cycloSal-d4TMP pronucleotides structural variations, mechanistic insights and antiviral activity.

abstract：:Transient Receptor Potential (TRP) cation channels participate in several processes of vital importance in cell and organism physiology, and have been demonstrated to participate in the detection of sensory stimuli. The thermo TRP's reviewed: TRPV1 (vanilloid 1), TRPM8 (melastatin 8) and TRPA1 (ankyrin-like 1) are kno...

journal_title：Current topics in medicinal chemistry

authors： Nieto-Posadas A,Jara-Oseguera A,Rosenbaum T

更新日期：2011-01-01 00:00:00

abstract：:Several non-cardiovascular drugs have been withdrawn from the market due to their inhibition of hERG K+ channels that can potentially lead to severe heart arrhythmia and death. As hERG safety testing is a mandatory FDArequired procedure, there is a considerable interest for developing predictive computational tools to...

journal_title：Current topics in medicinal chemistry

authors： Braga RC,Alves VM,Silva MF,Muratov E,Fourches D,Tropsha A,Andrade CH

更新日期：2014-01-01 00:00:00

abstract：:Increasing evidence has shown that chemokine receptors may form functional dimers with unique pharmacological profiles. A common practice to characterize such G protein-coupled receptor dimerization processes is to apply bivalent ligands as chemical probes which can interact with both receptors simultaneously. Current...

journal_title：Current topics in medicinal chemistry

authors： Arnatt CK,Zhang Y

更新日期：2014-01-01 00:00:00

abstract：:Nicotinic acid adenine dinucleotide phosphate (NAADP) is the most potent Ca²⁺ mobilizing endogenous compound known to date. Although its Ca²⁺ releasing activity has been demonstrated in many cell types and in response to different extracellular stimuli, several aspects of NAADP signaling are unclear. This overview foc...

journal_title：Current topics in medicinal chemistry

authors： Guse AH,Ernst IM,Fliegert R

更新日期：2013-01-01 00:00:00

abstract：:The computational assessment of drug metabolism has gained considerable interest in pharmaceutical research. Amongst others, machine learning techniques have been employed to model relationships between the chemical structure of a compound and its metabolic fate. Examples for these techniques, which were originally de...

journal_title：Current topics in medicinal chemistry

authors： Fox T,Kriegl JM

更新日期：2006-01-01 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：:The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available da...

journal_title：Current topics in medicinal chemistry

authors： Trautman EP,Crawford JM

更新日期：2016-01-01 00:00:00

abstract：:Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...

journal_title：Current topics in medicinal chemistry

authors： Szolcsányi J,Pintér E,Helyes Z,Petho G

更新日期：2011-01-01 00:00:00

abstract：:Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain. pH buffering of extra- and...

journal_title：Current topics in medicinal chemistry

authors： Thiry A,Dogné JM,Supuran CT,Masereel B

更新日期：2007-01-01 00:00:00

abstract：:The serotonin receptor subtype 5 HT(1A) was one of the first serotonin receptor subtypes pharmacologically characterized. Over the last twenty years the 5 HT(1A) receptor has been the object of intense research efforts as witnessed by the 5 HT(1A) acting drugs marketed as anxiolytics. In recent years, several new chem...

journal_title：Current topics in medicinal chemistry

authors： Lacivita E,Leopoldo M,Berardi F,Perrone R

更新日期：2008-01-01 00:00:00

abstract：:Aromatic polyketides represent important members of the family of polyketides, which have displayed a wide assortment of bioactive properties, such as antibacterial, antitumor, and antiviral activities. Bacterial aromatic polyketides are mainly synthesized by type II polyketide synthases (PKSs). Whereas malonyl-CoA is...

journal_title：Current topics in medicinal chemistry

authors： Zhan J

更新日期：2009-01-01 00:00:00

abstract：:L-DOPA is a di-hydroxy-phenyl, catecholamine precursor, amino acid, initially considered as an inert compound and now the key stone for the treatment of Parkinson's disease (PD) and some hereditary dystonias. L-DOPA, when administered to mammals, is rapidly metabolized to dopamine and 3-OM-DOPA, and its half-life in p...

journal_title：Current topics in medicinal chemistry

authors： Mena MA,Casarejos MJ,Solano RM,de Yébenes JG

更新日期：2009-01-01 00:00:00

abstract：:Our understanding of glutamatergic transmission in the central nervous system has been greatly expanded with the discovery and investigation of the metabotropic glutamate receptor family. Complementing the ionotropic glutamate-gated ion channels, these G-protein coupled receptors play critical roles in neuronal and gl...

journal_title：Current topics in medicinal chemistry

authors： Niswender CM,Jones CK,Conn PJ

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND:The considerable increase in the incidence of Candida infection in recent times has prompted the use of numerous antifungal agents, which has resulted in the development of resistance towards various antifungal agents. With rising Candida infections, the need for design and development of novel antifungal ag...

