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

Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs

(2020) Rishi R. Shah et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance

(2020) Ning Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation

(2020) Li Zhou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Optical Control of Small Molecule-Induced Protein Degradation

(2020) Yuta Naro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Androgen receptor degraders overcome common resistance mechanisms developed during prostate cancer treatment

(2020) Steven Kregel et al.   NEOPLASIA

PHOTACs enable optical control of protein degradation

(2020) Martin Reynders et al.   Science Advances

Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2, 3-dioxygenase 1

(2020) Mingxing Hu et al.   Acta Pharmaceutica Sinica B

First small-molecule PROTACs for G protein-coupled receptors: Inducing α1A-adrenergic receptor degradation

(2020) Zhenzhen Li et al.   Acta Pharmaceutica Sinica B

Fundamental aspects of DMPK optimization of targeted protein degraders

(2020) Carina Cantrill et al.   DRUG DISCOVERY TODAY

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

(2020) Xuan 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

Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

(2020) Yu-Hui Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase

(2020) Mei-Xin Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations

(2020) Xiaoyun Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

(2020) Mingliang Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

(2020) Ronen Gabizon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Multispecific drugs herald a new era of biopharmaceutical innovation

(2020) Raymond J. Deshaies   NATURE

PROTAC Technology: Opportunities and Challenges

(2020) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity

(2020) Yonghan He et al.   Nature Communications

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

(2019) Jiantao Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

A chemical approach for global protein knockdown from mice to non-human primates

(2019) Xiuyun Sun et al.   Cell Discovery

Targeting the untargetable KRAS in cancer therapy

(2019) Pingyu Liu et al.   Acta Pharmaceutica Sinica B

PROTAC Molecules for the Treatment of Autoimmune Disorders

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

(2019) Yonghui Sun et al.   LEUKEMIA

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

(2019) Johannes Popow et al.   JOURNAL OF MEDICINAL CHEMISTRY

Degrading proteins in animals: “PROTAC”tion goes in vivo

(2019) Jianping Guo et al.   CELL RESEARCH

Selective Degradation of CDK6 by a Palbociclib Based PROTAC

(2019) Sandeep Rana et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

(2019) Baishan Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

(2019) Michael J. Roy et al.   ACS Chemical Biology

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

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

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

Recent applications of click chemistry in drug discovery

(2019) Xiangyi Jiang et al.   Expert Opinion on Drug Discovery

Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes

(2019) Lu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

(2019) Xing Qiu et al.   ORGANIC LETTERS

Treatment of Prostate Cancers and Kennedy’s Disease by PROTAC-Androgen Receptor Degradation

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

(2019) Lijie Peng et al.   ACS Medicinal Chemistry Letters

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

(2019) M Catarina Silva et al.   eLife

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

(2019) Scott D. Edmondson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

Targeted protein degradation: elements of PROTAC design

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

Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation

(2019) Meiyang Xi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

(2019) Hao Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

(2019) William Farnaby et al.   Nature Chemical Biology

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

(2019) Xiaoyu Zhang et al.   Nature Chemical Biology

Bromodomains: a new target class for drug development

(2019) Andrea G. Cochran et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting IRAK4 for Degradation with PROTACs

(2019) Joao Nunes et al.   ACS Medicinal Chemistry Letters

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

(2019) Mélissanne de Wispelaere et al.   Nature Communications

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

(2019) Hannah Tovell et al.   ACS Chemical Biology

PROTACs– a game-changing technology

(2019) Markella Konstantinidou et al.   Expert Opinion on Drug Discovery

Progress on small-molecule proteolysis-targeting chimeras

(2019) Wenhai Huang et al.   Future Medicinal Chemistry

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

(2019) Shang Su et al.   JOURNAL OF MEDICINAL CHEMISTRY

Simple Structural Modifications Converting a Bona Fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

(2019) Jiuling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

TrkC-Targeted Kinase Inhibitors And PROTACs

(2019) Bosheng Zhao et al.   MOLECULAR PHARMACEUTICS

PROTAC Degradation of IRAK4 for the Treatment of Neurodegenerative and Cardiovascular Diseases

