Structural and functional regulation of lactate dehydrogenase-A in cancer.

abstract：:Class I PI3Ks are composed of four catalytic subunit variants (p110α, p110β, p110δ and p110γ). The PI3K pathway is among the most frequently activated pathways in many diseases, and has emerged as an attractive target for drug development, in particular for the treatment of many human cancers including breast, prostat...

journal_title：Future medicinal chemistry

authors： Jeong Y,Kwon D,Hong S

更新日期：2014-05-01 00:00:00

abstract：:Epigallocatechin gallate (EGCG), one of polyphenols isolated from green tea, exhibits biology-benefiting effects with minimum severe adverse. EGCG is known to be a mitochondrion-targeting medicinal agent, regulating mitochondrial metabolism, including mitochondrial biogenesis, mitochondrial bioenergetics, and mitochon...

journal_title：Future medicinal chemistry

authors： Shi W,Li L,Ding Y,Yang K,Chen Z,Fan X,Jiang S,Guan Y,Liu Z,Xu D,Wu L

更新日期：2018-04-01 00:00:00

abstract：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：:Prodrug entrapment into nanocarriers for tumor delivery is a strategy to achieve a valid therapy with high efficiency. The prodrug contains anticancer agents conjugating with functional moieties or ligands so that the active component is released after metabolism in the body or tumor. The advantages of nanosystems for...

journal_title：Future medicinal chemistry

authors： Lin MH,Hung CF,Hsu CY,Lin ZC,Fang JY

更新日期：2019-08-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND:Since trifluoromethyl-containing compounds have found diverse applications in the fields of pharmaceuticals and agrochemicals, facile and selective synthetic methods for trifluoromethyl-substituted compounds are an essential tool for advanced medicinal chemistry. Now that diverse synthetic transformations of...

journal_title：Future medicinal chemistry

authors： Shimizu M,Higashi M,Takeda Y,Murai M,Jiang G,Asai Y,Nakao Y,Shirakawa E,Hiyama T

更新日期：2009-08-01 00:00:00

abstract：AIM:To synthesize the new bioactive metabolites of mosapride (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxyben-zamide (R-isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxybenzamide (S-isomer) and evaluate their in vitro and in vivo pharmacological and ...

journal_title：Future medicinal chemistry

authors： Yao J,Li K,Song Y,He Z,Liu Z,Zhao L,Wang S

更新日期：2019-01-01 00:00:00

abstract：:Chronic pain is one of the most ubiquitous diseases in the world, but treatment is difficult with conventional methods, due to undesirable side effects of treatments and unknown mechanisms of pathological pain states. The endogenous peptide, dynorphin A has long been established as a target for the treatment of pain. ...

journal_title：Future medicinal chemistry

authors： Hall SM,Lee YS,Hruby VJ

更新日期：2016-01-01 00:00:00

abstract：:Computer-aided drug design (CADD) methodologies have made great advances and contributed significantly to the discovery and/or optimization of many clinically used drugs in recent years. CADD tools have likewise been applied to the discovery of inhibitors of HIV-1 integrase, a difficult and worthwhile target for the d...

journal_title：Future medicinal chemistry

authors： Liao C,Nicklaus MC

更新日期：2010-07-01 00:00:00

abstract：:Systematic investigation of the lipidome will reveal new opportunities for disease diagnosis and intervention. However, lipidomic research has been hampered by the lack of molecular tools to track specific lipids of interest. Accumulating reports indicate lipid recognition can be achieved with properly constructed sho...

journal_title：Future medicinal chemistry

authors： Gao J,Zheng H

更新日期：2013-05-01 00:00:00

abstract：:Several hundred genes associated or linked to obesity have been described in the scientific literature. Whereas many of these genes are potential targets for the treatment of obesity and associated conditions, none of them have permitted the developement of an efficient drug therapy. As proposed by the 'thrifty genoty...

journal_title：Future medicinal chemistry

authors： Braud S,Ciufolini M,Harosh I

更新日期：2010-12-01 00:00:00

abstract：:Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...

journal_title：Future medicinal chemistry

authors： Ebright RH

更新日期：2017-10-01 00:00:00

abstract：:Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca2+-sensing receptors and Zn2+-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review prov...

journal_title：Future medicinal chemistry

authors： Pongkorpsakol P,Moonwiriyakit A,Muanprasat C

更新日期：2017-03-01 00:00:00

abstract：:Aim: To synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities a...

journal_title：Future medicinal chemistry

authors： Tang X,He J,Li Q,Tang X,Chen M,Hao G,Huai Z,Huang Y,Xue W

更新日期：2020-08-01 00:00:00

abstract：:Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicina...

journal_title：Future medicinal chemistry

authors： Murphy KE,Sloan GF,Lawhern GV,Volk GE,Shumate JT,Wolfe AL

更新日期：2020-11-01 00:00:00

abstract：:The compound class of 3-carboranyl thymidine analogues (3CTAs) are boron delivery agents for boron neutron capture therapy (BNCT), a binary treatment modality for cancer. Presumably, these compounds accumulate selectively in tumor cells via intracellular trapping, which is mediated by hTK1. Favorable in vivo biodistri...

