Pyranose N-glycosyl amines: emerging targets with diverse biological potential.

abstract：:Psychiatric diagnosis has long been perceived as more of an art than a science since its foundations lie within the observation, and the self-report of the patients themselves and objective diagnostic biomarkers are lacking. Furthermore, the diagnostic tools in use not only stray away from the conventional medical fra...

journal_title：Current topics in medicinal chemistry

authors： Todeva-Radneva A,Paunova R,Kandilarova S,St Stoyanov D

更新日期：2020-01-01 00:00:00

abstract：:Identifying drug binding sites and elucidating drug action mechanisms are important components in a drug discovery process. In this review, we briefly compared three different approaches (sequence- based methods, structure-based methods and probe-based molecular dynamics (MD) methods) to identifying drug binding sites...

journal_title：Current topics in medicinal chemistry

authors： Wang Y,Lupala CS,Liu H,Lin X

更新日期：2018-01-01 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：:Multiple Gαi protein-coupled somatostatin receptors (SSTRs) are expressed in human kidney and liver tissues. Also, aberrant cAMP signaling has been shown to play a critical role in cysto-genesis and enlargement of the human kidney and liver. Thus, somatostatin (SST) analogs become potential and promising alternatives ...

journal_title：Current topics in medicinal chemistry

authors： Sun L,Yu CY,Mackey LV,Coy DH

更新日期：2015-01-01 00:00:00

abstract：:Due to the recent advancements in stem cell biology and engineering, scientists have been increasingly interested in creating in vitro niches for embryonic and adult stem cells, and, following induction and differentiation with the appropriate media, the production of large scale blood production. This artificially cr...

journal_title：Current topics in medicinal chemistry

authors： Didwania M,Didwania A,Mehta G,Basak GW,Yasukawa S,Takayama S,de Necochea-Campion R,Srivastava A,Carrier E

更新日期：2011-01-01 00:00:00

abstract：:The emergence of new DNA sequencing technologies has allowed an exponential growth of genomic and transcriptomic data that ultimately yielded important results to several areas such as medicine and biology. This continuous technological progress presents several advantages and caveats that have to be considered for ea...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Flores A,Abreu-Goodger C

更新日期：2014-01-01 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：:It is well established that matrix metalloproteinases (MMPs) contribute to the degradation of the extracellular matrix of coronary plaque and contribute to the thinning of the fibrous cap. As a result, the atheromatous plaque becomes unstable and prone to rupture with consequent clinical manifestations including acute...

journal_title：Current topics in medicinal chemistry

authors： Papageorgiou N,Tousoulis D,Hatzis G,Briasoulis A,Androulakis E,Giolis A,Siasos G,Latsios G,Vogiatzi G,Tentolouris C,Stefanadis C

更新日期：2012-01-01 00:00:00

abstract：:One year after its first outbreak reported in China, coronavirus disease 2019 (COVID-19) pandemic is still sweeping the World causing serious infections and claiming more fatalities. COVID-19 is caused by the novel corona virus SARS-CoV-2, which belongs to the genus Betacoronavirus (β-CoVs) which is of greatest clinic...

journal_title：Current topics in medicinal chemistry

authors： Sabbah DA,Hajjo R,Bardaweel SK,Zhong HA

更新日期：2021-01-18 00:00:00

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：:Degenerative diseases are becoming more common with increasing life expectancy of the human population. The 20th century faced a progressive demographic change in the industrialized world, followed by identical trends in population aging in Asia, Africa, and Middle and South America. A significant increase in chronic ...

journal_title：Current topics in medicinal chemistry

authors： Delogu GL,Matos MJ

更新日期：2017-01-01 00:00:00

abstract：:At present, a limited number of strategies exist for diagnostic imaging of patients with bacterial infection. While radiolabeled probes and white blood cells provide robust solutions to detect bacteria in humans, they also give false positives in cases of sterile inflammation. With the onset of bacterial drug resistan...

journal_title：Current topics in medicinal chemistry

authors： Sasser TA,Van Avermaete AE,White A,Chapman S,Johnson JR,Van Avermaete T,Gammon ST,Leevy WM

更新日期：2013-01-01 00:00:00

abstract：:This review reports the recent advances in chlorotoxin (CTX)-targeted nanoparticles (NPs) for imaging and therapy of glioma. CTX has been identified as a targeting ligand to specifically bind to glioma. Through different conjugation approaches, CTX can be conjugated onto iron oxide NPs, quantum dots, and rare-earth up...

journal_title：Current topics in medicinal chemistry

authors： Zhao L,Shi X,Zhao J

更新日期：2015-01-01 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：: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：: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：: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：: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

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：:This review mainly covers last five year literature on CCK1R agonists and antagonists. These CCK1R ligands have been found following the two usual and complementary strategies for drug discovery: rational design based on structure activity relationships on the CCK-7 and CCK-4 peptide sequences of the endogenous ligand...

journal_title：Current topics in medicinal chemistry

authors： García-López MT,González-Muñiz R,Martín-Martínez M,Herranz R

更新日期：2007-01-01 00:00:00

abstract：:Screening and identifying a disease-specific novel drug target is the first step towards a rational drug designing approach. Due to the advent of high throughput data generation techniques, the protein search space has now exceeded 24,500 human protein coding genes, which encodes approximately 1804proteins. This work ...

journal_title：Current topics in medicinal chemistry

authors： Jain B,Raj U,Varadwaj PK

更新日期：2018-01-01 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：BACKGROUND:Candida species are the important etiologic agents for candidiasis, the most prevalent cause of opportunistic fungal infections. Candida invasion results in mucosal to systemic infections through immune dysfunction and helps in further invasion and proliferation at several sites in the host. The host defence...

journal_title：Current topics in medicinal chemistry

authors： Wadhwa R,Pandey P,Gupta G,Aggarwal T,Kumar N,Mehta M,Satija S,Gulati M,Madan JR,Dureja H,Balusamy SR,Perumalsamy H,Maurya PK,Collet T,Tambuwala MM,Hansbro PM,Chellappan DK,Dua K

更新日期：2019-01-01 00:00:00

abstract：:A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacill...

journal_title：Current topics in medicinal chemistry

authors： Chandna N,Kapoor JK,Goyal V,Aggarwal NK,Kumari KM,Vijjulatha M

更新日期：2013-08-01 00:00:00

abstract：:Phyllanthus amarus is a medicinal herb used in traditional Indian medicine for liver disorders. Several researches also show that it acts primarily in the liver, but the molecules were unidentified for liver protective activity. This study was to determine whether the lignans isolated from P. amarus attenuates the D-g...

journal_title：Current topics in medicinal chemistry

authors： Bawankule DU,Trivedi P,Pal A,Shanker K,Singh M,Sharma P,Khan F,Maurya AK,Verma RK,Gupta MM

更新日期：2014-01-01 00:00:00

abstract：:Protein-ligand binding is among the most fundamental phenomena underlying all molecular biology, and a greater ability to more accurately and robustly predict the binding free energy of a small molecule ligand for its cognate protein is expected to have vast consequences for improving the efficiency of pharmaceutical ...

journal_title：Current topics in medicinal chemistry

authors： Abel R,Wang L,Mobley DL,Friesner RA

更新日期：2017-01-01 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：: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：: ...

journal_title：Current topics in medicinal chemistry

authors： Scotti MT,Muratov EN,González-Díaz H

更新日期：2019-01-01 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