NAADP signaling revisited.

abstract：:Sialorrhea or excessive drooling is a significant medical issue in Parkinson's disease (PD) and neurodegenerative disorders, although it is often underreported by patients. Sialorrhea affects a large proportion of PD patients, ranging up to 78% in advanced stages, with many PD patients considering drooling as their wo...

journal_title：Current topics in medicinal chemistry

authors： Farber NM,Perez-Lloret S,Gamzu ER

更新日期：2015-01-01 00:00:00

abstract：:The low affinity A(2B) adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various speci...

journal_title：Current topics in medicinal chemistry

authors： Volpini R,Costanzi S,Vittori S,Cristalli G,Klotz KN

更新日期：2003-01-01 00:00:00

abstract：:The atomic determination of the acetylcholine binding protein (AChBP), a molluscan cholinergic protein, homologous to the amino-terminal extracellular domain of nicotinic receptors (nAChRs), offers opportunities for the modeling of the acetylcholine binding site and its ligands. Recently, we constructed three-dimensio...

journal_title：Current topics in medicinal chemistry

authors： Grutter T,Le Novère N,Changeux JP

更新日期：2004-01-01 00:00:00

abstract：:G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited f...

journal_title：Current topics in medicinal chemistry

authors： Kontoyianni M

更新日期：2016-01-01 00:00:00

abstract：:Since the advent of high-throughput DNA sequencing technologies, the ever-increasing rate at which genomes have been published has generated new challenges notably at the level of genome annotation. Even if gene predictors and annotation softwares are more and more efficient, the ultimate validation is still in the ob...

journal_title：Current topics in medicinal chemistry

authors： Hernandez C,Waridel P,Quadroni M

更新日期：2014-01-01 00:00:00

abstract：:For effective tumour imaging by magnetic resonance imaging (MRI) there is a clear need to develop organ, tissue and cell specific contrast agents that can selectively bind to tumour biomarkers. The versatility of a range of bioconjugation techniques and facile coupling chemistries has facilitated the synthesis of MRI ...

journal_title：Current topics in medicinal chemistry

authors： Kamaly N,Miller AD,Bell JD

更新日期：2010-01-01 00:00:00

abstract：:Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivati...

journal_title：Current topics in medicinal chemistry

authors： Li HT,Zhu X

更新日期：2020-06-18 00:00:00

abstract：:Chagas disease and African sleeping sickness are trypanosomal infections that represent important public health problems in Latin America and Africa, respectively. The restriction of these diseases to the poorer parts of the world has meant that they have been largely neglected and limited progress has been made in th...

journal_title：Current topics in medicinal chemistry

authors： Wilkinson SR,Bot C,Kelly JM,Hall BS

更新日期：2011-01-01 00:00:00

abstract：:Cathepsin S has been of increasing interest as a target of medicinal chemistry efforts given its role in modulating antigen-presentation by major histocompatibility class II (MHC II) molecules as well as its involvement in extracellular proteolytic activities. Inhibition of the cathepsin S enzyme reduces degradation o...

journal_title：Current topics in medicinal chemistry

authors： Wiener JJ,Sun S,Thurmond RL

更新日期：2010-01-01 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：:Firefly shows bioluminescence by "luciferin-luciferase" (L-L) reaction using luciferin, luciferase, ATP and O2. The chemical photon generation by an enzymatic reaction is widely utilized for analytical methods including biological imaging in the life science fields. To expand photondetecting analyses with firefly biol...

journal_title：Current topics in medicinal chemistry

authors： Hirano T

更新日期：2016-01-01 00:00:00

abstract：:There exists a huge attrition rate of molecules in clinical trials. It was expected that high-throughput screening and combinatorial chemistry would make the task of producing drugs easier. However, the efforts of the past decade have not been an unvarnished success. As a result, a lot of experimental and computationa...

journal_title：Current topics in medicinal chemistry

authors： Ajay

更新日期：2002-12-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) are a class of peptides found across a wide array of organisms that play key roles in host defense. AMPs induce selective death in target cells and orchestrate specific or nonspecific immune responses. Many AMPs exhibit native anticancer activity in addition to antibacterial activity, and...

journal_title：Current topics in medicinal chemistry

authors： Rubin SJS,Qvit N

更新日期：2020-01-01 00:00:00

abstract：:This article is a review with 83 references of the application of NMR to the measurement of the dissociation constants of protein-ligand complexes. After briefly discussing some general concepts of molecular stability, the text turns to consider which NMR parameters are reporters of complex formation. The available da...

journal_title：Current topics in medicinal chemistry

authors： Fielding L

更新日期：2003-01-01 00:00:00

abstract：:Prion diseases or transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative disorders associated with the conformational conversion of the cellular prion protein, PrP(C), into a pathological form known as prion or PrP(Sc). They can be classified into sporadic, inherited and infectious forms. Spontan...

journal_title：Current topics in medicinal chemistry

authors： Biljan I,Ilc G,Giachin G,Legname G,Plavec J

更新日期：2013-01-01 00:00:00

abstract：:Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and ...

