Development of a human immunodeficiency virus vector-based, single-cycle assay for evaluation of anti-integrase compounds.

Therapeutic strategies aimed at inhibiting human immunodeficiency virus type 1 (HIV-1) replication employ a combination of drugs targeted to two viral enzymes (reverse transcriptase and protease) and to the viral entry/fusion step. However, the high propensity of HIV-1 to develop resistance makes the development of novel compounds targeting different steps of the HIV-1 life cycle essential. Among these, integrase (IN) inhibitors have successfully passed the early phases of clinical development.

Human terminal deoxynucleotidyl transferases as novel targets for anticancer chemotherapy.

Mammalian terminal deoxyribonucleotidyl transferase (TDT) catalyzes the non-template-directed polymerization of deoxyribonucleoside triphosphates and has a key role in V(D)J recombination during lymphocyte and repertoire development. Over 90% of leukemic cells in acute lymphocytic leukemia and approximately 30% of leukemic cells in the chronic myelogenous leukemia crisis show elevated TDT activity. This finding is connected to a poor prognosis and response to chemotherapy and reduced survival time.

Design, synthesis, biological evaluation, and molecular modeling studies of TIBO-like cyclic sulfones as non-nucleoside HIV-1 reverse transcriptase inhibitors.

TIBO- and TBO-like sulfone derivatives 1 and 2 were designed, synthesized, and tested for their ability to block the replication cycle of HIV-1 in infected cells. The anti-HIV-1 activities of sulfones 3, which were intermediates in the syntheses of 1 and 2, were also evaluated. Surprisingly, the sulfone analogues of TIBO R82913 (compounds 1) were inactive, whereas interesting results were obtained for truncated derivatives 2.

Mariano Semmola (1831-1895): the effect of low protein diet in primary albuminuria.

Mariano Semmola (1831-1895), the first Italian professor of pharmacology and clinical pharmacology, was born into a family of illustrious intellectuals and trained as a fellow of Claude Bernard, Trousseau and Rayer in Paris. His scientific activity included both animal investigations and clinical research. He is credited with important contributions to several areas of clinical medicine, from infectious diseases (cholera, and tuberculosis) to renal, cardiovascular and liver diseases.

Sleeping disorders in patients with end-stage renal disease and chronic kidney disease.

About 85% of patients on maintenance hemodialysis have sleep disorders that depend on comorbidities, age, morning dialytic shift, and blood pressure. They are ameliorated by erythropoietin, by transplantation, and by daily and nocturnal dialysis. Some data exist on sleep disorders in CKD patients, and show that lack of a refreshing sleep is present even at early stages of the disease and may affect 82.

Azimuthal angle correlations for rapidity separated Hadron pairs in d+Au collisions at square root of sNN=200 GeV.

Deuteron-gold (d+Au) collisions at the Relativistic Heavy Ion Collider provide ideal platforms for testing QCD theories in dense nuclear matter at high energy. In particular, models suggesting strong saturation effects for partons carrying small nucleon momentum fraction (x) predict modifications to jet production at forward rapidity (deuteron-going direction) in d+Au collisions. We report on two-particle azimuthal angle correlations between charged hadrons at forward/backward (deuteron/gold going direction) rapidity and charged hadrons at midrapidity in d+Au and p+p collisions at square root of sNN=200 GeV.

Common suppression pattern of eta and pi0 mesons at high transverse momentum in Au + Au collisions at square root S(NN) = 200 GeV.

Inclusive transverse momentum spectra of eta mesons have been measured within p(T) = 2-10 GeV/c at midrapidity by the PHENIX experiment in Au + Au collisions at square root S(NN) = 200 GeV. In central Au+Au the eta yields are significantly suppressed compared to peripheral Au + Au, d + Au, and p + p yields scaled by the corresponding number of nucleon-nucleon collisions. The magnitude, centrality, and p(T) dependence of the suppression is common, within errors, for eta and pi0.

[Palpebral cryptococcosis: case report].

This paper is about a patient with acquired immunodeficiency syndrome empirically treated for miliary tuberculosis. During the clinical evolution the patient presented lesions compromising the right eyelid and tarsal conjunctiva. The initial diagnostic hypothesis was ocular tuberculosis with conjunctival and eyelid involvement.

Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action.

The virally encoded integrase protein is an essential enzyme in the life cycle of the HIV-1 virus and represents an attractive and validated target in the development of therapeutics against HIV infection. Drugs that selectively inhibit this enzyme, when used in combination with inhibitors of reverse transcriptase and protease, are believed to be highly effective in suppressing the viral replication. Among the HIV-1 integrase inhibitors, the beta-diketo acids (DKAs) represent a major lead for anti-HIV-1 drug development.

Thiacalix[3]pyridine produces a stable mononuclear rhodium(II) complex with mutual Jahn-Teller effect.

Thiacalix[3]pyridine (Py3S3) consists of pyridines and bridging sulfur atoms producing a stable octahedral mononuclear Rh(II) complex [Rh(II)(Py3S3)2]2+ showing mutual Jahn-Teller effect, a metal based reversible redox couple of Rh(III/II) at 0.02 V vs. SCE and a g(perpendicular) > g(||) relationship in EPR measurements.

Measurement of identified and inclusive photon second-harmonic parameter and implications for direct photon production in [FORMULA: SEE TEXT] Au+Au.