journal_title：Future medicinal chemistry

authors： Khalil A,Ishita K,Ali T,Tjarks W

更新日期：2013-04-01 00:00:00

abstract：:Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis acti...

journal_title：Future medicinal chemistry

authors： Pires CT,Scodro RB,Cortez DA,Brenzan MA,Siqueira VL,Caleffi-Ferracioli KR,Vieira LC,Monteiro JL,Corrêa AG,Cardoso RF

更新日期：2020-09-01 00:00:00

abstract：:Aim: Anticancer immunochemotherapy represents an attractive paradigm to improve therapeutic responses and reduce side effects. Results & methodology: Here, we show that a naturally occurring host defense peptide, HN-1 inhibited multiple malignant cells proliferation and tumor growth in a xenografted human breast tumor...

journal_title：Future medicinal chemistry

authors： Qiao X,Yang H,Gao J,Cai S,Shi N,Wang M,Wang Y,Yu H

更新日期：2019-10-01 00:00:00

abstract：:PA-824 is an experimental anti-tubercular agent that has a novel mechanism of action. It is effective against both active and persistent forms of the disease and has recently shown early bactericidal activity in a Phase II clinical trial. This review summarizes recent studies on the mode of action of PA-824 and outlin...

journal_title：Future medicinal chemistry

authors： Denny WA,Palmer BD

更新日期：2010-08-01 00:00:00

abstract：:Aim: The orphan drug auranofin was recently found to exhibit antimicrobial properties. Materials & methods: We explored the efficacy of auranofin by evaluating the minimal inhibitory concentration against a collection of over 500 clinical isolates derived from multiple institutions, inclusive of drug resistant strains...

journal_title：Future medicinal chemistry

authors： Tharmalingam N,Ribeiro NQ,da Silva DL,Naik MT,Cruz LI,Kim W,Shen S,Dos Santos JD,Ezikovich K,D'Agata EM,Mylonakis E,Fuchs BB

更新日期：2019-06-01 00:00:00

abstract：AIM:Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-a...

journal_title：Future medicinal chemistry

authors： Singh A,Viljoen A,Kremer L,Kumar V

更新日期：2017-10-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：:The pharmacokinetic treatment strategy targets the drug molecule itself, aiming to reduce drug concentration at the site of action, thereby minimizing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Phase IIa contro...

journal_title：Future medicinal chemistry

authors： Gorelick DA

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND:Inhibitors of Trypanosoma cruzi with novel mechanisms of action are urgently required to diversify the current clinical and preclinical pipelines. Increasing the number and diversity of hits available for assessment at the beginning of the discovery process will help to achieve this aim. RESULTS:We report t...

journal_title：Future medicinal chemistry

authors： Keenan M,Alexander PW,Chaplin JH,Abbott MJ,Diao H,Wang Z,Best WM,Perez CJ,Cornwall SM,Keatley SK,Thompson RC,Charman SA,White KL,Ryan E,Chen G,Ioset JR,von Geldern TW,Chatelain E

更新日期：2013-10-01 00:00:00

abstract：:Agents that interfere with tubulin function have a broad anti-tumor spectrum and they represent one of the most significant classes of anticancer agents. In the past few years, several small synthetic molecules that have an indole nucleus as a core structure have been identified as tubulin inhibitors. Among these, sev...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Miller DD

更新日期：2012-10-01 00:00:00

abstract：:The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena. However, these advances have not led to improvements in drug-discovery success. Drug programs must find new ways to identify superior compounds. Advances in label-free assay technologies may provide advanta...

journal_title：Future medicinal chemistry

authors： Lunn CA

更新日期：2010-11-01 00:00:00

abstract：:Spinal muscular atrophy (SMA) is an inherited neurodegenerative disease that results in progressive dysfunction of motor neurons of the anterior horn of the spinal cord. SMA is caused by the loss of full-length protein expression from the survival of motor neuron 1 (SMN1) gene. The disease has a unique genetic profile...

journal_title：Future medicinal chemistry

authors： Cherry JJ,Androphy EJ

更新日期：2012-09-01 00:00:00

abstract：:Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...

journal_title：Future medicinal chemistry

authors： Chan CC

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND:4'-seleno-homonucleosides were synthesized as next-generation nucleosides, and their cellular phosphorylation was studied to confirm the hypothesis that bulky selenium atom can sterically hinder the approach of cellular nucleoside kinase to the 5'-OH for phosphorylation. RESULTS:4'-seleno-homonucleosides (n...

journal_title：Future medicinal chemistry

authors： Yu J,Sahu PK,Kim G,Qu S,Choi Y,Song J,Lee SK,Noh M,Park S,Jeong LS

更新日期：2015-01-01 00:00:00

abstract：:Aim: Alzheimer's disease (AD) is known to be themajor cause of dementia among the elderly. The structural properties and binding interactions of the AD drug physostigmine (-)-phy, and its analogues (-)-hex and (-)-phe and (+)-phe, were examined, as well as their impact on the conformational changes of two different AD...

journal_title：Future medicinal chemistry

authors： Adeniyi AA,Conradie J

更新日期：2019-08-01 00:00:00