Inhibition of Pyruvate Dehydrogenase Kinase as a Therapeutic Strategy against Cancer.

abstract：:Traditionally the role of sexual steroid hormones was focused primarily on reproductive organs: the breast, female reproductive tract (uterus, mammary gland, and ovary), and male reproductive tract (testes, epididymis and prostate), however our current understanding of tissue-specific effects of sex steroids has eluci...

journal_title：Current topics in medicinal chemistry

authors： Morimoto S,Jiménez-Trejo F,Cerbón M

更新日期：2011-01-01 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：:The recognition that malfunction of the microtubule (MT) associated protein tau is likely to play a defining role in the onset and/or progression of a number of neurodegenerative diseases, including Alzheimer's disease, has resulted in the initiation of drug discovery programs that target this protein. Tau is an endog...

journal_title：Current topics in medicinal chemistry

authors： Ballatore C,Brunden KR,Trojanowski JQ,Lee VM,Smith AB 3rd,Huryn DM

更新日期：2011-01-01 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：: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：: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：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：:Prenatal alcohol (ethanol) exposure (PAE) is the underlying cause for a variety of birth defects and neurodevelopmental deficits referred to as "Fetal Alcohol Spectrum Disorders (FASD)". The more visible phenotypes caused by PAE include growth retardation, and characteristic craniofacial abnormalities associated with ...

journal_title：Current topics in medicinal chemistry

authors： Liyanage VR,Curtis K,Zachariah RM,Chudley AE,Rastegar M

更新日期：2017-01-01 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：: ...

journal_title：Current topics in medicinal chemistry

authors： Nayarisseri A,Hood EA

更新日期：2018-01-01 00:00:00

abstract：:Despite the tremendous progress in the field of drug designing, discovering a new drug molecule is still a challenging task. Drug discovery and development is a costly, time consuming and complex process that requires millions of dollar and 10-15 years to bring new drug molecules in the market. This huge investment an...

journal_title：Current topics in medicinal chemistry

authors： Singla D,Dhanda SK,Chauhan JS,Bhardwaj A,Brahmachari SK,Open Source Drug Discovery Consortium.,Raghava GP

更新日期：2013-01-01 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：: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：:Compared with the increasing and widespread bacterial resistance to clinical medicines and the urgent need for cures of intractable diseases, there is a dramatic decline in the numbers of drugs reaching the market or clinical trials. Accordingly, it has become imperative to discover more rational and efficient strateg...

journal_title：Current topics in medicinal chemistry

authors： Wang T,Wu MB,Zhang RH,Chen ZJ,Hua C,Lin JP,Yang LR

更新日期：2016-01-01 00:00:00

abstract：:The emergence of multi-resistant bacteria to drugs is recognized as a major cause of the increasing number of deaths in hospitals. Killing these bacteria require multiple expensive drugs that can have side effects. Metal nanoparticles may provide a new strategy to combat them. Due the antimicrobial and antiviral prope...

journal_title：Current topics in medicinal chemistry

authors： Oktar FN,Yetmez M,Ficai D,Ficai A,Dumitru F,Pica A

更新日期：2015-01-01 00:00:00

abstract：:Safety and biocompatibility assessment of biomaterials are themes of constant concern as advanced materials enter the market as well as products manufactured by new techniques emerge. Within this context, this review provides an up-to-date approach on current methods for the characterization and safety assessment of b...

journal_title：Current topics in medicinal chemistry

authors： Oliveira JPR,Melendez-Ortiz HI,Bucio E,Alves PT,Lima MIS,Goulart LR,Mathor MB,Varca GHC,Lugao AB

更新日期：2018-01-01 00:00:00

abstract：:There are several significant setbacks including limited bioavailability, high clearance, and further current therapies require higher and frequent dosing to gain desired therapeutic effects. Nanomedicines have been widely investigated for rheumatoid arthritis (RA). Though, higher doses also increase the incidence of ...

journal_title：Current topics in medicinal chemistry

authors： Rahman M,Sharma G,Thakur K,Anwar F,Katare OP,Goni VG,Kumar V,Zamzami MA,Akhter S

更新日期：2017-01-01 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：: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：:Biomarkers in the clinical oncology field can have tremendous therapeutic impact especially if the marker is detected before clinical symptoms. This impact can be extended to the evaluation of clinical oncology treatments allowing evaluation of potential compounds to determine their efficacy in the disease treatment. ...

journal_title：Current topics in medicinal chemistry

authors： Belkowski SM,Polkovitch D,D'Andrea MR

更新日期：2005-01-01 00:00:00

abstract：:In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard t...

journal_title：Current topics in medicinal chemistry

authors： Johnson L,Goping IS,Rieger A,Mane JY,Huzil T,Banerjee A,Luduena R,Hassani B,Winter P,Tuszynski JA

更新日期：2017-01-01 00:00:00

abstract：:Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in clinical development is reviewed. The review is organized around three main decision points used in discovery including hit generation, lead optimization and final can...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Tang W,Dasgupta M,Hasting B

更新日期：2009-01-01 00:00:00

abstract：:Diabetes mellitus type 2 (DMT2) is a metabolic disease characterized by a chronic increase in glycemia that promotes several long-term complications and high mortality. Some enzymes involved in glycaemic control, such as α -(1,4)-glucosidase, have now been established as novel pharmacological targets. Coumarins have s...

journal_title：Current topics in medicinal chemistry

authors： Figueroa-Benavides C,Matos MJ,Peñaloza-Amion M,Veas R,Valenzuela-Barra G,Zapata G,Delogu G,Uriarte E,Santana L,Olea-Azar C,Delporte C

更新日期：2018-01-01 00:00:00

abstract：:The increase of pathogens being resistant to antibiotics represents a global health problem and therefore it is a pressing need to develop antibiotics with novel mechanisms of action. Host defense peptides, which have direct antimicrobial activity (also termed antimicrobial peptides) or immune modulating activity, are...

journal_title：Current topics in medicinal chemistry

authors： Lohner K

更新日期：2017-01-01 00:00:00

abstract：:Cyclic peptide scaffolds are key components of signal transduction pathways in both prokaryotic and eukaryotic organisms since they act as chemical messengers that activate or inhibit specific cognate receptors. In prokaryotic organisms these peptides are utilized in non-essential pathways, such as quorum sensing, tha...

journal_title：Current topics in medicinal chemistry

authors： Mull RW,Harrington A,Sanchez LA,Tal-Gan Y

更新日期：2018-01-01 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：:The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

journal_title：Current topics in medicinal chemistry

authors： Aiello F,Valacchi G

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：:Telomeres are structurally nucleoprotein complexes at termini of linear chromosomes and essential to chromosome stability/integrity. In normal human cells, telomere length erodes progressively with each round of cell divisions, which serves as an important barrier to uncontrolled proliferation and malignant transforma...

journal_title：Current topics in medicinal chemistry

authors： Yuan X,Dai M,Xu D

更新日期：2020-01-01 00:00:00

abstract：:Alzheimer's Disease (AD) once considered a rare disorder emerges as a major health concern in recent times. The disease pathogenesis is very complex and yet to be understood completely. However, "Amyloid Cascade" is the central event in disease pathogenesis. Several proteins of the amyloid cascade are currently being ...

journal_title：Current topics in medicinal chemistry

authors： Chakraborty S

更新日期：2017-01-01 00:00:00