Recent advances in the design of cathepsin S inhibitors.

abstract：:Several non-cardiovascular drugs have been withdrawn from the market due to their inhibition of hERG K+ channels that can potentially lead to severe heart arrhythmia and death.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：: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：: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：:Tuberculosis (TB) is caused by the bacterium Mycobacterium tuberculosis and is a common infectious disease with high mortality and morbidity. The increasing prevalence of drug-resistant strains of TB presents a major public health problem. Due to the lack of effective drugs to treat these drug-resistant strains, the d...

journal_title：Current topics in medicinal chemistry

authors： Koseki Y,Aoki S

更新日期：2014-01-01 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 genetics of Alzheimer's disease (AD) implies that restoring non-pathological levels or ratios of different amyloid-beta (Abeta) peptide species in the brain could prevent the onset or delay the progression of this neurodegenerative disease. In particular, a selective reduction of the longer Abeta(1-42) peptide whi...

journal_title：Current topics in medicinal chemistry

authors： Beher D

更新日期：2008-01-01 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：:The introduction of biochemical biomarkers in the evaluation of patients with cardiovascular disease has led to practice-changing advancements in the way these patients are diagnosed and managed. Measurements of cardiac troponins or brain-type natriuretic peptide (BNP) and its precursor, N-terminal brain-type natriure...

journal_title：Current topics in medicinal chemistry

authors： Giannopoulos G,Deftereos S,Panagopoulou V,Kossyvakis C,Kaoukis A,Bouras G,Pyrgakis V,Cleman MW

更新日期：2013-01-01 00:00:00

abstract：INTRODUCTION:Anxiety disorders manifest in women more than in men by almost twofold. This narrative review aims to summarize the sex-related biological factors, which underpin anxiety, focusing on the interactions of sex and tryptophan/serotonin with anxiety. METHODS:A literature search was conducted using Google Scho...

journal_title：Current topics in medicinal chemistry

authors： Songtachalert T,Roomruangwong C,Carvalho AF,Bourin M,Maes M

更新日期：2018-01-01 00:00:00

abstract：:The problem in this work is the computational characterization of cyclodextrins, crown ethers and hyaluronan (HA) as hosts of inclusion complexes for nanosized drug delivery vehicles in pharmaceutical formulations. The difficulty is addressed through a computational study of some thermodynamic, geometric and topologic...

journal_title：Current topics in medicinal chemistry

authors： Torrens F,Castellano G

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：BACKGROUND:Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS:A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofil...

journal_title：Current topics in medicinal chemistry

authors： Singla RK,Dubey AK

更新日期：2019-01-01 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 task of rationally designing vaccines that can effectively impact on the survival of cancer patients remains challenging. Monoclonal antibodies and T cell receptors have proven to be viable templates for the application of pharmacophore design principles to develop antigens and immunogens as these immune system mo...

journal_title：Current topics in medicinal chemistry

authors： Pashov A,Perry M,Dyar M,Chow M,Kieber-Emmons T

更新日期：2005-01-01 00:00:00

abstract：:The ryanodine receptor (RyR) is the major calcium (Ca(2+)) release channel in the sarcoplasmic reticulum (SR) of skeletal and cardiac muscle and is required for excitation-contraction (EC) coupling. The 565 kDa RyR protein forms a tetrameric channel that is part of a macromolecular signaling complex that also includes...

journal_title：Current topics in medicinal chemistry

authors： Lehnart SE,Huang F,Marx SO,Marks AR

更新日期：2003-01-01 00:00:00

abstract：:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular sys...

journal_title：Current topics in medicinal chemistry

authors： Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo C

更新日期：2014-01-01 00:00:00

abstract：:Angiotensin II (AII), Asp1-Arg2-Val3-Tyr4-Ile5-His6-Pro7-Phe8, the primary active hormone of the Renin-Angiotensin-System (RAS), is a major vasoconstrictor implicated in the cause of hypertension. To unravel the question of the biologically active conformation(s) of this flexible peptide hormone and to better understa...

journal_title：Current topics in medicinal chemistry

authors： Tzakos AG,Gerothanassis IP,Troganis AN

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：: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：: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：:Drugs with poor lipid and water solubility are some of the most challenging to formulate in nanocarriers, typically resulting in low encapsulation efficiencies and uncontrolled release profiles. PEGylated nanocapsules (PEG-NC) are known for their amenability to diverse modifications that allow the formation of domains...

journal_title：Current topics in medicinal chemistry

authors： Hervella P,Alonso-Sande M,Ledo F,Lucero ML,Alonso MJ,Garcia-Fuentes M

更新日期：2014-01-01 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：: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：: ...

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：: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：: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：: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 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：:Alzheimer's disease (AD) is a multifactorial complex disease. The pathogenesis of AD is very complicated, and involves the β-amyloid (Aβ) cascade, tau hyperphosphorylation, neuroinflammation, oxidative stress, mitochondrial dysfunction, reduced levels of neurotrophic factors, and damage and loss of synapses as well as...

journal_title：Current topics in medicinal chemistry

authors： Li L,Zhang L,Yang CC

更新日期：2016-01-01 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