About: A conjugated mTOR/MEK bifunctional inhibitor as potential polypharmacological anticancer agent: the prototype compound discovery

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About: A conjugated mTOR/MEK bifunctional inhibitor as potential polypharmacological anticancer agent: the prototype compound discovery Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	A conjugated mTOR/MEK bifunctional inhibitor as potential polypharmacological anticancer agent: the prototype compound discovery
Creator	Wang, Yong Wang, Hao Li, Jiaming Fang, • Liang, Jingtai Tao, Qiangqiang Zhao, Can Ma, •
Source	PMC
abstract	mTOR/MEK bifunctional inhibitors have the potential to surmount the drug resistance aroused from cross talk between PI3K/Akt/mTOR (PAM) and Ras/MEK/ERK pathways. Herein, we report the discovery of a conjugated dual-targeted molecule, compound 13, as the prototype mTOR/MEK bifunctional inhibitor. It exhibited moderately high inhibitory activity against mTOR and MEK1 with IC(50) values of 0.19 μM and 0.98 μM, respectively. In particular, it displayed attractive antiproliferative activity against both A549 (GI(50) = 4.66 μM) and HCT116 (GI(50) = 5.47 μM) cell lines. To our knowledge, it has been the first example of a conjugated mTOR/MEK bifunctional inhibitor. In addition, from this proof-of-principle study, it has become evident that the single-agent dual inhibition of mTOR and MEK can be fulfilled via covalently attaching mTOR kinase inhibitor to an allosteric MEK inhibitor.
has issue date	2020-01-13(xsd:dateTime)
bibo:doi	10.1007/s00044-020-02502-x
bibo:pmid	32435126
has license	no-cc
sha1sum (hex)	158744582ca0180d74abd118da02c40281b0e117
schema:url	https://doi.org/10.1007/s00044-020-02502-x
resource representing a document's title	A conjugated mTOR/MEK bifunctional inhibitor as potential polypharmacological anticancer agent: the prototype compound discovery
has PubMed Central identifier	PMC7223898
has PubMed identifier	32435126
schema:publication	Med Chem Res
resource representing a document's body	covid:158744582ca0180d74abd118da02c40281b0e117#body_text
is schema:about of	named entity 'bifunctional' covid:arg/158744582ca0180d74abd118da02c40281b0e117 named entity 'MEK' named entity 'PAM' named entity 'antiproliferative' named entity 'inhibitor' named entity 'activity' named entity 'study' named entity 'dual' named entity 'bifunctional' named entity 'MEK1' named entity 'bifunctional' named entity 'ERK' named entity 'discovery' named entity 'PAM' named entity '0.98' named entity 'molecule' named entity 'MEK/ERK' named entity 'inhibitory activity' named entity 'conjugated' named entity 'N 2' named entity 'sulfonyl chloride' named entity 'mmol' named entity 'allosteric' named entity 'tetrahydrofuran' named entity 'kinase' named entity 'PDB' named entity 'mmol' named entity 'MEK1' named entity 'substrate' named entity 'mTOR' named entity 'micromolar' named entity 'H-bond' named entity 'clinicaltrials.gov' named entity 'hydroxyl' named entity 'etiology' named entity 'MEK1' named entity 'structure-activity relationships' named entity 'mTOR' named entity 'inhibitory activity' named entity 'MEK1' named entity 'conjugated' named entity 'MEK inhibitors' named entity 'N 2' named entity 'piperazine' named entity '4E-BP1' named entity 'rhabdomyosarcoma' named entity 'monotherapy' named entity 'sulfonyl chloride' named entity '7.5' named entity 'mTOR' named entity 'mTOR' named entity '10.0' named entity 'MEK inhibitor' named entity 'MeOH' named entity 'molecular docking' named entity 'HCT116' named entity 'xenograft models' named entity 'methyl' named entity 'substrate' named entity 'ablating' named entity 'Molecular docking' named entity 'flash column chromatography' named entity '3.11' named entity 'feedback loop' named entity 'm/z' named entity 'MEK inhibitor' named entity 'cell lines' named entity 'antibody' named entity 'inhibitory activity' named entity 'MXD' named entity 'reagent' named entity 'tert-butyl' named entity '1-hydroxybenzotriazole'

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