'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 genotype' theory, obesity genes may have conferred an evolutionary advantage in times of food shortage through efficient energy exploitation, while 'lean' or 'energy expenditure' genes may have become very rare during the same periods. It is therefore a challenge to identify 'energy expenditure genes' or 'energy absorption genes,' whose mutations or single nucleotide polymorphisms do result in reduced energy intake. We submit that such 'energy absorption' or 'energy expenditure' genes (crucial genes) are potential new targets for the treatment of obesity. These genes can be identified in rare genetic diseases that produce a lean, failure-to-thrive, energy malabsorption or starvation phenotype.

journal_name

Future Med Chem

authors

Braud S,Ciufolini M,Harosh I

doi

10.4155/fmc.10.263

subject

Has Abstract

pub_date

2010-12-01 00:00:00

pages

1777-83

issue

12

eissn

1756-8919

issn

1756-8927

journal_volume

2

pub_type

杂志文章
  • 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 aw...

    journal_title:Future medicinal chemistry

    pub_type: 面试

    doi:10.4155/fmc-2017-0188

    authors: Ebright RH

    更新日期:2017-10-01 00:00:00

  • Anti-inflammatory and antioxidative effects of Camellia oleifera Abel components.

    abstract::Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2017-0109

    authors: Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

    更新日期:2017-11-01 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

  • Dynorphin A analogs for the treatment of chronic neuropathic pain.

    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

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.15.164

    authors: Hall SM,Lee YS,Hruby VJ

    更新日期:2016-01-01 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

  • Collaboration versus outsourcing: the need to think outside the box.

    abstract::As has been widely reviewed elsewhere, the pharmaceutical industry is experiencing an 'innovation deficit' as evidenced by the decline in new chemical entity output. This decline, compounded by increased costs and regulatory requirements highlights the need to significantly revise strategic options across the drug-dis...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.11.160

    authors: Robertson GM,Mayr LM

    更新日期:2011-12-01 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

  • Research progress of selective small molecule bromodomain-containing protein 9 inhibitors.

    abstract::The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential applicati...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2017-0243

    authors: Hui M,Jian Z,Peiyuan Z,Zhenwei W,Huibin Z

    更新日期:2018-04-01 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

  • Design and in vitro evaluation of a novel polymeric excipient for buccal applications.

    abstract:BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.13.33

    authors: Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch A

    更新日期:2013-04-01 00:00:00

  • Linolenic acid-modified MPEG-PEI micelles for encapsulation of amphotericin B.

    abstract::Aim: To encapsulate amphotericin B (AmB) with reduced toxicity and comparable activity. Results & methodology: The α-linolenic acid (ALA)-modified monomethoxy polyethylene glycol-g-PEI-g-ALA conjugate was employed to prepare AmB-loaded micelles (AmB-M). In vitro activity and release behavior of AmB-M were investigated...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2018-0580

    authors: Xu H,Teng F,Zhou F,Zhu L,Wen Y,Feng R,Song Z

    更新日期:2019-10-01 00:00:00

  • Enhancing the pharmacokinetic/pharmacodynamic properties of therapeutic nucleotides using lipid nanoparticle systems.

    abstract::Although activity has been reported in vivo, free nucleic acid-based drugs are rapidly degraded and cleared following systemic administration. To address these challenges and improve the potency and bioavailability of genetic drugs, significant efforts have been made to develop effective delivery systems of which lipi...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.15.108

    authors: Lin PJ,Tam YK

    更新日期:2015-01-01 00:00:00

  • Fatty acid and mineral receptors as drug targets for gastrointestinal disorders.

    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

    pub_type: 杂志文章,评审

    doi:10.4155/fmc-2016-0205

    authors: Pongkorpsakol P,Moonwiriyakit A,Muanprasat C

    更新日期:2017-03-01 00:00:00

  • Surface plasmon resonance--more than a screening technology: insights in the binding mode of σ70:core RNAP inhibitors.

    abstract:AIM:Antibiotic resistance has become a major health problem. The σ(70):core interface of bacterial RNA polymerase is a promising drug target. Recently, the coiled-coil and lid-rudder-system of the β' subunit has been identified as an inhibition hot spot. Materials & methods & Results: By using surface plasmon resonance...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.14.105

    authors: Hüsecken K,Hinsberger S,Elgaher WA,Haupenthal J,Hartmann RW

    更新日期:2014-09-01 00:00:00

  • Chemoinformatic characterization of activity and selectivity switches of antiprotozoal compounds.

    abstract:BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc.13.173

    authors: Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

    更新日期:2014-03-01 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

  • Structure-activity relationship of natural and synthetic coumarin derivatives against Mycobacterium tuberculosis.

