Clinical application of ropivacaine for the upper extremity.

abstract：:The H(3) histamine receptor is expressed in many brain regions, including those involved in sleep/wake regulation and cognitive functions. Inhibition of the H(3) receptor leads to increased release of multiple neurotransmitters in these regions, making this receptor an ideal target for the potential enhancement of aro...

journal_title：Current topics in medicinal chemistry

authors： Raddatz R,Tao M,Hudkins RL

更新日期：2010-01-01 00:00:00

abstract：:Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters s...

journal_title：Current topics in medicinal chemistry

authors： Colabufo NA,Berardi F,Contino M,Niso M,Perrone R

更新日期：2009-01-01 00:00:00

abstract：:The genetics of Alzheimer's disease (AD) implies that restoring non-pathological levels or ratios of different amyloid-beta (Abeta) peptide species in the brain could prevent the onset or delay the progression of this neurodegenerative disease. In particular, a selective reduction of the longer Abeta(1-42) peptide whi...

journal_title：Current topics in medicinal chemistry

authors： Beher D

更新日期：2008-01-01 00:00:00

abstract：:Parkinson's disease is a motor dysfunction that has been widely studied but many of the reports on commercial drugs for the treatment of this disease have afforded some undesirable side effects that generate an extensive and unviable treatment by economic costs and due to the bioavailability of the assayed compounds. ...

journal_title：Current topics in medicinal chemistry

authors： Fazel Nabavi S,Uriarte E,Rastrelli L,Modak B,Sobarzo-Sánchez E

更新日期：2016-01-01 00:00:00

abstract：:In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard t...

journal_title：Current topics in medicinal chemistry

authors： Johnson L,Goping IS,Rieger A,Mane JY,Huzil T,Banerjee A,Luduena R,Hassani B,Winter P,Tuszynski JA

更新日期：2017-01-01 00:00:00

abstract：:The first-ever World Chagas Disease Day, celebrated in April 14, 2020, is a key initiative to raise awareness of the impact of this neglected tropical disease (NTD). This landmark comes along with the first World NTD Day and the new WHO Road Map on NTDs for 2021-2030. ...

journal_title：Current topics in medicinal chemistry

authors： Ferreira LLG,Andricopulo AD

更新日期：2020-01-01 00:00:00

abstract：:Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However,...

journal_title：Current topics in medicinal chemistry

authors： Zhou XX,Littler E

更新日期：2006-01-01 00:00:00

abstract：:The replication cycle of human immunodeficiency virus (HIV) is divided into an early and a late phase. Most of the steps of the cycle have been targeted in antiviral therapy, although the drugs currently available for clinical use are only effective against two replication enzymes of the virus, either against the reve...

journal_title：Current topics in medicinal chemistry

authors： Tözsér J

更新日期：2003-01-01 00:00:00

abstract：:In this review the conformational studies of natural enkephalins (H-Tyr-Gly-Gly-Phe-Met-OH; the [Met(5)]enkephalin and H-Tyr-Gly-Gly-Phe-Leu-OH; the [Leu(5)]enkephalin), their acyclic and cyclic analogues, including those carried out in our laboratory, performed by experimental and theoretical methods and their combin...

journal_title：Current topics in medicinal chemistry

authors： Malicka J,Czaplewski C,Groth M,Wiczk W,Oldziej S,Lankiewicz L,Ciarkowski J,Liwo A

更新日期：2004-01-01 00:00:00

abstract：:Histone deacetylases (HDACs) have recently emerged as key elements in epigenetic control of gene expression. Due to the implication of HDACs in a variety of diseases ranging from cancer to neurodegenerative disorder, HDAC inhibitors have received increased attention in recent years. Over the last few decades, a myriad...

journal_title：Current topics in medicinal chemistry

authors： Kim B,Hong J

更新日期：2015-01-01 00:00:00

abstract：:In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During the last 10 years a number of novel p38 chemotypes were dis...

journal_title：Current topics in medicinal chemistry

authors： Diller DJ,Lin TH,Metzger A

更新日期：2005-01-01 00:00:00

abstract：:Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that ar...

journal_title：Current topics in medicinal chemistry

authors： Minkkilä A,Saario S,Nevalainen T

更新日期：2010-01-01 00:00:00

abstract：:Cancer cells alter their metabolism to support the uninterrupted supply of biosynthetic molecules required for continuous proliferation. Glucose metabolism is frequently reprogrammed in several tumors in addition to fatty acid, amino acid and glutamine metabolism. Pyruvate Dehydrogenase Kinase (PDK) is a gatekeeper en...

journal_title：Current topics in medicinal chemistry

authors： Sradhanjali S,Reddy MM

更新日期：2018-01-01 00:00:00

abstract：:Interest in the chemistry and biological properties of non-nucleoside N-glycosidic compounds has gathered pace over the past several years; the occurrence of the N-glycoside moiety in glycoproteins and a range of active natural products has prompted the synthesis of a diverse spectrum of related materials with promisi...

journal_title：Current topics in medicinal chemistry

authors： Norris P

更新日期：2008-01-01 00:00:00

abstract：INTRODUCTION:Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as ho...

journal_title：Current topics in medicinal chemistry

authors： Pant A,Pasupureddy R,Pande V,Seshadri S,Dixit R,Pandey KC

更新日期：2017-01-01 00:00:00

abstract：:This article focuses on the GDNF family of neurotrophic factors as a potential new class of therapeutics for neuropathic pain, with a particular emphasis on the ligands, artemin and GDNF. In vivo activity of the ligands, expression of ligands and receptors after peripheral nerve injury, and modulation of nerve injury-...

