Recent advances in the development of EGFR degraders: PROTACs and LYTACs

Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues

(2022) Shi Shi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Strategies for designing proteolysis targeting chimaeras (PROTACs)

(2022) Shipeng He et al.   MEDICINAL RESEARCH REVIEWS

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

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 novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy

(2022) Shi Shi et al.   BIOORGANIC CHEMISTRY

Development of Antibody-Based PROTACs for the Degradation of the Cell-Surface Immune Checkpoint Protein PD-L1

(2021) Adam D. Cotton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras

(2021) Xiaoyu Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

LYTACs that engage the asialoglycoprotein receptor for targeted protein degradation

(2021) Green Ahn et al.   Nature Chemical Biology

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research

(2021) Rui-Fang Dong et al.   PHARMACOLOGICAL RESEARCH

Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy

(2021) Chi Zhang et al.   Nature Communications

Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP

(2021) Mengzhu Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras

(2021) Troy A. Bemis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based classification predicts drug response in EGFR-mutant NSCLC

(2021) Jacqulyne P. Robichaux et al.   NATURE

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

(2021) Aleša Bricelj et al.   Frontiers in Chemistry

Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy

(2021) Adileh Ayati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

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

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

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders

(2020) Meng Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Newly Developed Prodrugs and Prodrugs in Development; an Insight of the Recent Years

(2020) Anas Najjar et al.   MOLECULES

Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC

(2020) Iosune Baraibar et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL

(2020) Bingqi Tong et al.   ACS Chemical Biology

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

(2020) Jaebong Jang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

Targeted protein degradation: current and future challenges

(2020) Alexander Hanzl et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

(2020) Tao Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation

(2020) Craig Donoghue et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The next tier of EGFR resistance mutations in lung cancer

(2020) Hannah L. Tumbrink et al.   ONCOGENE

Proteolysis targeting chimera ( PROTAC ) for epidermal growth factor receptor enhances anti‐tumor immunity in non‐small cell lung cancer

(2020) Kai Wang et al.   DRUG DEVELOPMENT RESEARCH

Discovery of potent small molecule PROTACs targeting mutant EGFR

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

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

(2020) Jie He et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Long term follow-up of EGFR mutated NSCLC cases

(2020) Gad Rennert et al.   Translational Oncology

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

(2019) Carl C. Ward et al.   ACS Chemical Biology

Advanced-Stage Non–Small Cell Lung Cancer: Advances in Thoracic Oncology 2018

(2019) Jordi Remon et al.   Journal of Thoracic Oncology

Curcumin overcome primary gefitinib resistance in non-small-cell lung cancer cells through inducing autophagy-related cell death

(2019) Ping Chen et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

ATTEC: a potential new approach to target proteinopathies

(2019) Zhaoyang Li et al.   Autophagy

Natural products as important tyrosine kinase inhibitors

(2019) Bo Yin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Epidermal Growth Factor Receptor Family and its Role in Gastric Cancer

(2019) Chiara Arienti et al.   Frontiers in Oncology

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

(2019) Daiki Takahashi et al.   MOLECULAR CELL

Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045

(2018) Peng Zhao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4- d ]pyrimidine scaffold

(2018) Hao Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of 2,4,6-trisubstitued pyrido[3,4- d ]pyrimidine derivatives as new EGFR-TKIs

(2018) Hao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2018) Jean-Charles Soria et al.   NEW ENGLAND JOURNAL OF MEDICINE

Conformational landscape of the epidermal growth factor receptor kinase reveals a mutant specific allosteric pocket

(2018) Srinivasaraghavan Kannan et al.   Chemical Science

EGFR mutation frequency in Middle East and African non-small cell lung cancer patients: a systematic review and meta-analysis

(2018) Zineb Benbrahim et al.   BMC CANCER

Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

(2018) Jana Fassunke et al.   Nature Communications

Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance

(2017) Harun Patel et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Comprehensive Analysis of EGFR -Mutant Abundance and Its Effect on Efficacy of EGFR TKIs in Advanced NSCLC with EGFR Mutations

(2017) Xuefei Li et al.   Journal of Thoracic Oncology

Epithelial-to-mesenchymal transition correlates with gefitinib resistance in NSCLC cells and the liver X receptor ligand GW3965 reverses gefitinib resistance through inhibition of vimentin

(2017) Yong Hu et al.   OncoTargets and Therapy

Targeting Tyrosine Kinase Inhibitor-Resistant Non-Small Cell Lung Cancer by Inducing Epidermal Growth Factor Receptor Degradation via Methionine 790 Oxidation

(2016) Elaine Lai-Han Leung et al.   ANTIOXIDANTS & REDOX SIGNALING

Not all epidermal growth factor receptor mutations in lung cancer are created equal: Perspectives for individualized treatment strategy

(2016) Yoshihisa Kobayashi et al.   CANCER SCIENCE

Types of Ubiquitin Ligases

(2016) Francesca Ester Morreale et al.   CELL

Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer

(2016) Yoshihisa Kobayashi et al.   MOLECULAR CANCER THERAPEUTICS

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

Structural insights into the catalysis and regulation of E3 ubiquitin ligases

(2016) Lori Buetow et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer

(2015) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the EGFR signaling pathway in cancer therapy

(2012) Parthasarathy Seshacharyulu et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Structural Optimization and Structure–Activity Relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine Derivatives, a New Class of Reversible Kinase Inhibitors Targeting both EGFR-Activating and Resistance Mutations

(2012) Jiao Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Effect of Acquired Cisplatin Resistance on Sensitivity to EGFR Tyrosine Kinase Inhibitors in EGFR Mutant Lung Cancer Cells

(2012) Jin Kyung Rho et al.   ONCOLOGY RESEARCH

Afatinib (BIBW 2992) development in non-small-cell lung cancer

(2011) Vera Hirsh   Future Oncology

Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer

(2009) Michael J. Eck et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Structure-Based View of Epidermal Growth Factor Receptor Regulation

(2008) Kathryn M. Ferguson   Annual Review of Biophysics

Structure and Clinical Relevance of the Epidermal Growth Factor Receptor in Human Cancer

(2008) Amit Kumar et al.   JOURNAL OF CLINICAL ONCOLOGY

Prodrugs: design and clinical applications

(2008) Jarkko Rautio et al.   NATURE REVIEWS DRUG DISCOVERY

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