New Experimental and Computational Tools for Drug Discovery. - Part-VII.

abstract：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 00:00:00

abstract：:Following the cloning of the classical opioid receptors (mu, delta and kappa), the opioid receptor like-1 (ORL-1) was identified as a G-protein coupled receptor (GPCR) with 65% structure homology to the other members of the opioid family. Its endogenous ligand nociception/orphanin FQ (N/OFQ) was discovered shortly the...

journal_title：Current topics in medicinal chemistry

authors： Fioravanti B,Vanderah TW

更新日期：2008-01-01 00:00:00

abstract：:Ascidians (tunicates; sea squirts) are marine animals which provide a source of diverse, bioactive natural products, and a model for toxicity screenings. Compounds isolated from ascidians comprise an approved anti-tumor drug and many others are potent drug leads. Furthermore, the use of invertebrate embryos for toxico...

journal_title：Current topics in medicinal chemistry

authors： Dumollard R,Gazo I,Gomes IDL,Besnardeau L,McDougall A

更新日期：2017-01-01 00:00:00

abstract：:Untargeted metabolomics is a promising approach for reducing the significant attrition rate for discovering and developing drugs in the pharmaceutical industry. This review aims to highlight the practical decision-making value of untargeted metabolomics for the advancement of drug candidates in drug discovery/developm...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Leo GC

更新日期：2017-01-01 00:00:00

abstract：AIMS:A series of 8-methoxy ciprofloxacin- hydrazone/acylhydrazone hybrids were evaluated for their activity against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin- resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU145 (MDR DU-145) prostate cancer cell...

journal_title：Current topics in medicinal chemistry

authors： Wang LP,Xu Z,Deng GY,Xu SL

更新日期：2020-01-01 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：: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：:Metabolic syndrome (MS) is a modern medical condition characterized by central obesity, hyperglycaemia, hypercholesterolemia and hypertension. The beneficial effects of mushrooms in lowering the symptoms of MS were known from both traditional and conventional medicine. Edible mushrooms, their extracts, polysaccharide ...

journal_title：Current topics in medicinal chemistry

authors： Kundaković T,Kolundžić M

更新日期：2013-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Nayarisseri A,Hood EA

更新日期：2018-01-01 00:00:00

abstract：:The field of quantitative structure activity relationships (QSAR) has evolved into an integral tool for pharmaceutical discovery. It is presently an accessible technology, as can be shown by the number papers which are easily found through PubMed literature searches. At one level, QSAR is used routinely and invisibly ...

journal_title：Current topics in medicinal chemistry

authors： Sprous DG,Palmer RK,Swanson JT,Lawless M

更新日期：2010-01-01 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：BACKGROUND:Chemoinformatics has several applications in the field of drug design, helping to identify new compounds against a range of ailments. Among these are Leishmaniasis, effective treatments for which are currently limited. OBJECTIVE:To construct new indole 2-aminothiophene molecules using computational tools an...

journal_title：Current topics in medicinal chemistry

authors： Félix MB,de Araújo RSA,Barros RPC,de Simone CA,Rodrigues RRL,de Lima Nunes TA,da Franca Rodrigues KA,Junior FJBM,Muratov E,Scotti L,Scotti MT

更新日期：2020-01-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) establish the first line of host defense mechanism against invading microorganisms including bacteria, viruses, fungi and parasites. In recent years, emergence and spread of antibiotic resistance bacterial pathogens have dawn considerable interest in investigations of AMPs. The ability of...

journal_title：Current topics in medicinal chemistry

authors： Bhattacharjya S

更新日期：2016-01-01 00:00:00

abstract：:Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor ...

journal_title：Current topics in medicinal chemistry

authors： Liby KT,Sporn MB

更新日期：2016-06-16 00:00:00

abstract：:Errors in the mitotic process are thought to be one of the principal sources of the genetic instability that hallmarks cancer. Unsurprisingly, many of the proteins that regulate mitosis are aberrantly expressed in tumour cells when compared to their normal counterparts. These may represent a good source of targets for...

journal_title：Current topics in medicinal chemistry

authors： Mortlock AA,Keen NJ,Jung FH,Heron NM,Foote KM,Wilkinson RW,Green S

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND:Farnesol is an acyclic sesquiterpene alcohol, endogenously synthesized via the ergosterol pathway. It is a quorum sensing molecule (QSM) that was first discovered in C. albicans, and is involved in the inhibition of hyphae formation. METHODS:This review focuses on the comprehensive details of occurrence, ch...

journal_title：Current topics in medicinal chemistry

authors： Gupta P,Sharma M,Arora N,Pruthi V,Poluri KM

更新日期：2018-01-01 00:00:00

abstract：:Thematic Analysis™ is a chemogenomic tool which has been developed and used to aid the process of GPCR drug discovery. This review covers the scientific rationale behind the development of this tool and provides examples of the successful application of the chemogenomic method in both hit finding and hit to lead stage...

