Literature DB >> 24834807

Synthesis of a FTO inhibitor with anticonvulsant activity.

Guanqun Zheng1, Thomas Cox, Leah Tribbey, Gloria Z Wang, Paulina Iacoban, Matthew E Booher, Gregory J Gabriel, Lu Zhou, Nancy Bae, Joie Rowles, Chuan He, Mark J Olsen.   

Abstract

We describe the rationale for and the synthesis of a new class of compounds utilizing a modular approach that are designed to mimic ascorbic acid and to inhibit 2-oxoglutarate-dependent hydroxylases. Preliminary characterization of one of these compounds indicates in vivo anticonvulsant activity (6 Hz mouse model) at nontoxic doses, inhibition of the 2-oxoglutarate-dependent hydroxylase FTO, and expected increase in cellular N(6)-methyladenosine. This compound is also able to modulate various microRNA, an interesting result in light of the recent view that modulation of microRNAs may be useful for the treatment of CNS disease.

Entities:  

Mesh:

Substances:

Year:  2014        PMID: 24834807      PMCID: PMC4140589          DOI: 10.1021/cn500042t

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN: 1948-7193            Impact factor:   4.418


  42 in total

1.  Inflammatory changes during epileptogenesis and spontaneous seizures in a mouse model of mesiotemporal lobe epilepsy.

Authors:  Fabien Pernot; Christophe Heinrich; Laure Barbier; André Peinnequin; Pierre Carpentier; Franck Dhote; Valérie Baille; Claire Beaup; Antoine Depaulis; Frédéric Dorandeu
Journal:  Epilepsia       Date:  2011-09-28       Impact factor: 5.864

2.  Inverse association of the obesity predisposing FTO rs9939609 genotype with alcohol consumption and risk for alcohol dependence.

Authors:  Agnieszka Sobczyk-Kopciol; Grazyna Broda; Marcin Wojnar; Pawel Kurjata; Andrzej Jakubczyk; Anna Klimkiewicz; Rafal Ploski
Journal:  Addiction       Date:  2010-12-23       Impact factor: 6.526

Review 3.  Hypoxia inducible factor prolyl 4-hydroxylase enzymes: center stage in the battle against hypoxia, metabolic compromise and oxidative stress.

Authors:  Ambreena Siddiq; Leila R Aminova; Rajiv R Ratan
Journal:  Neurochem Res       Date:  2007-03-07       Impact factor: 3.996

4.  Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.

Authors:  A T Hopper; D T Witiak; J Ziemniak
Journal:  J Med Chem       Date:  1998-02-12       Impact factor: 7.446

5.  Comprehensive analysis of mRNA methylation reveals enrichment in 3' UTRs and near stop codons.

Authors:  Kate D Meyer; Yogesh Saletore; Paul Zumbo; Olivier Elemento; Christopher E Mason; Samie R Jaffrey
Journal:  Cell       Date:  2012-05-17       Impact factor: 41.582

Review 6.  Critical review of current animal models of seizures and epilepsy used in the discovery and development of new antiepileptic drugs.

Authors:  Wolfgang Löscher
Journal:  Seizure       Date:  2011-02-02       Impact factor: 3.184

7.  The effects of alpha-tocopherol on hippocampal oxidative stress prior to in pilocarpine-induced seizures.

Authors:  A R Tomé; Dejiang Feng; R M Freitas
Journal:  Neurochem Res       Date:  2009-11-26       Impact factor: 3.996

8.  The fat mass and obesity associated gene (Fto) regulates activity of the dopaminergic midbrain circuitry.

Authors:  Martin E Hess; Simon Hess; Kate D Meyer; Linda A W Verhagen; Linda Koch; Hella S Brönneke; Marcelo O Dietrich; Sabine D Jordan; Yogesh Saletore; Olivier Elemento; Bengt F Belgardt; Thomas Franz; Tamas L Horvath; Ulrich Rüther; Samie R Jaffrey; Peter Kloppenburg; Jens C Brüning
Journal:  Nat Neurosci       Date:  2013-06-30       Impact factor: 24.884

9.  Depression in temporal lobe epilepsy: a review of prevalence, clinical features, and management considerations.

Authors:  C S Garcia
Journal:  Epilepsy Res Treat       Date:  2011-12-01

10.  Topology of the human and mouse m6A RNA methylomes revealed by m6A-seq.

Authors:  Dan Dominissini; Sharon Moshitch-Moshkovitz; Schraga Schwartz; Mali Salmon-Divon; Lior Ungar; Sivan Osenberg; Karen Cesarkas; Jasmine Jacob-Hirsch; Ninette Amariglio; Martin Kupiec; Rotem Sorek; Gideon Rechavi
Journal:  Nature       Date:  2012-04-29       Impact factor: 49.962

View more
  37 in total

Review 1.  Epitranscriptomic regulation by m6A RNA methylation in brain development and diseases.

