The role of genomics in antibacterial target discovery.

abstract：:Glutamate carboxypeptidase II (GCPII) is a membrane-bound binuclear zinc metallopeptidase with the highest expression levels found in the nervous and prostatic tissue. Throughout the nervous system, glia-bound GCPII is intimately involved in the neuron-neuron and neuron-glia signaling via the hydrolysis of N-acetylasp...

journal_title：Current medicinal chemistry

authors： Bařinka C,Rojas C,Slusher B,Pomper M

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Excessive norepinephrine (NE) release in the ischemic heart elicits severe and often lethal arrhythmias. Resident cardiac mast cells synthesize and store active renin, which is released upon degranulation, causing the activation of a local cardiac renin-angiotensin system (RAS) responsible for NE release and...

journal_title：Current medicinal chemistry

authors： Marino A,Levi R

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Resveratrol, a natural polyphenol product, is used in plant defense from fungal and microbial aggression. It is found naturally, especially in plants such as grapes, peanuts, and berries. It has the highest concentrations in blueberries, mulberries, blackberries, and the skin of red grapes. Resveratrol has v...

journal_title：Current medicinal chemistry

authors： Kumar S,Chang YC,Lai KH,Hwang TL

更新日期：2020-09-17 00:00:00

abstract：:Drug resistance is one of the major obstacles limiting the success of cancer chemotherapy. Biological mechanisms contributing to drug resistance may be present de novo and related to inherent features or may be raised after exposure to anticancer drugs. In recent years, both clinical observations and experimental stud...

journal_title：Current medicinal chemistry

authors： Sui M,Zhang H,Fan W

更新日期：2011-01-01 00:00:00

abstract：:Pyoverdine is the generic name given to a vast family of fluorescent green-yellowish pigments produced by Pseudomonas species. Pseudomonas aeruginosa is an opportunistic pathogen, particularly infecting humans with compromised natural defenses. These infections result in significantly higher morbidity, longer hospital...

journal_title：Current medicinal chemistry

authors： Cézard C,Farvacques N,Sonnet P

更新日期：2015-01-01 00:00:00

abstract：:Nowadays, enzymatic therapy is a very promising line of treatment for many different diseases. There is a group of disorders and conditions, caused by fibrotic and scar processes and associated with the excessive accumulation of collagen that needs to be catabolized to normalize the connective tissue content. The huma...

journal_title：Current medicinal chemistry

authors： Shekhter AB,Balakireva AV,Kuznetsova NV,Vukolova MN,Litvitsky PF,Zamyatnin AA Jr

更新日期：2019-01-01 00:00:00

abstract：:Current strategies in pharmaceutical research comprise two methodologically different but complementary approaches for lead finding purposes, namely the random screening of compound libraries and the structure-based effort, commonly termed rational drug design. The structure-based approach is aimed to exploit 3D struc...

journal_title：Current medicinal chemistry

authors： Müller G

更新日期：2000-09-01 00:00:00

abstract：:Fourier-transform infrared (FT-IR) based mapping and imaging is a fast emerging technology which is being increasingly applied to investigate tissues in the high-throughput mode. The high resolution close to the cellular level, the possibility to determine the bio-distribution of molecules of interest (proteins, pepti...

journal_title：Current medicinal chemistry

authors： Petter CH,Heigl N,Rainer M,Bakry R,Pallua J,Bonn GK,Huck CW

更新日期：2009-01-01 00:00:00

abstract：:In their structural multiplicity and in the extent to which they occur in nature the derivatives of benzofuran are significantly lesser than the isoelectronic analogue indoles. However, these heterocyclic compounds show a variety of pharmacological properties, and change of their structure offers a high degree of dive...