journal_title：Current topics in medicinal chemistry

authors： Gowda DV,Afrasim M,Meenakshi SI,Manohar M,Hemalatha S,Siddaramaiah H,Sathishbabu P,Rizvi SMD,Hussain T,Kamal MA

更新日期：2019-01-01 00:00:00

abstract：:The recognition that malfunction of the microtubule (MT) associated protein tau is likely to play a defining role in the onset and/or progression of a number of neurodegenerative diseases, including Alzheimer's disease, has resulted in the initiation of drug discovery programs that target this protein. Tau is an endog...

journal_title：Current topics in medicinal chemistry

authors： Ballatore C,Brunden KR,Trojanowski JQ,Lee VM,Smith AB 3rd,Huryn DM

更新日期：2011-01-01 00:00:00

abstract：:Recent advances in synthesis of functional poly-ε-caprolactone (PCL) and its self-assembly behavior, as well as application in drug delivery have been reviewed. Three strategies including end group functionalization, postpolymerization modification and new monomer preparation have been summarized to show possibilities...

journal_title：Current topics in medicinal chemistry

authors： Xiao Y,Yuan M,Zhang J,Yan J,Lang M

更新日期：2014-01-01 00:00:00

abstract：:The neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) family of hormones exhibit a wide variety of biological actions on the mammalian gastrointestinal tract through known G-protein coupled receptor pathways. At least four receptor subtypes, denoted as Y(1), Y(2), Y(4) an Y(5), each with specific ...

journal_title：Current topics in medicinal chemistry

authors： Vona-Davis LC,McFadden DW

更新日期：2007-01-01 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 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：:Sphingosine 1-phosphate (S1P) evokes a plethora of physiological responses by stimulating members of a G protein-coupled receptor family, known as S1P receptors. Currently five different mammalian S1P receptor subtypes, S1P₁₋₅, each with a different cellular expression pattern, were identified. The S1P₁ receptor in pa...

journal_title：Current topics in medicinal chemistry

authors： Bolli MH,Lescop C,Nayler O

更新日期：2011-01-01 00:00:00

abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...

journal_title：Current topics in medicinal chemistry

authors： Thai KM,Ngo TD,Tran TD,Le MT

更新日期：2013-01-01 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：:Asthma, a chronic inflammatory disease of the airways, is a significant burden on our healthcare system. There is high unmet need for treatments directed towards the underlying causes of the disease. The cell surface integrin VLA-4 (very late antigen-4; alpha4beta1; CD49d/CD29) plays an important role in the trafficki...

journal_title：Current topics in medicinal chemistry

authors： Singh J,Adams S,Carter MB,Cuervo H,Lee WC,Lobb RR,Pepinsky RB,Petter R,Scott D

更新日期：2004-01-01 00:00:00

abstract：:The sol-gel process provides a robust and versatile technology for the immobilization of biologicals. A wide range of inorganic, composites and hybrid materials can be prepared to encapsulate molecular drugs, proteins, antibodies/antigens, enzymes, nucleic acids, prokaryotic and eukaryotic cells into bulk gels, partic...

journal_title：Current topics in medicinal chemistry

authors： Wang X,Ahmed NB,Alvarez GS,Tuttolomondo MV,Hélary C,Desimone MF,Coradin T

更新日期：2015-01-01 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：:Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in clinical development is reviewed. The review is organized around three main decision points used in discovery including hit generation, lead optimization and final can...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Tang W,Dasgupta M,Hasting B

更新日期：2009-01-01 00:00:00

abstract：:Tanshinones are a class of bioactive compounds present in the Chinese herbal medicine Danshen (Salvia miltiorrhiza Bunge), containing among others, abietane diterpene quinone scaffolds. Chemical synthesis and biological activity studies of natural and unnatural tanshinone derivatives have been reviewed in this article...

journal_title：Current topics in medicinal chemistry

authors： Huang H,Song C,Chang J

更新日期：2020-01-01 00:00:00

abstract：:This is a general review of currently available antimalarial drugs, these compounds are gathered according with its chemical structure and the biological targets. A great number of these new antimalarial agents are now moving actively in the pipeline from basic science to clinical studies. ...

journal_title：Current topics in medicinal chemistry

authors： Domínguez JN

更新日期：2002-11-01 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：:Millions of deaths each year are attributed to malaria worldwide. Transmitted through the bite of an Anopheles mosquito, infection and subsequent death from the Plasmodium species, most notably P. falciparum, can readily spread through a susceptible population. A malaria vaccine does not exist and resistance to virtua...

journal_title：Current topics in medicinal chemistry

authors： Zhang VM,Chavchich M,Waters NC

更新日期：2012-01-01 00:00:00