. Read More

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February 2018

Proposed Biotransformation Pathways for New Metabolites of Paralytic Shellfish Toxins Based on Field and Experimental Mussel Samples.

J Agric Food Chem 2017 Jul 27;65(27):5494-5502. Epub 2017 Jun 27.

College of Environmental Science and Engineering, Ocean University of China , Qingdao, Shandong 266100, People's Republic of China.

A seafood poisoning event occurred in Qinhuangdao, China, in April 2016. Subsequently, the causative mussels (Mytilus galloprovincialis) were harvested and analyzed to reveal a high concentration [∼10 758 μg of saxitoxin (STX) equiv kg] of paralytic shellfish toxins (PSTs), including gonyautoxin (GTX)1/4 and GTX2/3, as well as new metabolites 11-hydroxy-STX (M2), 11,11-dihydroxy-STX (M4), open-ring 11,11-dihydroxy-STX (M6), 11-hydroxy-neosaxitoxin (NEO) (M8), and 11,11-dihydroxy-NEO (M10). To understand the origin and biotransformation pathways of these new metabolites, uncontaminated mussels (M. Read More

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Phase 1 dose-escalation study of IV ixazomib, an investigational proteasome inhibitor, in patients with relapsed/refractory lymphoma.

Blood Cancer J 2014 Oct 17;4:e251. Epub 2014 Oct 17.

Weill Cornell Medical College, New York, NY, USA.

Ixazomib is an investigational proteasome inhibitor that has shown preclinical activity in lymphoma models. This phase 1 study assessed the safety, tolerability, maximum tolerated dose (MTD), pharmacokinetics, pharmacodynamics and preliminary activity of intravenous (IV) ixazomib in relapsed/refractory lymphoma patients who had received ⩾ 2 prior therapies. Thirty patients with a range of histologies received ixazomib 0. Read More

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October 2014

A phase II randomized study evaluating the addition of iniparib to gemcitabine plus cisplatin as first-line therapy for metastatic non-small-cell lung cancer.

Ann Oncol 2014 Nov 19;25(11):2156-2162. Epub 2014 Aug 19.

Thoracic Cancer Unit, Department of Medicine, Gustave-Roussy, Villejuif, France.

Background: Iniparib is a novel anticancer agent initially considered a poly (ADP-ribose) polymerase (PARP) inhibitor, but subsequently shown to act via non-selective protein modification through cysteine adducts. This randomized phase II study investigated the addition of iniparib to gemcitabine-cisplatin in metastatic non-small-cell lung cancer (NSCLC) patients.

Patients And Methods: Patients with histologically confirmed stage IV NSCLC were randomized 2 : 1 to receive gemcitabine (1250 mg/m(2), days 1/8) and cisplatin (75 mg/m(2), day 1) with [gemcitabine/cisplatin/iniparib (GCI)] or without [gemcitabine/cisplatin (GC)] iniparib (5. Read More

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November 2014

In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis.

Antimicrob Agents Chemother 2012 Nov 27;56(11):5790-3. Epub 2012 Aug 27.

Global Health Institute, Ecole Polytechnique Fédérale de Lausanne, Lausanne, Switzerland.

Benzothiazinones (BTZ) are a new class of drug candidates to combat tuberculosis that inhibit decaprenyl-phosphoribose epimerase (DprE1), an essential enzyme involved in arabinan biosynthesis. Using the checkerboard method and cell viability assays, we have studied the interaction profiles of BTZ043, the current lead compound, with several antituberculosis drugs or drug candidates against Mycobacterium tuberculosis strain H37Rv, namely, rifampin, isoniazid, ethambutol, TMC207, PA-824, moxifloxacin, meropenem with or without clavulanate, and SQ-109. No antagonism was found between BTZ043 and the tested compounds, and most of the interactions were purely additive. Read More

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November 2012

Phase I studies of AVE9633, an anti-CD33 antibody-maytansinoid conjugate, in adult patients with relapsed/refractory acute myeloid leukemia.

Invest New Drugs 2012 Jun 26;30(3):1121-31. Epub 2011 Apr 26.

Hematology and Oncology Department, Saint-Antoine Hospital, AP-HP, Paris, France.

