CuAAC click chemistry accelerates the discovery of novel chemical scaffolds as promising protein tyrosine phosphatases inhibitors.

abstract：:Hypoxia in tumor cells is characterized by a lack of oxygen resulting from reduced blood supply to the surrounding tissue, and is a common characteristic of solid tumors as a consequence of rapid cell growth. Hypoxia in tumors is a predictor of both resistance to chemotherapy and of a metastatic/aggressive form of can...

journal_title：Current medicinal chemistry

authors： Liang D,Miller GH,Tranmer GK

更新日期：2015-01-01 00:00:00

abstract：:Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed almost 30 years ago, have crucial relevance for drug design. Indeed, formation of GPCR oligomers may affect the diversity and performance by which extracellular signals are transferred to G proteins in the process of receptor transductio...

journal_title：Current medicinal chemistry

authors： Kaczor AA,Selent J

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Smac mimetics (also known as IAP antagonist) are a new class of targeted drugs having a goal to suppress the IAPs, reestablishing the apoptotic pathways and inducing cancer cell death. Therefore, development of Smac mimetics was considered an attractive strategy for the development of new anticancer drugs. L...

journal_title：Current medicinal chemistry

authors： Ali R,Singh S,Haq W

更新日期：2018-01-01 00:00:00

abstract：:Dipeptidyl peptidase 4 (DPP-4), a substrate-specific serine protease, has been validated as a promising drug target for the treatment of type 2 diabetes. DPP-4 inhibitors significantly lowered blood glucose levels in patients with type 2 diabetes without common body weight gain, hypoglycemia and gastrointestinal distu...

journal_title：Current medicinal chemistry

authors： Liu Y,Hu Y,Liu T

更新日期：2012-01-01 00:00:00

abstract：:Angiotensin converting enzyme (ACE) 2 is a homologue of ACE that catalyzes the conversion of Angiotensin (Ang) II into Ang1-7, which induces vasodilation, anti-fibrotic, anti-proliferative and anti-inflammatory effects. Given that ACE2 counterbalances the effects of Ang II, it has been proposed as a biomarker in kidne...

journal_title：Current medicinal chemistry

authors： Anguiano L,Riera M,Pascual J,Soler MJ

更新日期：2017-01-01 00:00:00

abstract：:Recent advances have identified the podocyte as a key target in glomerular injury. The podocyte is a highly specialized cell which is responsible for the glomerular permselectivity for proteins in the kidney. Podocyte injury or loss leads to proteinuria. Apoptosis has been shown to contribute to renal cell loss, inclu...

journal_title：Current medicinal chemistry

authors： Moreno JA,Sanchez-Niño MD,Sanz AB,Lassila M,Holthofer H,Blanco-Colio LM,Egido J,Ruiz-Ortega M,Ortiz A

更新日期：2008-01-01 00:00:00

abstract：:Osteogenic peptides are, or have potential to be, therapies for the treatment of osteoporosis, fracture repair, and repair of loosened bone implants. Human parathyroid hormone has been approved for the treatment of post-menopausal osteoporosis. Constrained analogs of PTH and the parathyroid-hormone related peptide (PT...

journal_title：Current medicinal chemistry

authors： Willick GE,Morley P,Whitfield JF

更新日期：2004-11-01 00:00:00

abstract：:The discovery of the high-affinity, high-specificity folate receptor in mamalian kidney cells, coupled with the ability of folate to enter cells by folate receptor-mediated endocytosis and the subsequent elucidation of the folate receptor's overexpression in specific cancer cell types; heralded the arrival of the area...

journal_title：Current medicinal chemistry

authors： Carron PM,Crowley A,O'Shea D,McCann M,Howe O,Hunt M,Devereux M

更新日期：2018-01-01 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：:Diabetes mellitus (DM) is characterized by hyperglycemia, resulting from defects in insulin secretion, insulin action or both. There are several factors such as hyperlipidemia and oxidative stress (OS), namely the production of reactive oxygen/nitrogen species (ROS/RNS), that actively contribute to the development and...

journal_title：Current medicinal chemistry

authors： Sousa A,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-05-24 00:00:00

abstract：:Matrix metalloproteinase-9 (MMP-9) plays an important role in the onset and prognosis of myocardial infarction. Targets of angiotensin converting enzyme (ACE) inhibitors might include not only ACE but also MMP-9, and ACE seems to be closely associated with complications of hypertension such as cardiovascular remodelin...

journal_title：Current medicinal chemistry

authors： Yamamoto D,Takai S

更新日期：2009-01-01 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：:In order to ascertain the role of dietary flavonoids as antioxidants in vivo it is necessary to understand the chemical nature of the absorbed forms in the circulation in vivo and how the multiplicity of research findings in vitro reflect the bioactivity of flavonoids in vivo. Only when we gain adequate information on...

journal_title：Current medicinal chemistry

authors： Rice-Evans C

更新日期：2001-06-01 00:00:00

abstract：BACKGROUND:With global increase in elderly population, modern societies must find strategies to reduce the consequences of aging process; thereby decreasing the incidence of age-related neurodegenerative diseases. Oxidative stress and recently inflammation, have been pointed out as the leading causes of brain aging. Th...

journal_title：Current medicinal chemistry

authors： Sarubbo F,Moranta D,Asensio VJ,Miralles A,Esteban S

更新日期：2017-01-01 00:00:00

abstract：:Protein Kinase Inhibitors (PKIs) and Histone Deacetylase Inhibitors (HDACIs) are two important classes of anticancer agents and have provided a variety of small molecule drugs for the treatment of various types of human cancers. However, malignant tumors are of a multifactorial nature that can hardly be "cured" by tar...

