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

A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance

11 Jul 2024

Abstract excerpt

Despite tremendous progress in precision oncology, adaptive resistance mechanisms limit the long-term effectiveness of molecularly targeted agents. Here we evaluated the pharmacological profile of MTX-531 that was computationally designed to selectively target two key resistance drivers, epidermal growth factor receptor and phosphatidylinositol 3-OH kinase (PI3K). MTX-531 exhibits low-nanomolar potency against...

Read the complete abstract on PubMed

Topics

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

Share to Lung Cancer Treatments and Mutations
Share to Melanoma and MAPK Pathways
Share to PI3K/AKT/mTOR signaling in cancer

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Source

Identifiers

PMID: 38992135
DOI: 10.1038/s43018-024-00781-6

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 8 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistancePMID 38992135Read ↗

Direct K-Ras Inhibitors to Treat Cancers: Progress, New Insights, and Approaches to Treat Resistance.Semantic proximity Read ↗

Mechanisms of Resistance to PI3K Inhibitors in Cancer: Adaptive Responses, Drug Tolerance and Cellular PlasticitySemantic proximity Read ↗

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

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

RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.Semantic proximity Read ↗

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.Semantic proximity Read ↗

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

Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 InhibitorSemantic proximity Read ↗

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

A Pan-RAS Inhibitor with a Unique Mechanism of Action Blocks Tumor Growth and Induces Antitumor Immunity in Gastrointestinal CancerSemantic proximity Read ↗

Rational Design of Potent and Orally Efficacious PI3Kα/δ Degrader for PIK3CA Mutant Breast Cancer without Hyperglycemic Liability.Semantic proximity Read ↗

The phosphoinositide 3-kinase pathway and therapy resistance in cancerSemantic proximity Read ↗

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