The efficacy of anti-CD33 immunoconjugates had been previously demonstrated for gemtuzumab-ozogamicin. AVE9633 is an anti-CD33-maytansine conjugate created by ImmunoGen Inc. Phase I trials of AVE9633 were performed in patients with AML to evaluate tolerability, pharmacokinetics and pharmacodynamics. Read More

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Phase II study of gemcitabine combined with oxaliplatin in relapsed or refractory paediatric solid malignancies: An innovative therapy for children with Cancer European Consortium Study.

Eur J Cancer 2011 Jan 11;47(2):230-8. Epub 2010 Oct 11.

Institut Gustave Roussy, Université Paris-Sud, 39 rue Camille Desmoulins, 94805 Villejuif, France.

Aim: To assess objective response rates after 4 cycles of gemcitabine in combination with oxaliplatin in children and adolescents with relapsed or refractory solid tumours.

Methods: This multicentre, non-randomised Phase II study included five strata: neuroblastoma, osteosarcoma, medulloblastoma and other CNS tumours strata with two-stage Simon designs and a miscellaneous, extra-cranial solid tumour stratum with descriptive design. Eligibility criteria included: age 6 months to 21 years; measurable, relapsed or refractory solid malignancy; no more than one previous salvage therapy. Read More

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January 2011

[Benefits of an add-on treatment with the synthetic cannabinomimetic nabilone on patients with chronic pain--a randomized controlled trial].

Wien Klin Wochenschr 2006 Jun;118(11-12):327-35

Confraternität, Privatklinik Josefstadt, Wien, Austria.

Objective: The aim of this study was to investigate the efficacy and efficiency of an add-on treatment with the synthetic cannabinomimetic nabilone on patients with chronic pain. Of major interest were the evaluation of the influence the treatment had on pain and on quality of life as well as the subjective assessment of positive effects and side effects by the study participants.

Methods: The placebo-controlled double-blinded pilot study was divided into a 14 week cross-over period (two 4 week medication phases plus wash-out phases) followed by a 16 week medication switch period with free choice of the study drugs (drug A and drug B) by the study participants. Read More

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A factorial study of combination hypertension treatment with metoprolol succinate extended release and felodipine extended release results of the Metoprolol Succinate-Felodipine Antihypertension Combination Trial (M-FACT).

Am J Hypertens 2006 Apr;19(4):388-95

Department of Medicine and Pharmacology, New York Medical College, Valhalla, New York 10595, USA.

Background: Many hypertensive patients require combination therapy to achieve target blood pressure (BP). beta-Blockers and dihydropyridine calcium channel blockers are effective as monotherapy in hypertensive patients and have complementary mechanisms for lowering BP.

Methods: This multicenter, randomized, placebo-controlled, unbalanced factorial study included a 4- to 5-week single-blind placebo, 9-week, double-blind treatment as well as a 2-week double-blind, down-titration period. Read More

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Phase I study of intermittent and chronomodulated oral therapy with capecitabine in patients with advanced and/or metastatic cancer.

BMC Cancer 2006 Feb 24;6:42. Epub 2006 Feb 24.

Medical Oncology, University Campus Bio-Medico, Rome, Italy.

Background: The combination of capecitabine and gemcitabine at Fixed Dose Rate (FDR) has been demonstrated to be well tolerated, with apparent efficacy in patients with advanced cancers. FDR gemcitabine infusion leads to enhanced intracellular accumulation of drug and possible augmented clinical effect. The goals of this phase I study were to determine the maximum-tolerated dose (MTD) of chronomodulated capecitabine in patients with advanced cancer and to describe the dose-limiting toxicities (DLT), the safety profile of this way of administration. Read More

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February 2006

Physical characterizations of microemulsion systems using tocopheryl polyethylene glycol 1000 succinate (TPGS) as a surfactant for the oral delivery of protein drugs.

J Control Release 2005 Feb;102(2):489-507

Graduate Institute of Pharmaceutical Sciences, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC.