journal_title：Current topics in medicinal chemistry

authors： Sah DW,Ossipov MH,Rossomando A,Silvian L,Porreca F

更新日期：2005-01-01 00:00:00

abstract：:The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines. These subtypes have been explored and structure-a...

journal_title：Current topics in medicinal chemistry

authors： Ferraris D,Belyakov S,Li W,Oliver E,Ko YS,Calvin D,Lautar S,Thomas B,Rojas C

更新日期：2007-01-01 00:00:00

abstract：:Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can b...

journal_title：Current topics in medicinal chemistry

authors： Kirk KL

更新日期：2006-01-01 00:00:00

abstract：:Glycopeptide antibiotics are complex natural products biosynthesized by several actinomycete genera. They inhibit bacterial growth by interfering with cell wall biosynthesis. Glycopeptide antibiotics consist of a heptapeptide skeleton highly modified through cross-links of the aromatic moieties. In addition, they are ...

journal_title：Current topics in medicinal chemistry

authors： Donadio S,Sosio M

更新日期：2008-01-01 00:00:00

abstract：:The scaffold protein Axin plays important roles in multiple signaling pathways through mediating the formation of different signaling complexes. Axin is best known for its role as a negative regulator in Wnt/β-catenin pathway. Aberrant activation of the key components in Wnt/β-catenin pathway including Axin has been l...

journal_title：Current topics in medicinal chemistry

authors： Song X,Cai W,Li L

更新日期：2016-01-01 00:00:00

abstract：:Transition metal complexes with terpyridine ligands have attracted a widespread interest with respect to biomedical applications: [(tpy)PtCl]Cl and [(tpy)RuCl(3)] are potent anti-tumor agents with activities comparable to those of cisplatin and carboplatin. The Ru(II) complexes feature a high potential as reactive pro...

journal_title：Current topics in medicinal chemistry

authors： Winter A,Gottschaldt M,Newkome GR,Schubert US

更新日期：2012-01-01 00:00:00

abstract：:Leukocytes and lung structural cells contribute to the pathophysiology of asthma through the production of numerous mediators including serine proteases. Such proteases include mast cell tryptase and chymase; neutrophil elastase, cathepsin G and myeloblastin (proteinase 3); bronchial epithelial cell-derived transmembr...

journal_title：Current topics in medicinal chemistry

authors： Guay C,Laviolette M,Tremblay GM

更新日期：2006-01-01 00:00:00

abstract：:Many efforts are currently being made to connect small molecules to target proteins by extracting pharmacological data from bibliographic sources and storing them in annotated chemical libraries. Here, small molecules are further connected to biological pathways, with particular focus to pathways involving members of ...

journal_title：Current topics in medicinal chemistry

authors： Hettne K,Cases M,Boyer S,Mestres J

更新日期：2007-01-01 00:00:00

abstract：:Trichomoniasis, one of the most common non-viral sexually transmitted infections worldwide, is caused by the parasite Trichomonas vaginalis. The pathogen colonizes the human urogenital tract, and the infection is associated with complications such as adverse pregnancy outcomes, cervical cancer, and an increase in HIV ...

journal_title：Current topics in medicinal chemistry

authors： Ferla M,Tasca T

更新日期：2021-01-01 00:00:00

abstract：:In this paper we applied the "macromolecular docking" procedure to perform molecular modeling with the aim of screening transcription factor sequences for possible interaction to the HIV-1 TAR-RNA, employing the software Hex version 4.2. The molecular modeling data were compared with electrophoretic mobility shift ass...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Mischiati C,Ather A,Ohyama T,Dedachi K,Borgatti M,Kurita N,Gambari R

更新日期：2012-01-01 00:00:00

abstract：:Latest microarray-based technologies, including small molecule-, peptide-, protein- and cell-based arrays, and their applications in the field of proteomics are reviewed. ...

journal_title：Current topics in medicinal chemistry

authors： Chen GY,Uttamchandani M,Lue RY,Lesaicherrea ML,Yao SQ

更新日期：2003-01-01 00:00:00

abstract：:In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is fast becoming an alternative to other existing strategies of drug development. These hybrids also known as 'dual drugs' or 'double drugs' are especially found to be effective in overcoming drug resistance prob...

journal_title：Current topics in medicinal chemistry

authors： Manohar S,Tripathi M,Rawat DS

更新日期：2014-01-01 00:00:00

abstract：:Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects largely synovial joints. It has been postulated that activated autoreactive CD4 T cells play a key role in triggering and/or maintaining the chronic inflammatory process in RA. Dendritic cells (DCs) are antigen-presenting cells that ac...

journal_title：Current topics in medicinal chemistry

authors： Rodríguez-Fernández JL

更新日期：2013-01-01 00:00:00

abstract：:The Human Genome Project and the explosion of high-throughput data have transformed the areas of molecular and personalized medicine, which are producing a wide range of studies and experimental results and providing new insights for developing medical applications. Research in many interdisciplinary fields is resulti...

journal_title：Current topics in medicinal chemistry

authors： de la Iglesia D,García-Remesal M,de la Calle G,Kulikowski C,Sanz F,Maojo V

更新日期：2013-01-01 00:00:00

abstract：:Homologation is a concept introduced by Gerhard in 1853 to describe a homologous series in organic chemistry. Since then, the concept has been adapted and used in medicinal chemistry as one of the most important strategies for molecular modification. The homologation types, their influence on physico-chemical properti...

journal_title：Current topics in medicinal chemistry

authors： Lima LM,Alves MA,do Amaral DN

更新日期：2019-01-01 00:00:00