Novel RNA polymerase inhibitor found in soil extracts provides hope for future antibacterial drugs.

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 awards, including the Searle Scholar Award, the Walter J Johnson Prize, the Schering-Plough Award of the American Society for Biochemistry and Molecular Biology, the Waksman Award of the Theobold Smith Society, the MERIT Award of the National Institutes of Health, and membership in the American Academy of Arts and Science. He has more than 130 publications in peer-reviewed journals and more than 30 issued and pending patents.

journal_name

Future Med Chem

authors

Ebright RH

doi

10.4155/fmc-2017-0188

subject

Has Abstract

pub_date

2017-10-01 00:00:00

pages

1857-1861

issue

16

eissn

1756-8919

issn

1756-8927

journal_volume

9

pub_type

面试
  • Getting a handle on chemical probes of chomatin readers.

    abstract::The dynamic nature of histone post-translational modifications such as methylation or acetylation makes possible the alteration of disease associated epigenetic states through the manipulation of the associated epigenetic machinery. One approach is through small molecule perturbation. Chemical probes of epigenetic rea...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2019-0274

    authors: Waybright JM,James LI

    更新日期:2020-01-10 00:00:00

  • Prodrugs in combination with nanocarriers as a strategy for promoting antitumoral efficiency.

    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

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2018-0388

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

    更新日期:2019-08-01 00:00:00

  • Pseudomonas aeruginosa: targeting cell-wall metabolism for new antibacterial discovery and development.

    abstract::Pseudomonas aeruginosa is a leading cause of hospital-acquired infections and is resistant to most antibiotics. With therapeutic options against P. aeruginosa dwindling, and the lack of new antibiotics in advanced developmental stages, strategies for preserving the effectiveness of current antibiotics are urgently req...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2016-0017

    authors: Lamers RP,Burrows LL

    更新日期:2016-06-01 00:00:00

  • The search for a common structural moiety among selected pharmacological correctors of the mutant CFTR chloride channel.

    abstract:BACKGROUND:The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane and is responsible of a severe form of cystic fibrosis. Trafficking can be improved by small organic molecules called 'correctors'. MATERIALS & METHODS:By different synthetic ways, we prepared 4-chloroanisole ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.14.118

    authors: Nieddu E,Pollarolo B,Mazzei MT,Anzaldi M,Schenone S,Pedemonte N,Pesce E,Galietta LJ,Mazzei M

    更新日期:2014-01-01 00:00:00

  • Nanocapsules of platinum anticancer drugs: development towards therapeutic use.

    abstract::Platinum-based anticancer agents have been widely used in the clinic to successfully treat many different types of cancer. However, the therapeutic efficacy of platinum drugs is limited by serious side effects and the occurrence of inherent or acquired resistance of tumor cells. Nanoparticulate drug-delivery systems h...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.09.112

    authors: Bryde S,de Kroon AI

    更新日期:2009-11-01 00:00:00

  • Making way for suppressing the FGF19/FGFR4 axis in cancer.

    abstract::FGF19 is a noncanonical FGF ligand that can control a broad spectrum of physiological responses, which include bile acid homeostasis, liver metabolism and glucose uptake. Many of these responses are mediated by FGF19 binding to its FGFR4/β-klotho receptor complex and controlling activation of an array of intracellular...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2018-0099

    authors: Prieto-Dominguez N,Shull AY,Teng Y

    更新日期:2018-10-01 00:00:00

  • Enhancing anticancer activity through the combination of bioreducing agents and triterpenes.

    abstract:AIM:Triterpenes are natural compounds, whose wide biological activity predestines them for application as promising new chemotherapeutics. In this paper, we report the results of our investigations into the substitution of oleanolic acid with aromatic and nitroaromatic moieties acting as bioreducing agents. RESULTS:Th...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0154

    authors: Bednarczyk-Cwynar B,Ruszkowski P,Jarosz T,Krukiewicz K

    更新日期:2018-03-01 00:00:00

  • Synthesis of quinoline derivatives as potential cysteine protease inhibitors.

