Pyrazolo[1,5-a]pyrimidine TRPC6 antagonists for the treatment of gastric cancer

scientific article published on 31 May 2018

Pyrazolo[1,5-a]pyrimidine TRPC6 antagonists for the treatment of gastric cancer is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1016/J.CANLET.2018.05.041
P932PMC publication ID6345172
P698PubMed publication ID29859875

P50authorXuechuan HongQ42863996
P2093author name stringHui Zhou
Michael X Zhu
Hongbo Wang
Yuling Xiao
Guangyao Lv
Qingjun Zhou
Chunhong Yan
Jingwen Zhang
Huai-Rong Luo
Jinbin Tian
Yingmin Zhu
Chunrong Qu
Fuchun Xu
Xiaodong Zeng
Jiacheng Lin
Yungang Lu
Zixing Deng
Mingmin Ding
P2860cites workThe discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophoreQ44355684
Blockade of TRPC6 channels induced G2/M phase arrest and suppressed growth in human gastric cancer cells.Q45926994
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.Q45991914
Critical role of TRPC6 channels in VEGF-mediated angiogenesisQ47942617
Synthesis and Biological Evaluation of N-Heterocyclic Indolyl Glyoxylamides as Orally Active Anticancer AgentsQ53933668
Gastric cancerQ89391950
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffoldQ27675102
Global cancer statistics, 2012Q27860501
Molecular targeted therapy for the treatment of gastric cancerQ28072433
TRPC6 is a glomerular slit diaphragm-associated channel required for normal renal functionQ28594959
TRPC3 and TRPC6 are essential for angiotensin II-induced cardiac hypertrophyQ30478281
Clinical impact of tumour biology in the management of gastroesophageal cancerQ33922534
Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channelsQ33973423
Novel pharmacological TRPC inhibitors block hypoxia-induced vasoconstrictionQ34142319
A mutation in the TRPC6 cation channel causes familial focal segmental glomerulosclerosisQ34416768
Preparation, pharmacokinetics, biodistribution, antitumor efficacy and safety of Lx2-32c-containing liposomeQ34702599
Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channelsQ35595863
Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channelsQ35865421
Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).Q36064085
TRPC6 specifically interacts with APP to inhibit its cleavage by γ-secretase and reduce Aβ production.Q36417516
Deletion of TRPC4 and TRPC6 in mice impairs smooth muscle contraction and intestinal motility in vivo.Q37376306
Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.Q37436085
Enhanced expression of transient receptor potential channels in idiopathic pulmonary arterial hypertensionQ37533998
Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophyQ37543708
Targeting TRPC6 channels in oesophageal carcinoma growth.Q37710561
Vitamin D3 Prevents Calcium-Induced Progression of Early-Stage Prostate Tumors by Counteracting TRPC6 and Calcium Sensing Receptor UpregulationQ38729304
Natural product modulators of transient receptor potential (TRP) channels as potential anti-cancer agentsQ38738962
Design, synthesis, and structure-activity relationship of novel LSD1 inhibitors based on pyrimidine-thiourea hybrids as potent, orally active antitumor agentsQ38917642
Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathwaysQ39302766
Transient receptor potential channel C3 contributes to the progression of human ovarian cancerQ39893829
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 ChannelsQ40250028
Identification and Validation of Larixyl Acetate as a Potent TRPC6 Inhibitor.Q40325030
TRPC6 G757D Loss-of-Function Mutation Associates with FSGS.Q40974180
Long-term spironolactone treatment reduces coronary TRPC expression, vasoconstriction, and atherosclerosis in metabolic syndrome pigs.Q42339342
Chronic hypoxia-induced upregulation of store-operated and receptor-operated Ca2+ channels in pulmonary arterial smooth muscle cells: a novel mechanism of hypoxic pulmonary hypertensionQ42464729
P304page(s)47-55
P577publication date2018-05-31
P1433published inCancer LettersQ326372
P1476titlePyrazolo[1,5-a]pyrimidine TRPC6 antagonists for the treatment of gastric cancer
P478volume432

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cites work (P2860)
Q93165211Analysis of Mrgprb2 Receptor-Evoked Ca 2+ Signaling in Bone Marrow Derived (BMMC) and Peritoneal (PMC) Mast Cells of TRPC-Deficient Mice
Q64901873Novel near-infrared II aggregation-induced emission dots for in vivo bioimaging.
Q89823407PCC0208017, a novel small-molecule inhibitor of MARK3/MARK4, suppresses glioma progression in vitro and in vivo
Q58720903Prediction of key genes and pathways involved in trastuzumab-resistant gastric cancer
Q90395894TRP Channels in Digestive Tract Cancers
Q89468002TRPC channels: Structure, function, regulation and recent advances in small molecular probes

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