4.6 Article

HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations

Related references

Note: Only part of the references are listed.
Review Biochemistry & Molecular Biology

Chronicles of EGFR Tyrosine Kinase Inhibitors: Targeting EGFR C797S Containing Triple Mutations

Krishna Babu Duggirala et al.

Summary: EGFR is widely expressed in multiple cancers, with mutations leading to aberrant activation. Current EGFR inhibitors have limited clinical benefits and there is a need for the development of new treatment strategies.

BIOMOLECULES & THERAPEUTICS (2022)

Review Chemistry, Medicinal

The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation

Jie He et al.

Summary: Epidermal growth factor receptor (EGFR) is a crucial target for treating non-small cell lung cancer (NSCLC), with first to third-generation inhibitors showing efficacy but leading to resistance after 9-15 months. Major breakthroughs in understanding the resistance mechanisms of third-generation inhibitors are still lacking. The fourth-generation EGFR-TKIs show promise in overcoming resistance.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Oncology

Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy

Geun Taek Lee et al.

Summary: MTX-23 is a novel PROTAC small molecule that can simultaneously degrade AR-V7 and AR-FL, inhibiting proliferation of CRPC cells resistant to antiandrogen therapy and significantly reducing proliferation and inducing apoptosis in sensitive cells.

MOLECULAR CANCER THERAPEUTICS (2021)

Article Chemistry, Medicinal

Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems

Xiaojuan Qu et al.

Summary: PROTAC technology offers a promising strategy to target EGFR protein and overcome drug resistance in non-small cell lung cancer patients with EGFR mutations. The involvement of autophagy/lysosome system in PROTAC-mediated target protein degradation is demonstrated in this study, providing new insights into cancer treatment.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile

Chaowei Ren et al.

Summary: Proteolysis-targeting chimera (PROTAC) technology in drug discovery has gained much attention, and SIAIS164018, a novel degrader designed from the perspective of clinical benefits, has shown promising results in degrading important oncoproteins, inhibiting cell migration and invasion, and reshuffling kinome ranking compared to its precursor Brigatinib.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

George M. Burslem et al.

Article Chemistry, Medicinal

Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)

Hao Zhang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

Design and synthesis of selective degraders of EGFRL858R/T790M mutant

Xin Zhang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations

Jaebong Jang et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

Article Chemistry, Medicinal

Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects

Yiqing Yang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Oncology

Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer

Alessandro Leonetti et al.

BRITISH JOURNAL OF CANCER (2019)

Article Biotechnology & Applied Microbiology

Targeted protein degradation: expanding the toolbox

Matthieu Schapira et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

Article Biochemistry & Molecular Biology

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation

Alexandru D. Buhimschi et al.

BIOCHEMISTRY (2018)

Article Medicine, General & Internal

Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer

J. -C. Soria et al.

NEW ENGLAND JOURNAL OF MEDICINE (2018)

Editorial Material Chemistry, Medicinal

C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?

Tobias Grabe et al.

ACS MEDICINAL CHEMISTRY LETTERS (2018)

Article Biochemistry & Molecular Biology

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Daniel P. Bondeson et al.

CELL CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M

Kenneth S. Thress et al.

NATURE MEDICINE (2015)

Article Multidisciplinary Sciences

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

Teresa A. Soucy et al.

NATURE (2009)

Article Medicine, General & Internal

Screening for Epidermal Growth Factor Receptor Mutations in Lung Cancer.

Rafael Rosell et al.

NEW ENGLAND JOURNAL OF MEDICINE (2009)

Article Multidisciplinary Sciences

Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation

KM Sakamoto et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)