    abstract::Aim: Cysteine proteases are important molecular targets involved in the replication, virulence and survival of parasitic organisms, including Trypanosoma and Leishmania species. Methodology & results: Analogs of the 7-chloro-N-[3-(morpholin-4-yl)propyl]quinolin-4-amine were synthesized and their inhibitory activity ag...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2019-0201

    authors: Andrade MM,Martins LC,Marques GV,Silva CA,Faria G,Caldas S,Dos Santos JS,Leclercq SY,Maltarollo VG,Ferreira RS,Oliveira RB

    更新日期:2020-04-01 00:00:00

  • Recent advance of the hepatitis B virus inhibitors: a medicinal chemistry overview.

    abstract::Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.15.19

    authors: Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

    更新日期:2015-01-01 00:00:00

  • A comprehensive look of poly(ADP-ribose) polymerase inhibition strategies and future directions for cancer therapy.

    abstract::The finding of promising drugs represents a huge challenge in cancer therapeutics, therefore it is important to seek out novel approaches and elucidate essential cellular processes in order to identify potential drug targets. Studies on DNA repair pathway suggested that an enzyme, PARP, which plays a significant role ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2016-0113

    authors: Kumar C,Rani N,Velan Lakshmi PT,Arunachalam A

    更新日期:2017-01-01 00:00:00

  • Fluorinated MRI contrast agents and their versatile applications in the biomedical field.

    abstract::MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2018-0463

    authors: Hequet E,Henoumont C,Muller RN,Laurent S

    更新日期:2019-05-01 00:00:00

  • The specific role of O6-methylguanine-DNA methyltransferase inhibitors in cancer chemotherapy.

    abstract::The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2018-0069

    authors: Sun G,Zhao L,Zhong R,Peng Y

    更新日期:2018-08-01 00:00:00

  • Multitarget strategies in Alzheimer's disease: benefits and challenges on the road to therapeutics.

    abstract::Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2016-0003

    authors: Rosini M,Simoni E,Caporaso R,Minarini A

    更新日期:2016-04-01 00:00:00

  • New preparation and synthetic reactions of 3,3,3-trifluoropropynyllithium, -borate and -stannane: facile synthesis of trifluoromethylated allenes, arylacetylenes and enynes.

    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

    pub_type: 杂志文章

    doi:10.4155/fmc.09.69

    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

  • The nitroimidazooxazines (PA-824 and analogs): structure-activity relationship and mechanistic studies.

    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

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.10.207

    authors: Denny WA,Palmer BD

    更新日期:2010-08-01 00:00:00

  • Screening and evaluation of antioxidant activity of some 1,2,4-triazolo[1,5-a]quinazoline derivatives.

    abstract:AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0224

    authors: Al-Salahi R,Anouar EH,Marzouk M,Taie HA,Abuelizz HA

    更新日期:2018-02-01 00:00:00

  • Nonhuman targets in allergic lung conditions.

    abstract::Existing therapies for allergic asthma are far from perfect: the global prevalence of disease increases despite them and they are poorly effective in dealing with the exacerbations that account for hospitalization and asthma deaths. Commercially, there are pressures on these existing medicines too--a growing threat fr...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.12.204

    authors: Robinson C,Zhang J,Newton GK,Perrior TR

    更新日期:2013-02-01 00:00:00

  • Design, synthesis and biological evaluation of chromenopyrimidines as potential cytotoxic agents.

    abstract:AIM:The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS:Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhib...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0324

    authors: El-Bakhshawangy NM,El-Nassan HB,Kassab AE,Taher AT

    更新日期:2018-06-01 00:00:00

  • Anti-inflammatory indomethacin analogs endowed with preferential COX-2 inhibitory activity.

    abstract:AIM:The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. RESULTS:Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both the...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2018-0224

    authors: Amin NH,El-Saadi MT,Hefny AA,Abdelazeem AH,Elshemy HA,Abdellatif KR

    更新日期:2018-12-06 00:00:00

  • Antimalarial aminothiazoles and aminopyridines from phenotypic whole-cell screening of a SoftFocus(®) library.

    abstract::The current state of antimalarial drug resistance emphasizes the need for new therapies with novel modes of action that will add a significant benefit compared with current standards. In this regard, high throughput phenotypic whole-cell screening aids the discovery of novel antiplasmodial scaffolds that are inherentl...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.12.176

    authors: Paquet T,Gordon R,Waterson D,Witty MJ,Chibale K

    更新日期:2012-12-01 00:00:00

  • Purine homo-N-nucleoside+coumarin hybrids as pleiotropic agents for the potential treatment of Alzheimer's disease.