journal_title：Current medicinal chemistry

authors： De Luca L,Nieddu G,Porcheddu A,Giacomelli G

更新日期：2009-01-01 00:00:00

abstract：:Nowadays, the use of synthetic carriers as biochemical reagents and immunogens is entering a new phase. The multimeric nature of these constructs, the unambiguous composition and the ease, reliability and versatility of their production, make this type of carriers well-suited to various biotechnological and biochemica...

journal_title：Current medicinal chemistry

authors： Alexopoulos Ch,Sakarellos-Daitsiotis M,Sakarellos C

更新日期：2005-01-01 00:00:00

abstract：:We apply noval techniques, the Scaling Index Method (SIM), which reveals local topology of the structure, and the Minkowski Functionals (MF), which provide four global topological characteristics, to assess strength of the trabecular network of the human bone. We compare capabilities of these methods with the standard...

journal_title：Current medicinal chemistry

authors： Sidorenko I,Monetti R,Bauer J,Mueller D,Rummeny E,Eckstein F,Matsuura M,Lochmueller EM,Zysset P,Raeth C

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Since the serendipitous discovery of the antitumor activity of cisplatin there has been a continuous surge in studies aimed at the development of new cytotoxic metal complexes. While the majority of these complexes have been designed to interact with nuclear DNA, other targets for anticancer metallodrugs att...

journal_title：Current medicinal chemistry

authors： Erxleben A

更新日期：2019-01-01 00:00:00

abstract：:More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...

journal_title：Current medicinal chemistry

authors： Kidwai M,Sapra P,Bhushan KR

更新日期：1999-03-01 00:00:00

abstract：:Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...

journal_title：Current medicinal chemistry

authors： Pirozzi F,Ren K,Murabito A,Ghigo A

更新日期：2019-01-01 00:00:00

abstract：:Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...

journal_title：Current medicinal chemistry

authors： Casas A,Di Venosa G,Hasan T,Al Batlle

更新日期：2011-01-01 00:00:00

abstract：:Physalia physalis is a marine cnidarian from which high molecular weight toxins with hemolytic and neurotoxic effects have been isolated. In the present work, two novel toxins, PpV9.4 and PpV19.3 were purified from P. physalis by bioactive guideline isolation. It involved two steps of column chromatography, gel filtra...

journal_title：Current medicinal chemistry

authors： Diaz-Garcia CM,Fuentes-Silva D,Sanchez-Soto C,Domínguez-Pérez D,García-Delgado N,Varela C,Mendoza-Hernández G,Rodriguez-Romero A,Castaneda O,Hiriart M

更新日期：2012-01-01 00:00:00

abstract：:Since its discovery in 1995 adiponectin has garnered considerable interest from the academic, clinical and biotech communities due to its proposed salutary anti-inflammatory, anti-diabetic, anti-atherogenic and cardioprotective properties. As a result our appreciation of adiponectin's structure and the importance of p...

journal_title：Current medicinal chemistry

authors： Hickman IJ,Whitehead JP

更新日期：2012-01-01 00:00:00

abstract：:Demyelination occurs in several central nervous system (CNS) disorders, including multiple sclerosis, viral infection and spinal cord injury and can result in severe functional impairment. Therefore there is great interest in developing therapies promoting repair in CNS demyelinating diseases and trauma. Cell replacem...

journal_title：Current medicinal chemistry

authors： Lavdas AA,Papastefanaki F,Thomaidou D,Matsas R

更新日期：2008-01-01 00:00:00

abstract：:For many years the spotlight in drug discovery has been on a relatively small number of validated therapeutic target classes, such as G-protein coupled receptors and enzymes such as protein kinases, with well characterized enzymatic and cellular activities. However, with recent progress in genomics and proteomics, pro...

journal_title：Current medicinal chemistry

authors： De Giorgi M,Voisin-Chiret AS,Rault S

更新日期：2013-01-01 00:00:00

abstract：:Protein C is a vitamin K-dependent anticoagulant serine protease zymogen in plasma which upon activation by the thrombin-thrombomodulin complex down-regulates the coagulation cascade by degrading cofactors Va and VIIIa by limited proteolysis. In addition to its anticoagulant function, activated protein C (APC) also bi...