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

(2019) Patrick Pfaff et al.   ACS Central Science

Degradation of proteins by PROTACs and other strategies

(2019) Yang Wang et al.   Acta Pharmaceutica Sinica B

Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins

(2019) Nobumichi Ohoka et al.   ACS Chemical Biology

Protein targeting chimeric molecules specific for dual bromodomain 4 (BRD4) and Polo-like kinase 1 (PLK1) proteins in acute myeloid leukemia cells

(2019) Xupeng Mu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

PROTACs as Potential Therapeutic Agents for Cancer Drug Resistance

(2019) Xiuyun Sun et al.   BIOCHEMISTRY

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

(2019) Longchuan Bai et al.   CANCER CELL

Bifunctional chemical probes inducing protein–protein interactions

(2019) Chiara Maniaci et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Recent advances in the CRISPR genome editing tool set

(2019) Su Bin Moon et al.   EXPERIMENTAL AND MOLECULAR MEDICINE

Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

(2019) Quanju Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader

(2019) Jieli Wei et al.   JOURNAL OF MEDICINAL CHEMISTRY

Light-Induced Protein Degradation with Photocaged PROTACs

(2019) Gang Xue et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

Targeted protein degradation: expanding the toolbox

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

Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs

(2019) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Development of a PDEδ-Targeting PROTACs that Impair Lipid Metabolism

(2019) Michael Winzker et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development of selective mono or dual PROTAC degrader probe of CDK isoforms

(2019) Fei Zhou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of MEK PROTACs

(2019) Stefan Vollmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

(2019) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

(2019) Sajid Khan et al.   NATURE MEDICINE

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

(2019) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

(2018) Ka Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Resistance a major hindrance to chemotherapy in hepatocellular carcinoma: an insight

(2018) K. Lohitesh et al.   Cancer Cell International

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

In Vivo Photopharmacology

(2018) Katharina Hüll et al.   CHEMICAL REVIEWS

Monoclonal antibodies as immunomodulatory therapy against cancer and autoimmune diseases

(2018) Umbreen Hafeez et al.   CURRENT OPINION IN PHARMACOLOGY

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)

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

Phthalimide conjugations for the degradation of oncogenic PI3K

(2018) Wenlu Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review

(2018) Chengyuan Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

(2018) Chelsea E. Powell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

(2018) Nicola E. A. Chessum et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of selective androgen receptor modulators (SARMs)

(2018) Ramesh Narayanan et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Mechanisms of receptor tyrosine kinase activation in cancer

(2018) Zhenfang Du et al.   Molecular Cancer

Plasticity in binding confers selectivity in ligand-induced protein degradation

(2018) Radosław P. Nowak et al.   Nature Chemical Biology

Targeting the IL-6/JAK/STAT3 signalling axis in cancer

(2018) Daniel E. Johnson et al.   Nature Reviews Clinical Oncology

Delineating the role of cooperativity in the design of potent PROTACs for BTK

(2018) Adelajda Zorba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

(2018) John M. Hatcher et al.   ACS Medicinal Chemistry Letters

Recent Advances in the Treatment of Breast Cancer

(2018) Christy W. S. Tong et al.   Frontiers in Oncology

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

(2018) Zuni I. Bassi et al.   ACS Chemical Biology

Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)

(2018) Chung Hyo Kang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

(2018) Jinlei Bian et al.   BIOORGANIC CHEMISTRY

Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin–proteasome pathway

(2018) Hong Chen et al.   BIOORGANIC CHEMISTRY

Brigatinib versus Crizotinib in ALK-Positive Non–Small-Cell Lung Cancer

(2018) D. Ross Camidge et al.   NEW ENGLAND JOURNAL OF MEDICINE

Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase

(2018) Norihito Shibata et al.   Scientific Reports

Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer

(2018) Dennis Dobrovolsky et al.   BLOOD

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

(2018) John Hines et al.   CANCER RESEARCH

Receptor Tyrosine Kinase-Targeted Cancer Therapy

(2018) Toshimitsu Yamaoka et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

