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

Inhibition mechanism exploration of investigational drug TAK-441 as inhibitor against Vismodegib-resistant Smoothened mutant.

European journal of pharmacology - 15 Jan 2014

Ishii Tsuyoshi, Shimizu Yuji, Nakashima Kosuke, Kondo Shigeru, Ogawa Kazumasa, Sasaki Satoshi, Matsui Hideki

Abstract excerpt

Hedgehog signaling is a driving force in medulloblastoma and basal cell carcinoma (BCC), making it an attractive therapeutic target. Vismodegib recently received FDA approval for the treatment of inoperable BCC, but a drug-resistant Smoothened (Smo) mutant (D473H) was identified in a clinical study. TAK-441 is a pyrrolo[3,2-c]pyridine-4-one derivative that potently inhibits Hh signal transduction and is currently...

Read the complete abstract on PubMed

Topics

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

Share to Anilides
Share to Drugs, Investigational

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Hedgehog Proteins

Share to NIH 3T3 Cells

Share to Pyridines

Share to Pyrroles

Share to Receptors, G-Protein-Coupled

Share to Smoothened Receptor

Source

Identifiers

PMID: 24291104
DOI: 10.1016/j.ejphar.2013.11.014

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

Inhibition mechanism exploration of investigational drug TAK-441 as inhibitor against Vismodegib-resistant Smoothened mutant.PMID 24291104Read ↗

Biochemical characterization of smoothened receptor antagonists by binding kinetics against drug-resistant mutant.Semantic proximity Read ↗

Novel-smoothened inhibitors for therapeutic targeting of naïve and drug-resistant hedgehog pathway-driven cancers.Semantic proximity Read ↗

Smoothened (SMO) receptor mutations dictate resistance to vismodegib in basal cell carcinomaSemantic proximity Read ↗

Targeting the hedgehog pathway to treat basal cell carcinoma.Semantic proximity Read ↗

Hedgehog pathway inhibitors: a patent review (2009 – present)Semantic proximity Read ↗

Analysis of vismodegib resistance in D473G and W535L mutants of SMO receptor and design of novel drug derivatives using molecular dynamics simulations.Semantic proximity Read ↗

Design of Hedgehog pathway inhibitors for cancer treatmentSemantic proximity Read ↗

Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened.Semantic proximity Read ↗

Resistance to SMO Inhibitors in Advanced Basal Cell Carcinoma: A Case Highlighting the Role of Molecular Tumor Profiling.Semantic proximity Read ↗

Smoothened variants explain the majority of drug resistance in basal cell carcinoma.Semantic proximity Read ↗

Small Molecule Inhibitors of the Hedgehog Pathway in the Treatment of Basal Cell Carcinoma of the Skin.Semantic proximity Read ↗

Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation.Semantic proximity Read ↗

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