Molecular imaging PET and SPECT approaches for improving productivity of antipsychotic drug discovery and development.

abstract：:AG490 is a tyrphostin originally described as a Janus Activated Kinase (JAK) 2 inhibitor. AG490 also inhibits epidermal growth factor receptor (EGFR) and guanylyl cyclases (GC). More recently, AG490 was associated with oxidative stress protection in experimental acute kidney injury models. We now show that AG490 is al...

journal_title：Current medicinal chemistry

authors： Fernández-Sánchez R,Berzal S,Sánchez-Niño MD,Neria F,Gonçalves S,Calabia O,Tejedor A,Calzada MJ,Caramelo C,Deudero JJ,Ortiz A

更新日期：2012-01-01 00:00:00

abstract：:Heparins are used in "therapeutic doses" for systemic anticoagulation to treat patients who have confirmed venous thromboembolism, or in "prophylactic doses "for the prevention of venous thromboembolism: they are generally lower doses and are employed once a day. Structure-function relationships are strongly influence...

journal_title：Current medicinal chemistry

authors： Stratta P,Karvela E,Canavese C,Quaglia M,Lazzarich E,Fenoglio R,Pergolini P,Bellomo G,Cena T,Magnani C

更新日期：2009-01-01 00:00:00

abstract：:T helper (Th) cells belong to the adaptive immune system and provide an effective and antigen-specific means of host protection. Th17 cells are a subset of Th cells, characterized by the production of the inflammatory cytokines interleukin (IL)-17A (IL-17A) and IL-17F, which bind to a receptor complex comprised of IL-...

journal_title：Current medicinal chemistry

authors： Ghali JR,Holdsworth SR,Kitching AR

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Inflammation is one of the most misunderstood aspects of human health. People have been encouraged to eat foods that have a high antioxidant capacity, and in vitro tests for total antioxidant capacity emerged. They were based on measuring the destruction of oxidized test compounds in direct reactions with th...

journal_title：Current medicinal chemistry

authors： Smith RE

更新日期：2020-01-01 00:00:00

abstract：:gammadelta T lymphocytes are involved in the defence from viral and mycobacterial infections; however they are also responsible for autoimmune reactions. Herein, we discuss the characteristics of these cells, focusing on the mechanism(s) underlying extravasation and tissue localization. We show that Vdelta1 and Vdelta...

journal_title：Current medicinal chemistry

authors： Poggi A,Catellani S,Fenoglio D,Borsellino G,Battistini L,Zocchi MR

更新日期：2007-01-01 00:00:00

abstract：:Balance between excitatory glutamate and inhibitory GABA neurotransmitter is essential and critical for proper development and functioning of brain. GABAergic (gamma aminobutyric acid) and glutamatergic interneurons maintain excitability, integrity and synaptic plasticity. Several evidences implicated relative loss of...

journal_title：Current medicinal chemistry

authors： Purkayastha P,Malapati A,Yogeeswari P,Sriram D

更新日期：2015-05-04 00:00:00

abstract：:The COVID-19 pandemic has had catastrophic Global effects on financial markets, jobs and peoples' lives. Future prevention/therapy of COVID-19 will rely heavily on vaccine development and attempts to repurpose drugs previously used for other microbial diseases. Little attention, however, has been paid to possible diff...

journal_title：Current medicinal chemistry

authors： Ratcliffe NA,Castro HC,Paixão IC,Mello CB

更新日期：2020-10-27 00:00:00

abstract：:The fibrinolytic system includes a broad spectrum of proteolytic enzymes with physiological and pathophysiological functions in several processes, such as haemostatic balance, tissue remodeling, tumor invasion, angiogenesis and reproduction. The main enzyme of the plasminogen activator system is plasmin, which is resp...

journal_title：Current medicinal chemistry

authors： Zorio E,Gilabert-Estellés J,España F,Ramón LA,Cosín R,Estellés A

更新日期：2008-01-01 00:00:00

abstract：:Glucagon-like peptide-1 (GLP-1) is an insulinotropic hormone secreted from endocrine cells in the gut mucosa in response to meal ingestion. It is an important incretin hormone; mice with a null mutation in the GLP-1 receptor gene develop glucose intolerance. In addition, it inhibits gastrointestinal secretion and moti...

journal_title：Current medicinal chemistry

authors： Holst JJ

更新日期：1999-11-01 00:00:00

abstract：:Transient Receptor Potential Melastatin-related 7 (TRPM7) is a non-selective cation channel fused with a functional kinase domain. Physiologically, TRPM7 channel is involved in magnesium homeostasis, cell survival and gastrulation. The channel part is responsible for calcium, magnesium, and metal trace entries. Cation...