    abstract:AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.14.158

    authors: Kallitsakis MG,Yañez M,Soriano E,Marco-Contelles J,Hadjipavlou-Litina DJ,Litinas KE

    更新日期:2015-01-01 00:00:00

  • Design, synthesis, heme binding and density functional theory studies of isoindoline-dione-4-aminoquinolines as potential antiplasmodials.

    abstract::Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% of deaths affecting the African region. Results/methodology: Microwave promoted the synthesis of cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmod...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2019-0260

    authors: Rani A,Kumar S,Legac J,Adeniyi AA,Awolade P,Singh P,Rosenthal PJ,Kumar V

    更新日期:2020-02-01 00:00:00

  • Practical applications of matched series analysis: SAR transfer, binding mode suggestion and data point validation.

    abstract:AIM:The assumption in scaffold hopping is that changing the scaffold does not change the binding mode and the same structure-activity relationships (SARs) are seen for substituents decorating each scaffold. Results/methodology: We present the use of matched series analysis, an extension of matched molecular pair analys...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2016-0203

    authors: Hunt P,Segall M,O'Boyle N,Sayle R

    更新日期:2017-01-01 00:00:00

  • DYRK1A inhibition as potential treatment for Alzheimer's disease.

    abstract::In total, 47,500,000 people worldwide are affected by dementia and this number is estimated to double by 2030 and triple within 2050 resulting in a huge burden on public health. Alzheimer's disease (AD), a progressive neurodegenerative disorder, is the most common cause of dementia, accounting for 60-70% of all the ca...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2016-0013

    authors: Stotani S,Giordanetto F,Medda F

    更新日期:2016-04-01 00:00:00

  • Overview of computational methods employed in early-stage drug discovery.

    abstract:BACKGROUND:The understanding of biomolecular interactions ultimately depends on knowledge about the structural and dynamic details of the interacting system. Rational structure-based drug design implements computational methodology in this rationale. DISCUSSION:Together with increasing throughput of structural biology...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.09.7

    authors: Skjevik AA,Teigen K,Martinez A

    更新日期:2009-04-01 00:00:00

  • Comparison of structures and cytotoxicity of mupirocin and batumin against melanoma and several other cancer cell lines.

    abstract::Aim: To determine the computer-predicted anticancer activity of mupirocin and to compare its activities with those determined for another polyene antibiotic, batumin. Materials & methods: Molecular docking, cytotoxicity assays, cell microscopy and cell cycle progression were studied in cancer and nontumorigenic cell l...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2018-0333

    authors: Reva ON,Rademan S,Visagie MH,Lebelo MT,Gwangwa MV,Klochko VV,Joubert AM,Lall N

    更新日期:2019-04-01 00:00:00

  • 'Energy expenditure genes' or 'energy absorption genes': a new target for the treatment of obesity and Type II diabetes.

    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

    pub_type: 杂志文章

    doi:10.4155/fmc.10.263

    authors: Braud S,Ciufolini M,Harosh I

    更新日期:2010-12-01 00:00:00

  • Recent advances and new perspectives in targeting CFTR for therapy of cystic fibrosis and enterotoxin-induced secretory diarrheas.

    abstract::The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.12.1

    authors: Zhang W,Fujii N,Naren AP

    更新日期:2012-03-01 00:00:00

  • Dual-pharmacology muscarinic antagonist and β₂ agonist molecules for the treatment of chronic obstructive pulmonary disease.

    abstract::Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the world today. Bronchodilators, particularly muscarinic antagonists and β(2) agonists, are recommended for patients with moderate to severe COPD. Dual-pharmacology muscarinic antagonist- β(2) agonist (MABA) molecules present an exc...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.11.106

    authors: Hughes AD,Jones LH

    更新日期:2011-10-01 00:00:00

  • Azide-alkyne cycloaddition en route to 4-aminoquinoline-ferrocenylchalcone conjugates: synthesis and anti-TB evaluation.

    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

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0098

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

    更新日期:2017-10-01 00:00:00