NPY family of hormones: clinical relevance and potential use in gastrointestinal disease.

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：:As master regulators of lipid metabolism the peroxisome proliferator activated receptor (PPAR) family controls a wide variety of cellular processes, and thus it is not surprising that a large effort has focussed on discovering agents to pharmacologically modulate activity of these receptors. Early generation PPAR liga...

journal_title：Current topics in medicinal chemistry

authors： Etgen GJ,Mantlo N

更新日期：2003-01-01 00:00:00

abstract：:Results of various projects on Mexican Indian ethnobotany and some of the subsequent pharmacological and phytochemical studies are summarised focusing both on chemical-pharmacological as well as anthropological (ethnopharmacological) aspects of our research. We have identified taste and smell properties of medicinal (...

journal_title：Current topics in medicinal chemistry

authors： Heinrich M

更新日期：2003-01-01 00:00:00

abstract：:The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally α-amino acids with one or more stereogenic centers due to st...

journal_title：Current topics in medicinal chemistry

authors： Vogensen SB,Greenwood JR,Bunch L,Clausen RP

更新日期：2011-01-01 00:00:00

abstract：:Aptamers- short nucleic acid or peptide ligands- attracted considerable attention across various disciplines as target specific therapeutic, delivery vehicle and diagnostic tools. The applicability of aptamers - often termed as 'chemical antibodies' - continues to grow and possess certain edge over the antibody counte...

journal_title：Current topics in medicinal chemistry

authors： Veedu RN

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly a...

journal_title：Current topics in medicinal chemistry

authors： Nandi S,Kaur R,Kumar M,Sharma A,Naaz A,Mandal SC

更新日期：2018-01-01 00:00:00

abstract：:The adenosine A(2A) receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A(2A) receptor with several pathological conditions such as neurodegenerative disorde...

journal_title：Current topics in medicinal chemistry

authors： Clementina M,Giuseppe S

更新日期：2010-01-01 00:00:00

abstract：:This article reviews recent molecular dynamics simulations of the Alzheimer's amyloid-β protein, the primary component of the amyloid plaques found in the brain of Alzheimer's patients. Different simulation techniques, and their application to the study of monomeric, oligomeric, and fibrillar species is discussed. Thi...

journal_title：Current topics in medicinal chemistry

authors： Shea JE,Urbanc B

更新日期：2012-01-01 00:00:00

abstract：:Anticancer drug screening can accelerate drug discovery to save the lives of cancer patients, but cancer heterogeneity makes this screening challenging. The prediction of anticancer drug sensitivity is useful for anticancer drug development and the identification of biomarkers of drug sensitivity. Deep learning, as a ...

journal_title：Current topics in medicinal chemistry

authors： Tan X,Yu Y,Duan K,Zhang J,Sun P,Sun H

更新日期：2020-01-01 00:00:00

abstract：:Olefin metathesis has rapidly established itself as an essential tool in the synthetic chemist's armoury. The ease of operation and functional group tolerance that is obtained with the modern generation of catalysts makes the use of metathesis an extremely attractive option when preparing medicinally interesting molec...

journal_title：Current topics in medicinal chemistry

authors： Martin WH,Blechert S

更新日期：2005-01-01 00:00:00

abstract：:Although bioactivation is a well-documented process and the role of active metabolites in the drug discovery field has long been recognized, drug metabolites are usually ignored in virtual screening campaigns oriented to drug repositioning. The present article discusses different issues related to overlooking of the a...

journal_title：Current topics in medicinal chemistry

authors： Talevi A

更新日期：2016-01-01 00:00:00

abstract：:Structure-activity relationships of a 4-aminoquinoline MCH-1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4- and 6-positions of the original HTS hit. Improvements to the original screening lead were made by addition of lipophilic groups at the 2-position and biphenyl, cyc...

journal_title：Current topics in medicinal chemistry

authors： DeVita RJ

更新日期：2007-01-01 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：:Target-Related Affinity Profiling (TRAP) is a computational drug discovery technology that is based on 'affinity fingerprints', which are molecular descriptors derived from the protein binding preferences of small molecules. The underlying concepts of TRAP are reviewed. Affinity fingerprints are compared to molecular ...

journal_title：Current topics in medicinal chemistry

authors： Beroza P,Damodaran K,Lum RT

更新日期：2005-01-01 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：:Over the past decades, a tremendous rise in invasive fungal infection diseases attributed to the yeast Candida albicans in immunocompromised individuals poses a seriously challenging issue. Another concern is the emergence of multi-drug resistant pathogens to the existing medicines due to their overuse and misuse. It ...

journal_title：Current topics in medicinal chemistry

authors： Tratrat C

更新日期：2020-01-01 00:00:00

abstract：:Emergence of drug-resistant viral strains is one of the major milestones and the main cause for the failure of antiretroviral therapy. Combination of different anti-HIV agents has become the standard clinical practice to keep the viral load at low or even undetectable levels and to prevent emergence of virus-drug resi...

journal_title：Current topics in medicinal chemistry

authors： Camarasa MJ,San-Félix A,Velázquez S,Pérez-Pérez MJ,Gago F,Balzarini J

更新日期：2004-01-01 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：: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：: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：:A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Lang W,Masucci JA

更新日期：2012-01-01 00:00:00

abstract：:Cancer research has progressed leaps and bounds over the years. This review is a brief overview of the cancer research, milestone achievements and therapeutic studies on it over the one hundred ten years which would give us an insight into how far we have come to understand and combat this fatal disease leading to mil...

journal_title：Current topics in medicinal chemistry

authors： Shastri S,Chatterjee B,Thakur SS

更新日期：2019-01-01 00:00:00

abstract：:The vesicular acetylcholine transporter (VAChT) is a glycoprotein responsible for the accumulation of acetylcholine into pre-synaptic vesicules of cholinergic neurons. Cholinergic innervation has been shown to be decreased at the earlier stages of Alzheimer's disease (AD). Thus, the expression of VAChT has been correl...

journal_title：Current topics in medicinal chemistry

authors： Giboureau N,Som IM,Boucher-Arnold A,Guilloteau D,Kassiou M

更新日期：2010-01-01 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：:Iron chelators may be of value as therapeutic agents in the treatment of cancer. They may act by depleting iron, a necessary nutrient, and limiting tumor growth. Alternatively or additionally, they may form redox-active metal complexes that cause oxidative stress via production of reactive oxygen species, damaging cri...

journal_title：Current topics in medicinal chemistry

authors： Buss JL,Greene BT,Turner J,Torti FM,Torti SV

更新日期：2004-01-01 00:00:00

abstract：INTRODUCTION:Structure-based drug design is a wide area of identification of selective inhibitors of a target of interest. From the time of the availability of three dimensional structure of the drug targets, mostly the proteins, many computational methods had emerged to address the challenges associated with drug desi...

journal_title：Current topics in medicinal chemistry

authors： Velmurugan D,Pachaiappan R,Ramakrishnan C

更新日期：2020-01-01 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：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：: ...

journal_title：Current topics in medicinal chemistry

authors： Dea-Ayuela MA,Serrano DR

更新日期：2018-01-01 00:00:00

abstract：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00