journal_title：Current medicinal chemistry

authors： Gautier M,Perrière M,Monet M,Vanlaeys A,Korichneva I,Dhennin-Duthille I,Ouadid-Ahidouch H

更新日期：2016-01-01 00:00:00

abstract：:Since the outbreak of SARS (severe acute respiratory syndrome) in November 2002 in Southern China's Guangdong Province, considerable progress has been made in the development of drugs for SARS therapy. The present mini review is focused on the area of computer-aided drug discovery, i.e., the advances achieved mainly f...

journal_title：Current medicinal chemistry

authors： Chou KC,Wei DQ,Du QS,Sirois S,Zhong WZ

更新日期：2006-01-01 00:00:00

abstract：:Chagas disease is an infectious tropical disease included within the group of neglected tropical diseases. Though historically endemic to Latin America, it has lately spread to high-income countries due to human migration. At present, there are only two available drugs, nifurtimox and benznidazole, approved for this t...

journal_title：Current medicinal chemistry

authors： Bellera CL,Alberca LN,Sbaraglini ML,Talevi A

更新日期：2020-01-01 00:00:00

abstract：:In modern industrialized societies, people are exposed to thousands of naturally occurring and synthetic chemicals throughout their lifetime. Although certain occupational chemicals are known to be carcinogenic in humans, it has been difficult to definitively determine the adverse health effects of many environmental ...

journal_title：Current medicinal chemistry

authors： Weyandt J,Ellsworth RE,Hooke JA,Shriver CD,Ellsworth DL

更新日期：2008-01-01 00:00:00

abstract：:Human immunodeficiency virus (HIV) infection commonly results in a myriad of comorbid conditions secondary to immune deficiency. Infection also affects broad organ system function. Although current antiretroviral therapy (ART) reduces disease morbidity and mortality through effective control of peripheral viral load, ...

journal_title：Current medicinal chemistry

authors： Edagwa BJ,Zhou T,McMillan JM,Liu XM,Gendelman HE

更新日期：2014-01-01 00:00:00

abstract：:Artificial intelligence methods, in particular, machine learning, has been playing a pivotal role in drug development, from structural design to clinical trial. This approach is harnessing the impact of computer-aided drug discovery thanks to large available data sets for drug candidates and its new and complex manner...

journal_title：Current medicinal chemistry

authors： Musella S,Verna G,Fasano A,Di Micco S

更新日期：2020-11-11 00:00:00

abstract：:Dendritic cells (DCs) are the most powerful antigen-presenting cells which link the innate and adaptive immune responses. Depending on the context DCs initiate the immune responses or contribute to immune tolerance. Any disturbance in their phenotypes and functions may initiate inflammatory or autoimmune diseases. Hen...

journal_title：Current medicinal chemistry

authors： Rahimi K,Hassanzadeh K,Khanbabaei H,Haftcheshmeh SM,Ahmadi A,Izadpanah E,Mohammadi A,Sahebkar A

更新日期：2020-05-14 00:00:00

abstract：:Poisoning of DNA topoisomerase I is the mechanism by which camptothecins interfere with tumor growth. Although the clinical use of camptothecins has had a significant impact on cancer therapy, de novo or acquired clinical resistance to these drugs is common. Clinical resistance to camptothecins is still a poorly under...

journal_title：Current medicinal chemistry

authors： Beretta GL,Gatti L,Perego P,Zaffaroni N

更新日期：2013-01-01 00:00:00

abstract：:A growing body of evidence has shown that oxidative stress may be involved in the development of vascular complications associated with diabetes. However, the molecular mechanism for increased reactive oxygen species (ROS) production in diabetes remains uncertain. Among various possible mechanisms, attention have incr...

journal_title：Current medicinal chemistry

authors： Inoguchi T,Tsubouchi H,Etoh T,Kakimoto M,Sonta T,Utsumi H,Sumimoto H,Yu HY,Sonoda N,Inuo M,Sato N,Sekiguchi N,Kobayashi K,Nawata H

更新日期：2003-09-01 00:00:00

abstract：:To date, many scientific attempts have been directed towards the development of experimental models for the identification of neuronal mechanisms evoking cardiovascular and hemodynamic dysfunctions. The spontaneously hypertensive rat (SHR), a genetic model of essential hypertension, has become a valuable rodent for th...