    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

    pub_type: 杂志文章

    doi:10.4155/fmc-2018-0281

    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

  • Microvascular complications and diabetic retinopathy: recent advances and future implications.

    abstract::Retinal microvascular alterations have been observed during diabetic retinopathy (DR) due to the retinal susceptibility towards subtle pathological alterations. Therefore, retinal microvascular pathology is essential to understand the nature of retinal degenerations during DR. In this review, the role of retinal micro...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.12.206

    authors: Barot M,Gokulgandhi MR,Patel S,Mitra AK

    更新日期:2013-03-01 00:00:00

  • Photophysical approaches to responsive optical probes.

    abstract::Responsive optical probes play a vital role in following and understanding biological events. In this review, we focus on the use of lanthanide complexes as molecular probes, as they offer many advantages in imaging and assays, particularly when used in time-gated protocols. We describe systems that illustrate the key...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.09.173

    authors: Allain C,Faulkner S

    更新日期:2010-03-01 00:00:00

  • Benford's law in medicinal chemistry: Implications for drug design.

    abstract::Aim: The explosion of data based technology has accelerated pattern mining. However, it is clear that quality and bias of data impacts all machine learning and modeling. Results & methodology: A technique is presented for using the distribution of first significant digits of medicinal chemistry features: logP, logS, a...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2019-0006

    authors: García-Sosa AT

    更新日期:2019-09-01 00:00:00

  • Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model.

    abstract:BACKGROUND:Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acu...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0003

    authors: Trifirò P,Cappa A,Brambillasca S,Botrugno OA,Cera MR,Zuffo RD,Dessanti P,Meroni G,Thaler F,Villa M,Minucci S,Mercurio C,Varasi M,Vianello P

    更新日期:2017-07-01 00:00:00

  • ACAT1/SOAT1 as a therapeutic target for Alzheimer's disease.

    abstract::Alzheimer's disease (AD) is the most common cause of dementia with no cure at present. Cholesterol metabolism is closely associated with AD at several stages. ACAT1 converts free cholesterol to cholesteryl esters, and plays important roles in cellular cholesterol homeostasis. Recent studies show that in a mouse model,...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.15.161

    authors: Shibuya Y,Chang CC,Chang TY

    更新日期:2015-01-01 00:00:00

  • PEGylation and its impact on the design of new protein-based medicines.

    abstract::PEGylation is the covalent conjugation of PEG to therapeutic molecules. Protein PEGylation is a clinically proven approach for extending the circulation half-life and reducing the immunogenicity of protein therapeutics. Most clinically used PEGylated proteins are heterogeneous mixtures of PEG positional isomers conjug...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.14.125

    authors: Ginn C,Khalili H,Lever R,Brocchini S

    更新日期:2014-01-01 00:00:00

  • Tuning heavy metal compounds for anti-tumor activity: is diversity the key to ruthenium's success?

    abstract::This review aims to bring the reader up to date with the more recent ruthenium compounds that have been synthesized and tested for their cytotoxicity. The chemistry of these transition metal complexes will be introduced and the basic principles that govern their common behavior outlined. The recent history of establis...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.09.25

    authors: Page SM,Boss SR,Barker PD

    更新日期:2009-06-01 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

  • PAAP: a web server for predicting antihypertensive activity of peptides.

    abstract:AIM:Hypertension is associated with development of cardiovascular disease and has become a significant health problem worldwide. Naturally-derived antihypertensive peptides have emerged as promising alternatives to synthetic drugs. MATERIALS & METHODS:This study introduces predictor of antihypertensive activity of pep...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2017-0300

    authors: Win TS,Schaduangrat N,Prachayasittikul V,Nantasenamat C,Shoombuatong W

    更新日期:2018-08-01 00:00:00

  • Development and strategies of VEGFR-2/KDR inhibitors.

    abstract::VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. As an essential receptor protein tyrosine kinase propagating cellular signal transduction processes, VEGFR-2 is a central target for drug discovery against tumor-associated angiogenesis. Since the autophosphorylation of VEGFR-2 re...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.12.121

    authors: Huang L,Huang Z,Bai Z,Xie R,Sun L,Lin K

    更新日期:2012-09-01 00:00:00

  • Cyclin-dependent kinase 7 inhibitors in cancer therapy.

    abstract::Cyclin-dependent kinase 7 (CDK7) plays crucial roles in the regulation of cell cycle and transcription that are tightly associated with cancer development and metastasis. The recent identification of the first covalent inhibitor which possesses high specificity against CDK7 prompts intense studies on designing highly ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章

    doi:10.4155/fmc-2019-0334

    authors: Wang M,Wang T,Zhang X,Wu X,Jiang S

    更新日期:2020-05-01 00:00:00

  • Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis.

    abstract::Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor ty...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.12.25

    authors: Chiba K,Adachi K

    更新日期:2012-04-01 00:00:00

  • Drugging the schistosome zinc-dependent HDACs: current progress and future perspectives.

    abstract::Schistosomes, like many eukaryotic pathogens, typically display morphologically distinct stages during their life cycles. Epigenetic mechanisms underlie the pathogens' morphological transformations, and the targeting of epigenetics-driven cellular programs therefore represents an Achilles' heel of parasites. To speed ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.4155/fmc.15.25

    authors: Marek M,Oliveira G,Pierce RJ,Jung M,Sippl W,Romier C

    更新日期:2015-01-01 00:00:00