The therapeutic potential of PROTACs

Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer

(2020) Thomas L. Gonzalez et al.   BREAST CANCER RESEARCH AND TREATMENT

FAK-targeting PROTAC as a chemical tool for the investigation of non-enzymatic FAK function in mice

(2020) Hongying Gao et al.   Protein & Cell

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

Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors: an updated patent review (2016-2018)

(2019) William T. McElroy   EXPERT OPINION ON THERAPEUTIC PATENTS

Targeting Nuclear Receptors with PROTAC degraders

(2019) John J. Flanagan et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

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

Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation

(2019) Hong Chen et al.   BIOORGANIC CHEMISTRY

Selective oestrogen receptor degraders in breast cancer

(2019) Andrea Gombos   CURRENT OPINION IN ONCOLOGY

Bromodomains: a new target class for drug development

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

PROTACs– a game-changing technology

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

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015–2019)

(2019) Concepción Sánchez-Martínez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A kinase-independent role for CDK8 in BCR-ABL1+ leukemia

(2019) Ingeborg Menzl et al.   Nature Communications

Design, synthesis, and biological evaluation of small molecule PROTACs for potential anticancer effects

(2019) Yang Da et al.   MEDICINAL CHEMISTRY RESEARCH

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

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

Modulating the masters: chemical tools to dissect CBP and p300 function

(2018) Meghan E Breen et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers

(2018) Luping Qiu et al.   PLoS One

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

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

Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors

(2018) Dazhi Liu et al.   Therapeutics and Clinical Risk Management

Moonlighting with WDR5: A Cellular Multitasker

(2018) Alissa Guarnaccia et al.   Journal of Clinical Medicine

Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F-18]-T807

(2018) David T. Chien et al.   JOURNAL OF ALZHEIMERS DISEASE

Androgen-targeted therapy in men with prostate cancer: evolving practice and future considerations

(2018) E. David Crawford et al.   PROSTATE CANCER AND PROSTATIC DISEASES

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

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

The Histone H3 Lysine 4 Presenter WDR5 as an Oncogenic Protein and Novel Epigenetic Target in Cancer

(2018) Kebin Lu et al.   Frontiers in Oncology

A WEE1 Inhibitor Analog of AZD1775 Maintains Synergy with Cisplatin and Demonstrates Reduced Single-Agent Cytotoxicity in Medulloblastoma Cells

(2016) Christopher J. Matheson et al.   ACS Chemical Biology

The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain

(2016) Sarah E. Skerratt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting EZH2 in cancer

(2016) Kimberly H Kim et al.   NATURE MEDICINE

Exploitation of EP300 and CREBBP Lysine Acetyltransferases by Cancer

(2016) Narsis Attar et al.   Cold Spring Harbor Perspectives in Medicine

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

The MYC-WDR5 Nexus and Cancer

(2015) L. R. Thomas et al.   CANCER RESEARCH

Alike but Different: RAF Paralogs and Their Signaling Outputs

(2015) Enrico Desideri et al.   CELL

Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer

(2015) Donald P. McDonnell et al.   JOURNAL OF MEDICINAL CHEMISTRY

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

(2015) Trevor Dale et al.   Nature Chemical Biology

FAK signaling in human cancer as a target for therapeutics

(2015) Brian Y. Lee et al.   PHARMACOLOGY & THERAPEUTICS

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

(2014) Stuart W. J. Ember et al.   ACS Chemical Biology

RIP kinases: key decision makers in cell death and innate immunity

(2014) F Humphries et al.   CELL DEATH AND DIFFERENTIATION

Mechanisms of protein-folding diseases at a glance

(2014) J. S. Valastyan et al.   Disease Models & Mechanisms

Understanding the Roles of FAK in Cancer

(2014) Hyunho Yoon et al.   JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY

Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders

(2014) Divya Chaudhary et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evaluating TBK1 as a Therapeutic Target in Cancers with Activated IRF3

(2014) Asli Muvaffak et al.   MOLECULAR CANCER RESEARCH

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

(2014) Jennifer A. Woyach et al.   NEW ENGLAND JOURNAL OF MEDICINE

EZH2 as a potential target in cancer therapy

(2014) Michael T McCabe et al.   Epigenomics

B-Raf and the inhibitors: from bench to bedside

(2013) Tiangui Huang et al.   Journal of Hematology & Oncology

Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized Phase II study

(2012) Irene Kuter et al.   BREAST CANCER RESEARCH AND TREATMENT

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Central Theme of Parkinson’s Disease: α-Synuclein

(2012) Mehmet Ozansoy et al.   MOLECULAR NEUROBIOLOGY

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors

(2011) Hongbo Zeng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

WEE1 Kinase Targeting Combined with DNA-Damaging Cancer Therapy Catalyzes Mitotic Catastrophe

(2011) P. C. De Witt Hamer et al.   CLINICAL CANCER RESEARCH

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

(2011) Chuangxing Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Diaryl Ether-Based Ligands for Estrogen-Related Receptor α as Potential Antidiabetic Agents

(2011) Raymond J. Patch et al.   JOURNAL OF MEDICINAL CHEMISTRY

PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments

(2010) Isabelle Tanjoni et al.   CANCER BIOLOGY & THERAPY

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Mechanisms of tau-induced neurodegeneration

(2009) Khalid Iqbal et al.   ACTA NEUROPATHOLOGICA

SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples

(2009) Andrew Conroy et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants

(2008) Sara Redaelli et al.   JOURNAL OF CLINICAL ONCOLOGY

Phenotype, genotype, and worldwide genetic penetrance of LRRK2-associated Parkinson's disease: a case-control study

(2008) Daniel G Healy et al.   LANCET NEUROLOGY