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

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

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

Design and Synthesis of a Trifunctional Molecular System “Programmed” to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells

(2020) Julie Schmitt et al.   JOURNAL OF MEDICINAL CHEMISTRY

An essential role for Argonaute 2 in EGFR-KRAS signaling in pancreatic cancer development

(2020) Sunita Shankar et al.   Nature Communications

Poly(ADP-ribose)-dependent chromatin unfolding facilitates the association of DNA-binding proteins with DNA at sites of damage

(2019) Rebecca Smith et al.   NUCLEIC ACIDS RESEARCH

Targeted protein degradation: expanding the toolbox

(2019) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

Insights into the biogenesis, function, and regulation of ADP-ribosylation

(2018) Michael S Cohen et al.   Nature Chemical Biology

Epidermal Growth Factor Receptor-Targeting Peptide Nanoparticles Simultaneously Deliver Gemcitabine and Olaparib To Treat Pancreatic Cancer with Breast Cancer 2 (BRCA2) Mutation

(2018) Chong Du et al.   ACS Nano

Gefitinib or Erlotinib vs Chemotherapy for EGFR Mutation-Positive Lung Cancer: Individual Patient Data Meta-Analysis of Overall Survival

(2017) Chee Khoon Lee et al.   JNCI-Journal of the National Cancer Institute

Lung cancer: current therapies and new targeted treatments

(2017) Fred R Hirsch et al.   LANCET

The multifaceted roles of PARP1 in DNA repair and chromatin remodelling

(2017) Arnab Ray Chaudhuri et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Survival of pancreatic cancer cells lacking KRAS function

(2017) Mandar Deepak Muzumdar et al.   Nature Communications

Gefitinib or Erlotinib vs Chemotherapy for EGFR Mutation-Positive Lung Cancer: Individual Patient Data Meta-Analysis of Overall Survival

(2017) Chee Khoon Lee et al.   JNCI-Journal of the National Cancer Institute

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Polypharmacology: Challenges and Opportunities in Drug Discovery

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

EGFR-Activating Mutations Correlate with a Fanconi Anemia-like Cellular Phenotype That Includes PARP Inhibitor Sensitivity

(2013) H. N. Pfaffle et al.   CANCER RESEARCH

Antiproliferative and Proapoptotic Activity of Sunitinib on Endothelial and Anaplastic Thyroid Cancer Cells via Inhibition of Akt and ERK1/2 Phosphorylation and by Down-Regulation of Cyclin-D1

(2013) Teresa Di Desidero et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Dual targeting strategies with bispecific antibodies

(2012) Roland Kontermann   mAbs

Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor

(2012) S Yoshikawa et al.   ONCOGENE

Combination Therapy of Bortezomib with Novel Targeted Agents: An Emerging Treatment Strategy

(2010) J. J. Wright   CLINICAL CANCER RESEARCH

Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled phase 3 study

(2010) Federico Cappuzzo et al.   LANCET ONCOLOGY

Protein-binding assays in biological liquids using microscale thermophoresis

(2010) Christoph J. Wienken et al.   Nature Communications

Crosstalk Between Epidermal Growth Factor Receptor- and Insulin-Like Growth Factor-1 Receptor Signaling: Implications for Cancer Therapy

(2009) J. Veeken et al.   CURRENT CANCER DRUG TARGETS