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 cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.

Bioorganic & medicinal chemistry letters - 1 Aug 2016

Radi Marco, Schneider Ralf, Fallacara Anna Lucia, Botta Lorenzo, Crespan Emmanuele, Tintori Cristina, Maga Giovanni, Kissova Miroslava, Calgani Alessia, Richters André, Musumeci Franesca, Rauh Daniel, Schenone Silvia

Abstract excerpt

The major clinical challenge in drug-resistant chronic myelogenous leukemia (CML) is currently represented by the Bcr-Abl T315I mutant, which is unresponsive to treatment with common first and second generation ATP-competitive tyrosine kinase inhibitors (TKIs). Allosteric inhibition of Bcr-Abl represent a new frontier in the fight against resistant leukemia and few candidates have been identified in the last few...

Read the complete abstract on PubMed

Topics

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

Share to Allosteric Regulation
Share to Cell Death

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cell Survival

Share to Drug Screening Assays, Antitumor

Share to Leukemia, Myelogenous, Chronic, BCR-ABL Positive

Share to Molecular Structure

Share to Neoplasm Proteins

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 27374241
DOI: 10.1016/j.bmcl.2016.06.051

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

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.PMID 27374241Read ↗

Expanding the diversity of allosteric bcr-abl inhibitors.Semantic proximity Read ↗

Insight into the allosteric inhibition of Abl kinase.Semantic proximity Read ↗

The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug.Semantic proximity Read ↗

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.Semantic proximity Read ↗

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Semantic proximity Read ↗

Identification of novel tyrosine kinase inhibitors for drug resistant T315I mutant BCR-ABL: a virtual screening and molecular dynamics simulations study.Semantic proximity Read ↗

Advances in Targeting BCR-ABLT315I Mutation with Imatinib Derivatives and Hybrid Anti-Leukemic Molecules.Semantic proximity Read ↗

The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase.Semantic proximity Read ↗

Recent developments in the third generation inhibitors of Bcr-Abl for overriding T315I mutation.Semantic proximity Read ↗

Virtual Screening and Identification of Non-covalent Reversible Small-molecule BTK Inhibitors from a Library of Known Bioactive CompoundsSemantic proximity Read ↗

Derivates of 1,6-dihyadroazaazulenes as inhibitors of tyrosine kinases BCR-ABL1 wild type and mutant T315I: a molecular dynamics approach.Semantic proximity Read ↗

Identification of common inhibitors of wild-type and T315I mutant of BCR-ABL through the parallel structure-based virtual screening.Semantic proximity Read ↗

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