Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686

Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation

(2022) Hualin Zhang et al.   ACS Medicinal Chemistry Letters

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands

(2022) Hong-Yi Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2021) Xiaojuan Qu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

(2021) Si-Min Qi et al.   Frontiers in Pharmacology

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

(2020) Hao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of selective degraders of EGFRL858R/T790M mutant

(2020) Xin Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

(2020) Xin Li et al.   Journal of Hematology & Oncology

Discovery and biological evaluation of proteolysis targeting chimeras (PROTACs) as an EGFR degraders based on osimertinib and lenalidomide

(2020) Kailun He et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Fundamental Evaluation of Radioiodinated Rociletinib (CO-1686) as a Probe to Lung Cancer with L858R/T790M Mutations of Epidermal Growth Factor Receptor (EGFR)

(2020) Muammar Fawwaz et al.   MOLECULES

Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers

(2020) Chaoguo Cao et al.   JOURNAL OF MEDICINAL CHEMISTRY

The next tier of EGFR resistance mutations in lung cancer

(2020) Hannah L. Tumbrink et al.   ONCOGENE

Discovery of potent small molecule PROTACs targeting mutant EGFR

(2020) Hong-Yi Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

(2020) Shenxin Zeng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PROTACs to address the challenges facing small molecule inhibitors

(2020) Pedro Martín-Acosta et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Second-generation EGFR and ErbB tyrosine kinase inhibitors as first-line treatments for non-small cell lung cancer

(2019) Shouzheng Wang et al.   OncoTargets and Therapy

Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance

(2019) Haikui Yang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mechanisms of acquired resistance to first- and second-generation EGFR tyrosine kinase inhibitors

(2018) D Westover et al.   ANNALS OF ONCOLOGY

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Structural basis of mutant-selectivity and drug-resistance related to CO-1686

(2017) Xiao-E Yan et al.   Oncotarget

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

(2014) D. A. E. Cross et al.   Cancer Discovery

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

MG132, a proteasome inhibitor, induces apoptosis in tumor cells

(2012) Na GUO et al.   Asia-Pacific Journal of Clinical Oncology

EGFR Mutations and Lung Cancer

(2011) Gilda da Cunha Santos et al.   Annual Review of Pathology-Mechanisms of Disease

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA