Essentiality, toxicology and chelation therapy of zinc and copper.

abstract：:Raltegravir, the only drug targeting the integration step in HIV-1 life cycle, makes β-ketoenol integrase (IN) strand transfer inhibitor (STI) gain a definitive place in the treatment of HIV-1 infection. However, the emergence of viral strains resistant to β-ketoenol STI demands a continued effort toward the discovery...

journal_title：Current medicinal chemistry

authors： Yu S,Zhao G

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a growing health problem. AD is currently treated by symptomatic drugs, the acetylcholinesterase inhibitors, based on the...

journal_title：Current medicinal chemistry

authors： Francotte P,Graindorge E,Boverie S,de Tullio P,Pirotte B

更新日期：2004-07-01 00:00:00

abstract：:Frontotemporal Lobar Degeneration (FTLD) is characterized by behavioral changes, executive dysfunctions, and language impairment, sustained by different neuropathological patterns. The collective efforts of clinical, pathological and genetic studies have recently opened new insights into the underpinnings of pathologi...

journal_title：Current medicinal chemistry

authors： Bigni B,Premi E,Pilotto A,Padovani A,Borroni B

更新日期：2012-01-01 00:00:00

abstract：:Antisynthetase syndrome is a group of closely related rare diseases which clinically manifest with inflammatory myopathies, interstitial lung disease, inflammatory arthritis, skin hyperkeratosis (mechanic’s hands) and Raynaud phenomenon. The pathophysiology of antisynthetase syndrome is not entirely understood, but ge...

journal_title：Current medicinal chemistry

authors： Mirrakhimov AE

更新日期：2015-05-13 00:00:00

abstract：:Cardiotrophin-1 (CT-1), a member of the interleukin (IL)-6 family, is reported to exhibit a plethora of pleiotropic effects in the heart such as cytoprotective, pro-proliferative and pro-fibrotic ones. An extensive research has been devoted on proliferative and profibrotic effects of CT-1 on the heart. Thus the presen...

journal_title：Current medicinal chemistry

authors： García-Cenador MB,Lopez-Novoa JM,Díez J,García-Criado FJ

更新日期：2013-01-01 00:00:00

abstract：:Mast cells are potent effectors playing a key role in IgE-associated hypersensitivity reactions, allergic disorders, inflammation and protective immune responses. Mast cell development in vivo occurs mainly in non-hematopoietic microenvironments and increased mast cell numbers can be seen in various inflammatory disea...

journal_title：Current medicinal chemistry

authors： Hu ZQ,Zhao WH,Shimamura T

更新日期：2007-01-01 00:00:00

abstract：:Fulvestrant is a novel endocrine therapy for breast cancer, with a unique structure and mode of action. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant has reached the clinic via extensive pre-clinical and clinic...

journal_title：Current medicinal chemistry

authors： Johnston SJ,Cheung KL

更新日期：2010-01-01 00:00:00

abstract：:Atrial fibrillation represents a major clinical, social and economical matter, and its importance is expected to increase even more in the near future. The progressive ageing of population is associated with an inevitable rising in incidence and prevalence of this rhythm disorder, which limits functional capability, f...

journal_title：Current medicinal chemistry

authors： Lombardi F,Terranova P

更新日期：2006-01-01 00:00:00

abstract：:Schizophrenia is a chronic psychiatric disorder that affects about 1 in 100 people around the world and results in persistent emotional and cognitive impairments. Untreated schizophrenia leads to deterioration in quality of life and premature death. Although the clinical efficacy of dopamine D2 receptor antagonists ag...

journal_title：Current medicinal chemistry

authors： Jankowska A,Satała G,Partyka A,Wesołowska A,Bojarski AJ,Pawłowski M,Chłoń-Rzepa G

更新日期：2019-01-01 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：:Plant foods are not only a main source of nutrients, but they are also rich in physiologically bioactive bionutrients or phytochemicals. Consumption of fruit and vegetables is associated with a decreased risk of pathological status, including cancer. Reactive oxygen species play a key role in the genesis and developme...

journal_title：Current medicinal chemistry

authors： Matés JM,Segura JA,Alonso FJ,Márquez J

更新日期：2011-01-01 00:00:00

abstract：:Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This mini...

journal_title：Current medicinal chemistry

authors： Fabbrizzi P,Menchi G,Guarna A,Trabocchi A

更新日期：2014-01-01 00:00:00

abstract：:The Src family consists of eight non-receptor protein tyrosine kinases characterised by a common structure. Based on their amino acid sequence, Src family kinases are grouped into two subfamilies, which are also characterised by different tissue specificity. Src kinases are involved in signal transduction pathways tri...

journal_title：Current medicinal chemistry

authors： Benati D,Baldari CT

更新日期：2008-01-01 00:00:00

abstract：:Osteoporosis is a pathological loss of bone mass due to an imbalance in bone remodeling where osteoclast-mediated bone resorption exceeds osteoblast-mediated bone formation resulting in skeletal fragility and fractures. Anti-resorptive agents such as bisphosphonates and SERMs, and anabolic drugs that stimulate bone fo...

journal_title：Current medicinal chemistry

authors： Li H,Xiao Z,Quarles LD,Li W

更新日期：2020-03-30 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：:The transport mechanisms of ascorbic acid (AA) are described. The metabolism of AA and its function as an antioxidant are covered in some detail. Subsequently, indications for postoperative substitution are discussed. The supplementation of up to 300 mg of AA per day in postoperative intensive care unit patients durin...

journal_title：Current medicinal chemistry

authors： Rümelin A

更新日期：2009-01-01 00:00:00

abstract：:Virtual screening is an important means for lead compound discovery. The scoring function is the key to selecting hit compounds. Many scoring functions are currently available; however, there are no all-purpose scoring functions because different scoring functions tend to have conflicting results. Recently, neural net...

journal_title：Current medicinal chemistry

authors： Shan W,Li X,Yao H,Lin K

更新日期：2020-05-26 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：BACKGROUND:The sterile alpha motif (Sam) domain is a small helical protein module, able to undergo homo- and hetero-oligomerization, as well as polymerization, thus forming different types of protein architectures. A few Sam domains are involved in pathological processes and consequently, they represent valuable target...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Mercurio FA,Leone M

更新日期：2020-01-01 00:00:00

abstract：:Marine organisms are abundant sources of bioactive natural products. Among metabolites produced by sponges and their associated microbial communities, halogenated natural compounds accounted for an important part due to their potent biological activities. The present review updates and compiles a total of 258 halogena...

journal_title：Current medicinal chemistry

authors： Li C,Shi D

更新日期：2020-01-01 00:00:00

abstract：:Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as inc...

journal_title：Current medicinal chemistry

authors： Chen X,Hussain S,Parveen S,Zhang S,Yang Y,Zhu C

更新日期：2012-01-01 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：:Epigenetics is a field of biological sciences focused on the study of reversible, heritable changes in gene function not due to modifications of the genomic sequence. These changes are the result of a complex cross-talk between several molecular mechanisms, that is in turn orchestrated by genetic and environmental fac...

journal_title：Current medicinal chemistry

authors： De Riso G,Cocozza S

更新日期：2020-11-17 00:00:00

abstract：:Protein-ligand docking is currently an important tool in drug discovery efforts and an active area of research that has been the subject of important developments over the last decade. These are well portrayed in the rising number of available protein-ligand docking software programs, increasing level of sophisticatio...

journal_title：Current medicinal chemistry

authors： Sousa SF,Ribeiro AJ,Coimbra JT,Neves RP,Martins SA,Moorthy NS,Fernandes PA,Ramos MJ

更新日期：2013-01-01 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：: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：:Perceiving a pharmacophore is the first essential step towards understanding the interaction between a receptor and a ligand. Once a pharmacophore is established, a beneficial use of it is 3D database searching to retrieve novel compounds that would match the pharmacophore, without necessarily duplicating the topologi...

journal_title：Current medicinal chemistry

authors： Kurogi Y,Güner OF

更新日期：2001-07-01 00:00:00

abstract：:Phosphonated nucleosides represent a promising alternative in the improvement of the biological activity of nucleoside analogues in antiviral and anticancer chemotherapy. The basic concept, the chemistry, the different structural modifications and their effects on the antiviral potency will be discussed in this review...

journal_title：Current medicinal chemistry

authors： Piperno A,Chiacchio MA,Iannazzo D,Romeo R

更新日期：2006-01-01 00:00:00

abstract：:Homocysteine is a thiol aminoacid synthesized during the metabolism of methionine. Increased plasma levels of homocysteine can be the result of mutations in the enzymes responsible for homocysteine metabolism, particularly cystathionine-beta synthase (CBS) and 5,10-methylenetetrahydrofolate reductase (MTHFR). Addition...

journal_title：Current medicinal chemistry

authors： Pezzini A,Del Zotto E,Padovani A

更新日期：2007-01-01 00:00:00