journal_title：Current medicinal chemistry

authors： Giusi G,Alò R,Avolio E,Zizza M,Facciolo RM,Talani G,Biggio G,Sanna E,Canonaco M

更新日期：2012-01-01 00:00:00

abstract：:In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a ...

journal_title：Current medicinal chemistry

authors： Bergese P,Cretich M,Oldani C,Oliviero G,Di Carlo G,Depero LE,Chiari M

更新日期：2008-01-01 00:00:00

abstract：:Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...

journal_title：Current medicinal chemistry

authors： Bedin C,Crotti S,Tasciotti E,Agostini M

更新日期：2018-01-01 00:00:00

abstract：: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 leu...

journal_title：Current medicinal chemistry

authors： Di Santo R,Maga G

更新日期：2006-01-01 00:00:00

abstract：:Ten years elapsed since the discovery by Sanofi of SR141716A the first selective CB(1) cannabinoid receptor antagonist. Shortly after, Sanofi also reported the synthesis of the first selective CB(2) cannabinoid receptor antagonist, SR144528. Since these two milestones in the cannabinoid field, many other compounds, mo...

journal_title：Current medicinal chemistry

authors： Muccioli GG,Lambert DM

更新日期：2005-01-01 00:00:00

abstract：:Natural products from symbiotic or commensal associations between marine invertebrate and microbial organisms show exceptional promise as pharmaceuticals in many therapeutic areas. An economic and sustainable global market supply due to difficulty of synthesis is cited as the main obstacle for exploitation of these ot...

journal_title：Current medicinal chemistry

authors： Dunlap WC,Jaspars M,Hranueli D,Battershill CN,Perić-Concha N,Zucko J,Wright SH,Long PF

更新日期：2006-01-01 00:00:00

abstract：:Trypanosomatids are a group of flagellated unicellular eukaryotes, causing serious human diseases including Chagas disease (Trypanosoma cruzi), sleeping sickness (Trypanosoma brucei spp.) and Leishmaniasis (Leishmania spp.). The second messenger cAMP is involved in numerous and fundamental processes in these parasites...

journal_title：Current medicinal chemistry

authors： Schoijet AC,Sternlieb T,Alonso GD

更新日期：2019-01-01 00:00:00

abstract：:Apoptosis or programmed cell death is a cellular mechanism used to regulate cell number and eliminate damaged or mutated cells. Many chemotherapeutic agents and ionizing radiation induce not only apoptotic signaling pathways, but also survival responses such as DNA damage responses and cell cycle arrest, which allow f...

journal_title：Current medicinal chemistry

authors： Sharma V,Hupp CD,Tepe JJ

更新日期：2007-01-01 00:00:00

abstract：:Bicarbonate (HCO₃⁻) membrane transport systems are crucial players in the physiology of several tissues. The molecular basis of HCO₃⁻ membrane transport is of major physiological relevance since this ion is involved in the establishment of intracellular and extracellular ionic composition, osmolariy and pH. The membra...

journal_title：Current medicinal chemistry

authors： Bernardino RL,Jesus TT,Martins AD,Sousa M,Barros A,Cavaco JE,Socorro S,Alves MG,Oliveira PF

更新日期：2013-01-01 00:00:00

abstract：:For more than 20 years there has been increasing interest in the development of novel therapies to raise levels of high-density lipoprotein cholesterol (HDL-C). However, well publicized failures of recent clinical trials of agents that raise HDL-C levels have stimulated considerable controversy with regard to the pote...

journal_title：Current medicinal chemistry

authors： Duong M,Nicholls SJ

更新日期：2014-01-01 00:00:00

abstract：:Many of the currently available treatments for obsessive-compulsive and related disorders (OCRDs) such as pharmacotherapy augmentation strategies, partial hospitalization programs, deep brain stimulation, and neurosurgery are efficacious for individuals suffering from more severe forms of these conditions. Unfortunate...

journal_title：Current medicinal chemistry

authors： Fontenelle LF,Zeni-Graiff M,Quintas JN,Yücel M

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Histone deacetylases (HDAC) are an important class of enzymes that play a pivotal role in epigenetic regulation of gene expression that modifies the terminal of core histones leading to remodelling of chromatin topology and thereby controlling gene expression. HDAC inhibitors (HDACi) counter this action and ...

journal_title：Current medicinal chemistry

authors： Sultana F,Manasa KL,Shaik SP,Bonam SR,Kamal A

更新日期：2019-01-01 00:00:00