Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.

Acta pharmacologica Sinica - 1 Nov 2018

Wang Jia, Gong Grace Qun, Zhou Yan, Lee Woo-Jeong, Buchanan Christina Maree, Denny William Alexander, Rewcastle Gordon William, Kendall Jackie Diane, Dickson James Michael Jeremy, Flanagan Jack Urquhart, Shepherd Peter Robin, Yang De-Hua, Wang Ming-Wei

Abstract excerpt

The phosphatidylinositol 3-kinase (PI3K) pathway is involved in many cellular functions including cell growth, metabolism, and transformation. Hyperactivation of this pathway contributes to tumorigenesis, therefore, PI3K is a major target for anticancer drug discovery. Since the PI3Kα isoform is implicated mostly in cancer, we conducted a high-throughput screening (HTS) campaign using a 3-step PI3K homogenous...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to High-Throughput Screening Assays
Share to Hydrogen Bonding

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Isoenzymes

Share to Molecular Docking Simulation

Share to Phosphatidylinositol 3-Kinases

Share to Phosphoinositide-3 Kinase Inhibitors

Share to Protein Binding

Share to Protein Kinase Inhibitors

Source

Open in PubMed Open full text

Identifiers

PMID: 29991713
DOI: 10.1038/s41401-018-0057-z
PMCID: PMC6289374

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.PMID 29991713Read ↗

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.Semantic proximity Read ↗

Phosphatidylinositol 3-kinase (PI3K) inhibitors: a recent update on inhibitor design and clinical trials (2016-2020).Semantic proximity Read ↗

Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.Semantic proximity Read ↗

Structural Insights into the Development of Inhibitors Against Cancer-Specific Mutations of PI3Kα.Semantic proximity Read ↗

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the ClinicSemantic proximity Read ↗

Targeting PI3K family with small-molecule inhibitors in cancer therapy: current clinical status and future directionsSemantic proximity Read ↗

Strategies and techniques for preclinical therapeutic targeting of PI3K in oncology: where do we stand in 2024?Semantic proximity Read ↗

Exploring a kinase inhibitor targeting PI3KCA mutant cancer cells.Semantic proximity Read ↗

PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects.Semantic proximity Read ↗

Identification of a chemical probe for lipid kinase phosphatidylinositol-5-phosphate 4-kinase gamma (PI5P4Kγ)Semantic proximity Read ↗

Somatic mutations in PI3Kα: Structural basis for enzyme activation and drug designSemantic proximity Read ↗

In vitro multifaceted activities of a specific group of novel phosphatidylinositol 3-kinase inhibitors on hotspot mutant PIK3CA.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.