journal_title：Current medicinal chemistry

authors： Ling Y,Liu J,Qian J,Meng C,Guo J,Gao W,Xiong B,Ling C,Zhang Y

更新日期：2020-01-01 00:00:00

abstract：:The term Lewy body diseases (LBDs) refers to a subset of neurodegenerative disorders that share the accumulation of the so-called Lewy bodies (LB) including: Parkinson's disease (PD), dementia with Lewy bodies (DLB), and PD later characterized by the occurrence of dementia (PDD). Moreover, multiple system atrophy (MSA...

journal_title：Current medicinal chemistry

authors： Bauckneht M,Arnaldi D,Nobili F,Aarsland D,Morbelli S

更新日期：2018-01-01 00:00:00

abstract：:Cervical spondylotic myelopathy (CSM) is a very common and debilitating disease; however, its underlying pathocellular process remains uncertain. Attempts have been made to reproduce CSM in experimental animal models in order to deepen the knowledge on the molecular pathobiology of this disease. The up-to-date observa...

journal_title：Current medicinal chemistry

authors： Karadimas SK,Gialeli CH,Klironomos G,Tzanakakis GN,Panagiotopoulos E,Karamanos NK,Gatzounis G

更新日期：2010-01-01 00:00:00

abstract：:Universal stress proteins are ubiquitously expressed in bacteria, archaea and plants and other eukaryotes. A general property of USPs is their role in adaptation of bacteria to oxidative stress, high temperature, low pH and/or hypoxia. There is increasing evidence that these proteins facilitate the adaption of bacteri...

journal_title：Current medicinal chemistry

authors： O'Connor A,McClean S

更新日期：2017-11-24 00:00:00

abstract：:High-resolution nuclear magnetic resonance (NMR) spectroscopy is a universal analytical tool. It can provide detailed information on chemical shifts, J coupling constants, multiplet patterns, and relative peak areas. It plays an important role in the fields of chemistry, biology, medicine, and pharmacy. A highly homog...

journal_title：Current medicinal chemistry

authors： Lin Y,Zeng Q,Lin L,Chen Z

更新日期：2019-01-01 00:00:00

abstract：:Endothelial cells (ECs) play a pivotal role in physiological and altered tissue neovascularization. They face multiple morphological, biochemical and functional changes during the different phases of angiogenesis, under the regulation of a great number of proangiogenic and antiangiogenic signals, including soluble and...

journal_title：Current medicinal chemistry

authors： Munaron L,Fiorio Pla A

更新日期：2009-01-01 00:00:00

abstract：:The present article reviews interesting cationic liposomes (cationic transfection lipids) with novel cationic cholesterol derivatives, a new strategy in gene transfection developed by our group and the presently accepted molecular mechanism of gene transfection. Use of confocal laser scanning microscopy and atomic for...

journal_title：Current medicinal chemistry

authors： Nakanishi M

更新日期：2003-07-01 00:00:00

abstract：:Now cisplatin and its analogs are some of the most effective chemotherapeutic agents in clinical use as the first line of treatment in testicular and ovarian cancers. Unfortunately, they have several major drawbacks, such as cumulative toxicities of nephrotoxicity and ototoxicity, inherent or treatment-induced resista...

journal_title：Current medicinal chemistry

authors： Zhang J,Zhang F,Li H,Liu C,Xia J,Ma L,Chu W,Zhang Z,Chen C,Li S,Wang S

更新日期：2012-01-01 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：:Limitations associated with the production cost, metabolic instability, side-effects, resistance and poor pharmacokinetics of organic protease inhibitors (PIs), which form an essential component of the front line HAART treatment for HIV, have fuelled efforts into finding novel, transition metal-based alternatives. Som...

journal_title：Current medicinal chemistry

authors： Kellett A,Prisecaru A,Slator C,Molphy Z,McCann M

更新日期：2013-01-01 00:00:00

abstract：:Although the assortment of antifungal drugs is broad, the most commonly used agents have major drawbacks. Toxicity, serious side effects or the emergence of drug resistance are amongst them. New drugs and drug candidates under clinical trials do not guarantee better pharmacological parameters. These new medicines may ...

journal_title：Current medicinal chemistry

authors： Musiol R,Serda M,Hensel-Bielowka S,Polanski J

更新日期：2010-01-01 00:00:00

abstract：:The hemostatic system comprises platelet aggregation, coagulation and fibrinolysis also termed primary, secondary and tertiary hemostasis. From the platelet transcriptome 6000 mRNA species and represent receptors, ion channels, signalling molecules, kinases, phosphatases, and structural, metabolic and regulatory prote...

journal_title：Current medicinal chemistry

authors： Stassen JM,Arnout J,Deckmyn H

更新日期：2004-09-01 00:00:00

abstract：:The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to prov...

journal_title：Current medicinal chemistry

authors： Matute MS,Matute R,Merino P

更新日期：2016-01-01 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

abstract：:Alzheimer's disease (AD) is a highly complex and rapidly progressive neurodegenerative disorder characterized by the systemic collapse of cognitive function and formation of dense amyloid plaques and neurofibrillary tangles. AD pathology is derived from the cholinergic, amyloid and tau hypotheses, respectively. Curren...

journal_title：Current medicinal chemistry

authors： Mohamed T,Rao PP

更新日期：2011-01-01 00:00:00

abstract：:Several lines of defense maintain the surface integrity of the delicate airway epithelium which is regularly subjected to severe trauma. These defense mechanisms include protection by the mucus layer, rapid repair by restitution (cell migration) and regeneration via proliferation and differentiation. Luminal surveilla...

journal_title：Current medicinal chemistry

authors： Hoffmann W

更新日期：2007-01-01 00:00:00