journal_title：Current topics in medicinal chemistry

authors： Crossley R,Macritchie JA,Slater MJ

更新日期：2011-01-01 00:00:00

abstract：:Thermolysin (TLN) and other thermolysin-like zinc metalloproteinases (TLPs),are important virulence factors for pathogenesis of bacterial infections by suppressing the innate immune system of the host. Therapeutic inhibition ofTLPs is believed to be a novel strategy inthe development of a new generation antibiotics.In...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Dedachi K,Matsui T,Kurita N,Borgatti M,Gambari R,Sylte I

更新日期：2012-01-01 00:00:00

abstract：:Parkinson's disease (PD) is one of the most prevalent and severe neurodegenerative disease affecting more than 6.1 million people globally. It is characterized by age-related progressive deterioration of neurological functions caused by neuronal damage or neuronal death. During PD, the dopamineproducing cells in the s...

journal_title：Current topics in medicinal chemistry

authors： Kumar B,Pandey M,Fayaz F,Izneid TA,Pottoo FH,Manchanda S,Sharma A,Sahoo PK

更新日期：2020-01-01 00:00:00

abstract：:Recent advances in DNA microarray technology have great impact on many areas of biomedical research and pharmacogenomics: discovering novel targets and genes, elucidating signatures of complex diseases, transcriptional profiling of models for diseases, and the development of individually optimized drugs based on diffe...

journal_title：Current topics in medicinal chemistry

authors： Hackl H,Sanchez Cabo F,Sturn A,Wolkenhauer O,Trajanoski Z

更新日期：2004-01-01 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：:Apoptosis is a vital physiological process, which is observed in various biological events. The anti-apoptotic and pro-apoptotic members of Bcl-2 family are the most characterized proteins which are involved in the regulation of apoptotic cell death. The anti-apoptotic proteins such as Bcl-2 and Bcl-xL prevent apoptos...

journal_title：Current topics in medicinal chemistry

authors： Salam AAA,Nayek U,Sunil D

更新日期：2018-01-01 00:00:00

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：:Protein kinases (Ser/Thr and Tyr) play a key role in signal transduction pathways. It has been shown that deregulation of the Cdk activity is linked to cell proliferation and cancer. Inhibition of cyclin-dependent kinases (Cdks) is an important target for potential new anti-cancer drugs. Following the discovery of Olo...

journal_title：Current topics in medicinal chemistry

authors： Haesslein JL,Jullian N

更新日期：2002-09-01 00:00:00

abstract：:In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...

journal_title：Current topics in medicinal chemistry

authors： González-Díaz H,Arrasate S,Gómez-SanJuan A,Sotomayor N,Lete E,Besada-Porto L,Ruso JM

更新日期：2013-01-01 00:00:00

abstract：:This review discusses the state of the art, challenges and perspectives in recent applications of electrochemistry in the life sciences. It deals mainly with the elucidation of molecular mechanisms of drug action, drug design and development, involving electron transfer, pharmaco-electrochemistry (the combination of e...

journal_title：Current topics in medicinal chemistry

authors： de Paiva YG,da Rocha Ferreira F,Silva TL,Labbe E,Buriez O,Amatore C,Fonseca Goulart MO

更新日期：2015-01-01 00:00:00

abstract：:The development of computational tools for the prediction of passive transport is reviewed with particular reference to four diverse approaches: the rule-of-5, polar surface area, Volsurf and Abraham's General Solvation Equation. To illustrate the current state of the art, several examples of the application of in sil...

journal_title：Current topics in medicinal chemistry

authors： Clark DE,Grootenhuis PD

更新日期：2003-01-01 00:00:00

abstract：:Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structu...

journal_title：Current topics in medicinal chemistry

authors： Smelcerovic A,Miljkovic F,Kolarevic A,Lazarevic J,Djordjevic A,Kocic G,Anderluh M

更新日期：2015-01-01 00:00:00

abstract：:Fragment-based drug discovery (FBDD) needs a biophysical assay to complement, or even replace, biochemical screening. NMR is the best choice for this because NMR delivers many different types of data that impacts medicinal chemistry decisions. There are a multitude of different NMR methods which can be employed to the...

journal_title：Current topics in medicinal chemistry

authors： Zartler ER,Mo H

更新日期：2007-01-01 00:00:00

abstract：:Among the many important physiological functions of the activated vitamin D receptor (VDR) is the signaling of monocytic differentiation, first demonstrated by conversion of malignant myeloid leukemia cells to nonproliferating cells with mature monocyte/macrophage appearance. However, the understanding of how 1, 25-di...

journal_title：Current topics in medicinal chemistry

authors： Studzinski GP,Garay E,Patel R,Zhang J,Wang X

更新日期：2006-01-01 00:00:00