Attempts were to develop microemulsion systems using medium chain triglyceride, deionized water, and TPGS as surfactant for the oral delivery of protein drugs or poorly water-soluble drugs. Phase diagrams were constructed to elucidate the phase behavior of systems composed of Captex 300 and water with D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) as main surfactant, polysorbates (Tween 20, Tween 40, Tween 60 and Tween 80) as adjuvant surfactants, and polyethylene glycols (PEG 400 and PEG 600) and polyols (ethanediol, 1,2-propanediol, 1,3-propanediol, 1,3-butanediol, 1,4-butanediol and glycerin) as cosurfactants. The ratios of TPGS to Tweens, PEGs or polyols (K(m)) were set at 4/1, 2/1, 1/1, 1/2, and 1/4. Read More

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February 2005

The post-antibiotic effects of rokitamycin (a 16-membered ring macrolide) on susceptible and erythromycin-resistant strains of Streptococcus pyogenes.

Int J Antimicrob Agents 2004 Sep;24(3):254-60

Center of Respiratory Pharmacology, Department of Pharmacology, School of Medicine, University of Milan, Via Vanvitelli 32, 20129 Milano, Italy.

The post-antibiotic effects (PAEs) on susceptible and erythromycin-resistant strains of Streptococcus pyogenes (M phenotype and inducibly resistant) of rokitamycin and erythromycin were investigated in vitro using microbiological impedance measurement. Exposure of susceptible S. pyogenes strains to 1/4, 1/2, 1 and 2 MIC erythromycin and rokitamycin resulted in PAEs of rokitamycin in the same order of magnitude as those of erythromycin and that were dose dependent. Read More

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September 2004

Phase I trial of fludarabine and paclitaxel in non-Hodgkin's lymphoma.

Med Oncol 2003 ;20(1):53-8

Department of Medicine, Jacobi Medical Center, Bronx, NY, USA.

Fludarabine is an active agent in low-grade non-Hodgkin's lymphoma and chronic lymphocytic leukemia. Paclitaxel is also active in patients with refractory lymphoma, and preclinical data suggest an additive effect with fludarabine in vitro. We performed a phase I trial of fludarabine (25 mg/m(2) d 1-3) plus a 3-h infusion of paclitaxel (125, 150, or 175 mg/m(2)) on d 3 every 28 d in 13 patients with non-Hodgkin's lymphoma. Read More

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October 2003

Cholinergic modulation of basal and amphetamine-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens.

Brain Res 2002 Dec;958(1):176-84

Division of Psychopharmacology, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, TN 37212, USA.

Behavioral evidence suggests that muscarinic/cholinergic inhibition of brain dopaminergic activity may be a useful principle for developing novel antipsychotic drugs (APDs). Thus, oxotremorine, a muscarinic agonist, attenuates amphetamine-induced locomotor activity in rodents, an effect also produced by a wide variety of proven APDs, whereas scopolamine, a muscarinic antagonist, has the opposite effect. Since atypical APDs such as clozapine, olanzapine, risperidone, ziprasidone and quetiapine, increase brain acetylcholine as well as dopamine (DA) release in a region-specific manner, their effects on cholinergic and dopaminergic neurotransmission may also contribute to various actions of these drugs. Read More

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December 2002

Infusional vinorelbine in relapsed or refractory lymphomas.

Leuk Lymphoma 2000 Oct;39(3-4):291-9

Department of Lymphoma and Myeloma, The University of Texas M.D. Anderson Cancer Center, Houston, Texas 77030, USA.

Vinorelbine (Navelbine is a semisynthetic vinca alkaloid devoid of serious neurotoxicity. When given weekly vinorelbine has documented activity against many tumors, including lymphomas. Since weekly schedules cannot be easily incorporated in combination regimens, we tested an infusional schedule of vinorelbine given every 21 days in adults with relapsed or refractory lymphoma. Read More

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October 2000

Oxidation of thymine to 5-formyluracil in DNA promotes misincorporation of dGMP and subsequent elongation of a mismatched primer terminus by DNA polymerase.

J Biol Chem 2001 May 29;276(19):16501-10. Epub 2001 Jan 29.

Department of Mathematical and Life Sciences, Graduate School of Science, Hiroshima University, Higashi-Hiroshima 739-8526, Japan.

5-Formyluracil (fU) is a major oxidative thymine lesion generated by ionizing radiation and reactive oxygen species. In the present study, we have assessed the influence of fU on DNA replication to elucidate its genotoxic potential. Oligonucleotide templates containing fU at defined sites were replicated in vitro by Escherichia coli DNA polymerase I Klenow fragment deficient in 3'-5'-exonuclease. Read More

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Action of free radical in podophyllic acid piperindyl hydrazone nitroxide radical on its antitumor activity and toxicity.