The azimuthal distribution of identified pi0 and inclusive photons has been measured in [FORMULA: SEE TEXT] Au+Au collisions with the PHENIX experiment at the Relativistic Heavy-Ion Collider (RHIC). The second-harmonic parameter (nu2) was measured to describe the observed anisotropy of the azimuthal distribution. The measured inclusive photon is consistent with the value expected for the photons from hadron decay and is also consistent with the lack of direct photon signal over the measured pT range 1-6 GeV/c.

Nuclear modification of electron spectra and implications for heavy quark energy loss in Au+Au collisions at [FORMULA: SEE TEXT].

The PHENIX experiment has measured midrapidity ([FORMULA: SEE TEXT]) transverse momentum spectra ([FORMULA: SEE TEXT]) of electrons as a function of centrality in Au+Au collisions at [FORMULA: SEE TEXT]. Contributions from photon conversions and from light hadron decays, mainly Dalitz decays of pi0 and eta mesons, were removed. The resulting nonphotonic electron spectra are primarily due to the semileptonic decays of hadrons carrying heavy quarks.

Single electrons from heavy-flavor decays in collisions at.

The invariant differential cross section for inclusive electron production in p+p collisions at [FORMULA: SEE TEXT] has been measured by the PHENIX experiment at the BNL Relativistic Heavy Ion Collider over the transverse momentum range 0.4 View Article and Find Full Text PDF

J/psi production and nuclear effects for d + Au and p + p collisions at square root of S(NN) = 200 GeV.

J/psi production in d + Au and p + p collisions at square root of S(NN) = 200 GeV has been measured by the PHENIX experiment at rapidities -2.2 < y < +2.4.

Sleeping disorders in early chronic kidney disease.

Studies in patients on maintenance hemodialysis have disclosed a high prevalence of sleeping disorders, which have been linked to various factors including blood urea levels, creatinine levels, parathyroid hormone levels, anemia, systolic and diastolic blood pressure, quality of life, disease intrusiveness, and comorbidities. In contrast, few studies have been performed in patients with chronic kidney disease (CKD), who represent the target of the present study. A group of 52 CKD patients were enrolled after characterization of their renal function.

Insomnia and its comorbidities in chronic kidney disease.

Sleep disorders are among the factors that can reduce the quality of life in patients with chronic kidney disease. Chronic kidney disease patients could benefit from an accurate evaluation and treatment of insomnia because this sleep disorder is associated with a high persistence-relapse rate, poor physical health, and mental disease (anxiety, depression) both in terms of comorbidity and antecedent. A multilayer evaluation of insomnia is possible because of valid and reliable instruments (both objective and subjective).

Measurement of transverse single-spin asymmetries for midrapidity production of neutral pions and charged hadrons in polarized p + p collisions at square root(s) = 200 GeV.

Transverse single-spin asymmetries to probe the transverse-spin structure of the proton have been measured for neutral pions and nonidentified charged hadrons from polarized proton-proton collisions at midrapidity and square root(s) = 200 GeV. The data cover a transverse momentum (pT) range 1.0-5.

Pharmacological testing of anisocoria.

Anisocoria, or a difference in pupil size, is a common condition. Its aetiology ranges from benign to life-threatening conditions. The clinical evaluation of anisocoria is discussed, emphasising the pharmacological aids (e.

Simple but highly effective three-dimensional chemical-feature-based pharmacophore model for diketo acid derivatives as hepatitis C virus RNA-dependent RNA polymerase inhibitors.

A molecular modeling strategy using aryl diketo acid (ADK) derivatives recently reported in the literature as hepatitis C virus (HCV) polymerase inhibitors was designed. A 3D chemical-feature-based pharmacophore model was developed using Catalyst software, which produced 10 pharmacophore hypotheses. The top-ranked one (Hypo 1), characterized by a high correlation coefficient (r = 0.

A complete series of copper(II) halide complexes (X = F, Cl, Br, I) with a novel Cu(II)-C(sp3) bond.

A complete series of copper(ii) halide complexes [CuX(tptm)](X = F (), Cl (), Br (), I (); tptm = tris(2-pyridylthio)methyl) with a novel Cu(II)-C(sp(3)) bond has been prepared by the reactions of [Cu(tptm)(CH(3)CN)]PF(6)(.PF(6)) with corresponding halide sources of KF or n-Bu(4)NX (X = Cl, Br, I), and the trigonal bipyramidal structures have been confirmed by X-ray crystallography and/or EPR spectroscopy. The iodide complex easily liberates the iodide anion in acetonitrile forming the acetonitrile complex as a result.

Saturation of azimuthal anisotropy in Au + Au collisions at (square root)s(NN) = 62-200 GeV.

New measurements are presented for charged hadron azimuthal correlations at midrapidity in Au+Au collisions at (square root)s(NN) = 62.4 and 200 GeV. They are compared to earlier measurements obtained at (square root)s(NN) = 130 GeV and in Pb + Pb collisions at (square root)s(NN) = 17.

Centrality dependence of direct photon production in (square root)S(NN) = 200 GeV Au + Au collisions.

The first measurement of direct photons in Au + Au collisions at (square root)S(NN) = 200 GeV is presented. The direct photon signal is extracted as a function of the Au + Au collision centrality and compared to next-to-leading order perturbative quantum chromodynamics calculations. The direct photon yield is shown to scale with the number of nucleon-nucleon collisions for all centralities.