Authors:  Anil K Chokkalla; Suresh L Mehta; Raghu Vemuganti
Journal:  J Cereb Blood Flow Metab       Date:  2020-09-23       Impact factor: 6.200

2.  Influence of the Ring Size on the Binding Ability of FTO Investigated by Fluorescence Spectroscopy.

Authors:  Wu He; Zhigang Li; Lingling Yang; Qingwei Jiang; Ting Ren; Lijiao Zhang; Zhenhua Shen; Qinghua Yang; Ruiyong Wang; Junbiao Chang
Journal:  J Fluoresc       Date:  2015-09-16       Impact factor: 2.217

Review 3.  Role of N6-methyladenosine modification in cancer.

Authors:  Xiaolan Deng; Rui Su; Xuesong Feng; Minjie Wei; Jianjun Chen
Journal:  Curr Opin Genet Dev       Date:  2017-10-14       Impact factor: 5.578

Review 4.  RNA N6-methyladenosine modification in regulating cancer stem cells and tumor immune microenvironment and its implication for cancer therapy.

Authors:  Subhadra Kumari; Santosh Kumar; Srinivasan Muthuswamy
Journal:  J Cancer Res Clin Oncol       Date:  2022-07-07       Impact factor: 4.553

Review 5.  N6-methyladenosine and Neurological Diseases.

Authors:  Nan Zhang; Chunhong Ding; Yuxin Zuo; Yu Peng; Lielian Zuo
Journal:  Mol Neurobiol       Date:  2022-01-15       Impact factor: 5.590

6.  Novel evidence for m6A methylation regulators as prognostic biomarkers and FTO as a potential therapeutic target in gastric cancer.

Authors:  Tadanobu Shimura; Raju Kandimalla; Yoshinaga Okugawa; Masaki Ohi; Yuji Toiyama; Chuan He; Ajay Goel
Journal:  Br J Cancer       Date:  2021-10-21       Impact factor: 9.075

Review 7.  m6A Modification in Coding and Non-coding RNAs: Roles and Therapeutic Implications in Cancer.

Authors:  Huilin Huang; Hengyou Weng; Jianjun Chen
Journal:  Cancer Cell       Date:  2020-03-16       Impact factor: 31.743

8.  Small-Molecule Inhibitors of the RNA M6A Demethylases FTO Potently Support the Survival of Dopamine Neurons.

Authors:  Simona Selberg; Li-Ying Yu; Olesja Bondarenko; Esko Kankuri; Neinar Seli; Vera Kovaleva; Koit Herodes; Mart Saarma; Mati Karelson
Journal:  Int J Mol Sci       Date:  2021-04-26       Impact factor: 5.923

9.  Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia.

Authors:  Yue Huang; Rui Su; Yue Sheng; Lei Dong; Ze Dong; Hongjiao Xu; Tengfeng Ni; Zijie Scott Zhang; Tao Zhang; Chenying Li; Li Han; Zhenyun Zhu; Fulin Lian; Jiangbo Wei; Qiangqiang Deng; Yungui Wang; Mark Wunderlich; Zhiwei Gao; Guoyu Pan; Dafang Zhong; Hu Zhou; Naixia Zhang; Jianhua Gan; Hualiang Jiang; James C Mulloy; Zhijian Qian; Jianjun Chen; Cai-Guang Yang
Journal:  Cancer Cell       Date:  2019-04-15       Impact factor: 38.585

10.  Targeting FTO Suppresses Cancer Stem Cell Maintenance and Immune Evasion.

Authors:  Rui Su; Lei Dong; Yangchan Li; Min Gao; Li Han; Mark Wunderlich; Xiaolan Deng; Hongzhi Li; Yue Huang; Lei Gao; Chenying Li; Zhicong Zhao; Sean Robinson; Brandon Tan; Ying Qing; Xi Qin; Emily Prince; Jun Xie; Hanjun Qin; Wei Li; Chao Shen; Jie Sun; Prakash Kulkarni; Hengyou Weng; Huilin Huang; Zhenhua Chen; Bin Zhang; Xiwei Wu; Mark J Olsen; Markus Müschen; Guido Marcucci; Ravi Salgia; Ling Li; Amir T Fathi; Zejuan Li; James C Mulloy; Minjie Wei; David Horne; Jianjun Chen
Journal:  Cancer Cell       Date:  2020-06-11       Impact factor: 38.585

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.