journal_title：Current medicinal chemistry

authors： Rezaie AR

更新日期：2010-01-01 00:00:00

abstract：:Antimicrobial resistance is an ever-increasing problem throughout the world and has already reached severe proportions. Two very common neglected tropical diseases are Chagas' disease and leishmaniasis. Chagas' disease is a severe health problem, mainly in Latin America, causing approximately 50000 deaths a year and m...

journal_title：Current medicinal chemistry

authors： Bandyopadhyay D,Samano S,Villalobos-Rocha JC,Sanchez-Torres LE,Nogueda-Torres B,Rivera G,Banik BK

更新日期：2017-01-01 00:00:00

abstract：:Complement plays a vital role in our innate immune defense against invasive microorganisms. Excessive complement activation or insufficient control of activation on host cells, however, is associated with several chronic disorders. Essential to the activation and amplification of the Alternative Pathway (AP) of comple...

journal_title：Current medicinal chemistry

authors： Wiles JA,Galvan MD,Podos SD,Geffner M,Huang M

更新日期：2020-01-01 00:00:00

abstract：:Hydrogen sulfide (H2S), previously known only as a toxic agent, in the last decades has been recognized as an important endogenous gasotransmitter, playing a key role in the homeostasis of the cardiovascular system. In the last years, the growing evidence about a protective role exhibited by H2S against myocardial isc...

journal_title：Current medicinal chemistry

authors： Citi V,Piragine E,Testai L,Breschi MC,Calderone V,Martelli A

更新日期：2018-01-01 00:00:00

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...

journal_title：Current medicinal chemistry

authors： López-Rodríguez ML,Ayala D,Benhamú B,Morcillo MJ,Viso A

更新日期：2002-02-01 00:00:00

abstract：:Nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) belong to the protein family of neurotrophins. They both display profound neuromodulatory functions and are essentially involved in the survival and homeostatic maintenance of central and peripheral neurons during development and adulthood. Moreove...

journal_title：Current medicinal chemistry

authors： Schulte-Herbrüggen O,Braun A,Rochlitzer S,Jockers-Scherübl MC,Hellweg R

更新日期：2007-01-01 00:00:00

abstract：:Traditional opioids, mainly alkaloids, have been used in the clinical management of pain for a number of years but are often associated with numerous side-effects including sedation, dizziness, physical dependence, tolerance, addiction, nausea, vomiting, constipation and respiratory depression which prevent their effe...

journal_title：Current medicinal chemistry

authors： Garg S,Nurgali K,Mishra VK

更新日期：2016-01-01 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 discovery of anandamide as an endogenous ligand for the cannabinoid receptors has led to a resurgence of interest in the fatty acid amides. However, N-palmitoylethanolamine (PEA), a shorter and fully saturated analogue of anandamide, has been known since the fifties. This endogenous compound is a member of the N-a...

journal_title：Current medicinal chemistry

authors： Lambert DM,Vandevoorde S,Jonsson KO,Fowler CJ

更新日期：2002-03-01 00:00:00

abstract：:Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in Diabetes Mellitus (DM) and contributes to the develo...

journal_title：Current medicinal chemistry

authors： Tentolouris A,Eleftheriadou I,Tzeravini E,Tsilingiris D,Paschou SA,Siasos G,Tentolouris N

更新日期：2020-01-01 00:00:00

abstract：:Amyotrophic Lateral Sclerosis (ALS) is a fatal neurodegenerative disease characterized by progressive degeneration of motor neurons which brings to muscular atrophy, paralysis and death in 3-5 years from starting symptoms. In about 10% of cases ALS is familiar and in a relevant percent of these cases, mutations of the...

journal_title：Current medicinal chemistry

authors： Contestabile A

更新日期：2011-01-01 00:00:00