(2018) Vittoria Zoppi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

(2018) Philipp M. Cromm et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

(2017) Scott J. Hughes et al.   Essays in Biochemistry

Targeted therapies in non-small cell lung cancer: a focus on ALK/ROS1 tyrosine kinase inhibitors

(2017) Assunta Sgambato et al.   Expert Review of Anticancer Therapy

Polycomb Repressor Complex 2 in Genomic Instability and Cancer

(2017) Zoe Veneti et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Editorial: Seeing is not always believing: lessons from knockout mice

(2017) Emilie Vénéreau et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

(2017) Andrew P. Crew et al.   JOURNAL OF MEDICINAL CHEMISTRY

A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

(2017) Ryan P. Wurz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

(2017) Kwok-Ho Chan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

(2017) Bing Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

(2017) Calla M Olson et al.   Nature Chemical Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Delivery technologies for genome editing

(2017) Hao Yin et al.   NATURE REVIEWS DRUG DISCOVERY

Alectinib versus Crizotinib in Untreated ALK-Positive Non–Small-Cell Lung Cancer

(2017) Solange Peters et al.   NEW ENGLAND JOURNAL OF MEDICINE

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation

(2017) Kenichiro Shimokawa et al.   ACS Medicinal Chemistry Letters

Genetic compensation: A phenomenon in search of mechanisms

(2017) Mohamed A. El-Brolosy et al.   PLoS Genetics

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

New strategy for renal fibrosis: Targeting Smad3 proteins for ubiquitination and degradation

(2016) Xin Wang et al.   BIOCHEMICAL PHARMACOLOGY

Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand

(2016) Yosuke Demizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Induced protein degradation: an emerging drug discovery paradigm

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

Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia

(2016) Andrew W. Roberts et al.   NEW ENGLAND JOURNAL OF MEDICINE

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

(2015) Ashton C. Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies

(2015) M. J. Niederst et al.   CLINICAL CANCER RESEARCH

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

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

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Mechanism-based pharmacokinetic/pharmacodynamic meta-analysis of navitoclax (ABT-263) induced thrombocytopenia

(2014) Aksana Kaefer et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Privileged Structures: Efficient Chemical “Navigators” toward Unexplored Biologically Relevant Chemical Spaces

(2014) Jonghoon Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Generation of targeted mouse mutants by embryo microinjection of TALENs

(2014) Benedikt Wefers et al.   METHODS

Suppression of Feedback Loops Mediated by PI3K/mTOR Induces Multiple Overactivation of Compensatory Pathways: An Unintended Consequence Leading to Drug Resistance

(2014) E. Rozengurt et al.   MOLECULAR CANCER THERAPEUTICS

Erasers of Histone Acetylation: The Histone Deacetylase Enzymes

(2014) E. Seto et al.   Cold Spring Harbor Perspectives in Biology

Targeting PI3K/Akt/mTOR Signaling in Cancer

(2014) Camillo Porta et al.   Frontiers in Oncology

The complex transcriptional landscape of the anucleate human platelet

(2013) Paul F Bray et al.   BMC GENOMICS

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

(2013) Peter E. Czabotar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Next Generation Sequencing Analysis of Human Platelet PolyA+ mRNAs and rRNA-Depleted Total RNA

(2013) Antheia Kissopoulou et al.   PLoS One

Pirin is an iron-dependent redox regulator of NF- B

(2013) F. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular Epidemiology of EGFR and KRAS Mutations in 3,026 Lung Adenocarcinomas: Higher Susceptibility of Women to Smoking-Related KRAS-Mutant Cancers

(2012) S. Dogan et al.   CLINICAL CANCER RESEARCH

Rational Approaches to Improving Selectivity in Drug Design

(2012) David J. Huggins et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

Cellular functions of FAK kinases: insight into molecular mechanisms and novel functions

(2010) M. D. Schaller   JOURNAL OF CELL SCIENCE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors

(2010) Jianyong Chen et al.   ACS Medicinal Chemistry Letters

AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer

(2009) Krishna M. Vasudevan et al.   CANCER CELL

Cyclin-dependent kinases: a family portrait

(2009) Marcos Malumbres et al.   NATURE CELL BIOLOGY