Recent development in acetyl-CoA carboxylase inhibitors and their potential as novel drugs.


:Acetyl-CoA carboxylase (ACC), a critical enzyme in the regulation of fatty acid synthesis and metabolism, has emerged as an attractive target for a plethora of emerging diseases, such as diabetes mellitus, nonalcoholic fatty liver disease, cancer, bacterial infections and so on. With decades of efforts in medicinal chemistry, significant progress has been made toward the design and discovery of a considerable number of inhibitors of this enzyme. In this review, we not only clarify the role of ACC in emerging diseases, but also summarize recent developments of potent ACC inhibitors and discuss their molecular mechanisms of action and potentials as novel drugs as well as future perspectives toward the design and discovery of novel ACC inhibitors.


Future Med Chem


Wu X,Huang T




Has Abstract


2020-03-01 00:00:00












  • N3-substituted thymidine bioconjugates for cancer therapy and imaging.

    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

    pub_type: 杂志文章,评审


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

    更新日期:2013-04-01 00:00:00

  • Chromenes: potential new chemotherapeutic agents for cancer.

    abstract::Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Patil SA,Patil R,Pfeffer LM,Miller DD

    更新日期:2013-09-01 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


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

    更新日期:2019-05-01 00:00:00

  • 5-azacytosine compounds in medicinal chemistry: current stage and future perspectives.

    abstract::This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA app...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Krečmerová M,Otmar M

    更新日期:2012-05-01 00:00:00

  • Discovery of novel dual acetylcholinesterase inhibitors with antifibrillogenic activity related to Alzheimer's disease.

    abstract:AIM:Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the acceler...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: de Almeida JR,Figueiro M,Almeida WP,de Paula da Silva CHT

    更新日期:2018-05-01 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


    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

  • The essential roles of chemistry in high-throughput screening triage.

    abstract::It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage suffers from a lack of scientists trained in the art and science of early drug discovery chemistry. Many recent publications report the discovery of compounds by screening that are most likely artifacts or promiscuous bioacti...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Dahlin JL,Walters MA

    更新日期:2014-07-01 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


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

    更新日期:2018-12-06 00:00:00

  • Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase.

    abstract::Despite the wealth of information available for the reverse transcriptase (RT)-associated ribonuclease H (RNaseH) domain of lentiviruses, gammaretroviruses and long terminal repeat containing retrotransposons, exploiting this information in the form of an RNaseH inhibitor with high specificity and low cellular toxicit...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Corona A,Masaoka T,Tocco G,Tramontano E,Le Grice SF

    更新日期:2013-12-01 00:00:00

  • Microwave synthesis of cucurbit[n]urils.

    abstract:BACKGROUND:Cucurbit[n]urils (CB[n]; n = 5, 6, 7, 8 or 10) are a family of macrocycles made from the acid-catalyzed condensation of glycoluril and formaldehyde. RESULTS:The synthesis of CB[n] using microwave radiation has been examined and the effect of acid type, reaction time and temperature on the distribution of pr...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Wheate NJ,Patel N,Sutcliffe OB

    更新日期:2010-02-01 00:00:00

  • Butterfly structure: a scaffold of therapeutic importance.

    abstract::Graphical abstract [Formula: see text]. ...

    journal_title:Future medicinal chemistry

    pub_type: 社论


    authors: Choudhary S,Silakari O

    更新日期:2020-02-01 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


    authors: Hughes AD,Jones LH

    更新日期:2011-10-01 00:00:00

  • Novel neuraminidase inhibitors: identification, biological evaluation and investigations of the binding mode.

    abstract:BACKGROUND:The pathogenicity of influenza A and B viruses depends on the function of influenza neuraminidase (NA). Emerging resistant influenza A viruses of subtype H1N1 increasingly challenge the effectiveness of established NA inhibitors. Recent computational studies have indicated several weak points of NA that can ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Kirchmair J,Rollinger JM,Liedl KR,Seidel N,Krumbholz A,Schmidtke M

    更新日期:2011-03-01 00:00:00

  • Antimicrobial, anti-TB, anticancer and anti-HIV evaluation of new s-triazine-based heterocycles.

    abstract:BACKGROUND:The acquirement of resistance by microorganisms to the antimicrobial arsenal is a threat to public health. A recent WHO report estimated that 1.3 million HIV-negative people and 0.38 million HIV-positive people died from TB in 2009. Various forms of cancer account for a high percentage of deaths in both wome...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Patel RV,Kumari P,Rajani DP,Pannecouque C,De Clercq E,Chikhalia KH

    更新日期:2012-06-01 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


    authors: García-Sosa AT

    更新日期:2019-09-01 00:00:00

  • A small cytotoxic peptide from frog elicits potent antitumor immunity to prevent local tumor growth and metastases.

    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

    pub_type: 杂志文章


    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

  • 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


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

    更新日期:2018-03-01 00:00:00

  • Carbonic anhydrase IX inhibitors in cancer therapy: an update.

    abstract::Carbonic anhydrases (CAs; EC are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Supuran CT,Winum JY

    更新日期:2015-01-01 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


    authors: Chiba K,Adachi K

    更新日期:2012-04-01 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


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

    更新日期:2013-03-01 00:00:00

  • Synthesis and biological evaluation of thiophene-based hydroxamate derivatives as HDACis with antitumor activities.

    abstract::Aim:   Histone deacetylases (HDACs) are one of the validated targets for cancer treatments. In our previous work, we designed a series of bis-substituted aromatic amide HDAC inhibitors (HDACis), among which compounds 7 and 8 showed promising anticancer effects. However, the low solubilities prevented their subsequent ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Yang F,Han L,Zhao N,Yang Y,Ge D,Zhang H,Chen Y

    更新日期:2020-04-01 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


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

    更新日期:2014-01-01 00:00:00

  • Discovery of anti-TB agents that target the cell-division protein FtsZ.

    abstract::The emergence of multidrug-resistant Mycobacterium tuberculosis strains has made many of the currently available anti-tuberculosis (TB) drugs ineffective. Accordingly, there is a pressing need to identify new drug targets. Filamentous temperature-sensitive protein Z (FtsZ), a bacterial tubulin homologue, is an essenti...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章,评审


    authors: Kumar K,Awasthi D,Berger WT,Tonge PJ,Slayden RA,Ojima I

    更新日期:2010-08-01 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


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

    更新日期:2018-08-01 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


    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

  • Ask the experts: future of the pharmaceutical industry. Interview by Future Medicinal Chemistry.

    abstract::The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Cottens S,Eaton M,Fuhr J,Geary S,Johnson DS,Li G,Raveglia L,Robertson GM,Westwell A

    更新日期:2011-11-01 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


    authors: Allain C,Faulkner S

    更新日期:2010-03-01 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


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

    更新日期:2016-04-01 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


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

    更新日期:2019-08-01 00:00:00

  • Membrane-targeting antibiotics: recent developments outside the peptide space.

    abstract::The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mech...

    journal_title:Future medicinal chemistry

    pub_type: 杂志文章


    authors: Dias C,Rauter AP

    更新日期:2019-02-25 00:00:00