Zhongguo Yao Li Xue Bao 1999 Jun;20(6):571-6

Department of Biology, Lanzhou University, China.

Aim: To study the action of free radical in the spin-labeled podophyllotoxin derivative, podophyllic acid piperindyl hydrazone nitroxide radical (GP-1) on its antitumor activity and toxicity, by comparison with those of its free radical reduced product, podophyllic acid piperindyl hydrazone (GP-1-H).

Methods: After treatment with GP-1 and GP-1-H, the inhibitory effects on the growth of mouse transplantable tumors were determined; MTT formazan formation, [3H]deoxythymidine ([3H]TdR) incorporation, cell cycle progression, and mitotic index of SGC-7901 or L1210 cells were measured; the acute toxicity and immune function of mice were assayed.

Results: At doses of 1/6 and 1/12 LD50, the inhibitory rates against Lewis lung carcinoma were 60. Read More

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Comparative effects of L-methionine, S-adenosyl-L-methionine and 5'-methylthioadenosine on the growth of preneoplastic lesions and DNA methylation in rat liver during the early stages of hepatocarcinogenesis.

Anticancer Res 1991 Jul-Aug;11(4):1617-24

Istituto di Patologia Generale, Università di Sassari, Italy.

Male Wistar rats, initiated with diethylnitrosamine (DENA), were subjected to a selection treatment, according to the "resistant hepatocyte" model, followed or not followed by phenobarbital (PB). Rats received, for 3 weeks after selection, 4 i.m. Read More

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January 1992

Sodium channel comodification with full activator reveals veratridine reaction dynamics.

Mol Pharmacol 1990 Feb;37(2):144-8

Institut für Pharmakologie und Toxikologie, Technischen Universität München, FRG.

Veratridine association and dissociation rates were determined at single sodium channels in outside-out patches of cultured ventricular myocytes obtained from late-fetal rat hearts. In single cardiac sodium channels depolarized from -110 to -30 mV, intracellular veratridine induced a long lasting (tau = 0.48 sec) open state with small current amplitude (-0. Read More

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February 1990

Control of parturient behaviour by prostaglandin F-2 alpha in the tammar wallaby (Macropus eugenii).

G Shaw

J Reprod Fertil 1990 Jan;88(1):335-42

Department of Anatomy, Monash University, Clayton, Victoria, Australia.

Nulliparous female tammar wallabies during the non-breeding season and adult male wallabies were treated with PGF-2 alpha at doses of 0.008, 0.04, 0. Read More

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January 1990

Prostaglandins E and F, and 19-hydroxylated E and F (series I and II) in semen of fertile men. Gas and liquid chromatographic separation with selected ion detection.

J M Tusell E Gelpi

J Chromatogr 1980 Mar;181(3-4):295-310

Low concentrations of prostaglandins (PG) could be related to male clinical infertility althought relevant experimental data are scarce. The aim of this work is to establish reliable seminal PG levels in fertile men by rigorous sample control, to prevent degradation, and by rapid and simple extraction and assay procedures. Single semen samples from healthy fertile men were immediately centrifuged (within 30 min of ejaculation) adding PGF2 alpha D4 to the seminal plasma as internal standard. Read More

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Estrogenic properties of 3,9-dihydroxy-7,12-dimethylbenz[a]anthracene in rats.

J Natl Cancer Inst 1979 Jun;62(6):1585-8

Previously, the 3,9-dihydroxy derivative of benz[a]-anthracene was shown to be weakly estrogenic. The availability of the related diol of the mammary carcinogen dimethylbenz[a]-anthracene, i.e. Read More

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[Determination of glycoside concentrations in human tissue by means of radioimmunoassay (author's transl)].

Klin Wochenschr 1977 Jan;55(1):23-30

After extraction of myocardial and skeletal muscle biopsy and autopsy specimens tissue glycoside concentrations can be determined by radioimmunoassay. Total tissue extraction of digoxin and beta-methyl-digoxin varies between 87 and 95%, the variation coefficient for repeated determinations is 10.2%. Read More

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January 1977
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