journal_title：Current topics in medicinal chemistry

authors： Rayar AM,Lagarde N,Ferroud C,Zagury JF,Montes M,Sylla-Iyarreta Veitia M

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:Nowadays, malaria is still one of the most important and lethal diseases worldwide, causing 445,000 deaths in a year. Due to the actual treatment resistance, there is an emergency to find new drugs. OBJECTIVE:The aim of this work was to find potential inhibitors of phosphoglycerate mutase 1 from P. falcipar...

journal_title：Current topics in medicinal chemistry

authors： Ríos-Soto L,Avitia-Domínguez C,Sierra-Campos E,Valdez-Solana M,Cisneros-Martínez J,Palacio-Gastellum MG,Téllez-Valencia A

更新日期：2018-01-01 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：:The dynamics of gene expression are regulated by histone acetylases (HATs) and histone deacetylases (HDACs) that control the acetylation state of lysine side chains of the histone proteins of chromatin. The catalytic activity of these two enzymes remodels chromatin to control gene expression without altering gene sequ...

journal_title：Current topics in medicinal chemistry

authors： Wiech NL,Fisher JF,Helquist P,Wiest O

更新日期：2009-01-01 00:00:00

abstract：:Although water molecules are small and only consist of two different atom types, they play various roles in cellular systems. This review discusses their influence on the binding process between biomacromolecular targets and small molecule ligands and how this influence can be modeled in computational drug design appr...

journal_title：Current topics in medicinal chemistry

authors： de Beer SB,Vermeulen NP,Oostenbrink C

更新日期：2010-01-01 00:00:00

abstract：:Over the last decade, a number of computational methods have been developed, which attempt to evaluate the thermodynamic properties of individual water molecules at the solute-solvent interface, in order to assess contributions to protein-ligand binding. In some cases, these tools tell us what we already know, e.g. th...

journal_title：Current topics in medicinal chemistry

authors： Graves AP,Wall ID,Edge CM,Woolven JM,Cui G,Le Gall A,Hong X,Raha K,Manas ES

更新日期：2017-01-01 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：:Much attention has focused on the development of protein kinases as drug targets to treat a variety of human diseases including diabetes, cancer, hypertension and arthritis. To date, Gleevec is one example of a drug targeting protein that has successfully treated human cancer. Several other protein kinase inhibitors a...

journal_title：Current topics in medicinal chemistry

authors： Haystead TA

更新日期：2006-01-01 00:00:00

abstract：:The genetic material in humans contains approximately 6 billion base pairs in the nuclear genome and 16,569 base pairs in the mitochondrial genome [1-3]. In some cases the difference between a healthy and a sick individual consists in only one nucleotide. Thus, it is evident that the pristine replication of the genome...

journal_title：Current topics in medicinal chemistry

authors： Brieba LG

更新日期：2008-01-01 00:00:00

abstract：:Pyrola (Pyrolaceae), also known as Luxiancao/in China, was recorded in Sheng Nong's Herbal Classic listed in top grade. Pyrola herbs were used as medicinal plants for a long history with wide-ranging activities such as nourishing kidney-yang, strengthening muscles and bones, activating blood, stopping bleeding, dispel...

journal_title：Current topics in medicinal chemistry

authors： Yang X,She J,Liu J,Yang T,An G,Chen Q,Fan C,Li S,Liu Q,Qian C,Liu Y,Zhou Y,Zhao J

更新日期：2020-01-01 00:00:00

abstract：:Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and recept...

journal_title：Current topics in medicinal chemistry

authors： Pereira TM,Franco DP,Vitorio F,Kummerle AE

更新日期：2018-01-01 00:00:00

abstract：:Cells rely on several transition metals to regulate a wide range of metabolic and signaling functions. The diversity and efficiency of their physiological functions are derived from atomic properties that are specific to transition metals, most notably an incomplete inner valence subshell. These properties impart upon...

journal_title：Current topics in medicinal chemistry

authors： Hamai D,Bondy SC,Becaria A,Campbell A

更新日期：2001-12-01 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：BACKGROUND:Antimicrobial research is being focused to look for more effective therapeutics against antibiotic-resistant infections caused by methicillin-resistant Staphylococcus aureus (MRSA). In this direction, antimicrobial peptides (AMP) appear as promising tool. OBJECTIVES:This study evaluated the antimicrobial ac...

journal_title：Current topics in medicinal chemistry

authors： Ciandrini E,Morroni G,Arzeni D,Kamysz W,Neubauer D,Kamysz E,Cirioni O,Brescini L,Baffone W,Campana R

更新日期：2018-01-01 00:00:00

abstract：:Combinatorial chemistry has had a major impact on the discovery and optimisation of potential lead compounds. This review details some of the fundamental principles behind combinatorial chemistry and describes a variety of methods employed in the search for new therapeutically interesting compounds including the conce...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Martin RM,Mittoo S,Bradley M

更新日期：2004-01-01 00:00:00