Recent advancements in the discovery of cereblon-based protease-targeted chimeras with potential for therapeutic intervention

Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer

(2021) Hidetomo Yokoo et al.   ACS Medicinal Chemistry Letters

Structure-Based Discovery of SIAIS001 as an Oral Bioavailability ALK Degrader Constructed from Alectinib

(2021) Chaowei Ren et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a PROTAC targeting ALK with in vivo activity

(2021) Guoyi Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy

(2021) Liguo Wang et al.   Nature Chemical Biology

Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer

(2021) Linrong Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs

(2021) Ga Yeong Kim et al.   MOLECULES

Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax

(2021) Hannah M. King et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

AZD5438-PROTAC: A selective CDK2 degrader that protects against cisplatin- and noise-induced hearing loss

(2021) Santanu Hati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation

(2021) Haixia Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Developments of CRBN-based PROTACs as potential therapeutic agents

(2021) Chao Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PROTACs: A novel strategy for cancer therapy

(2020) Jing Liu et al.   SEMINARS IN CANCER BIOLOGY

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

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

(2020) Sajid Khan et al.   ONCOGENE

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

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

Molecular mechanisms of thalidomide and its derivatives

(2020) Takumi ITO et al.   PROCEEDINGS OF THE JAPAN ACADEMY SERIES B-PHYSICAL AND BIOLOGICAL SCIENCES

Developing drugs for the ‘undruggable’

(2020) Abigail Sawyer   BIOTECHNIQUES

PROTAC: A promising technology for cancer treatment

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

PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases

(2020) Xueyang Jiang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo

(2020) Mingming Wei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications

(2020) Laura Goracci et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and pharmaceutical applications of proteolysis-targeting chimeric molecules

(2020) Yuqing Liang et al.   BIOCHEMICAL PHARMACOLOGY

Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs

(2020) Yun Chen et al.   ACS Medicinal Chemistry Letters

Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion

(2020) Xiaqiu Qiu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective Degradation of CDK6 by a Palbociclib Based PROTAC

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

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

(2019) Miriam Girardini et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeted protein degradation: elements of PROTAC design

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

Progress on small-molecule proteolysis-targeting chimeras

(2019) Wenhai Huang et al.   Future Medicinal Chemistry

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

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation

(2018) Andrea Testa et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

(2018) Sainan An et al.   EBioMedicine

Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

(2017) Pedro Soares et al.   JOURNAL OF MEDICINAL CHEMISTRY

Glutamine Triggers Acetylation-Dependent Degradation of Glutamine Synthetase via the Thalidomide Receptor Cereblon

(2016) Thang Van Nguyen et al.   MOLECULAR CELL

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

(2016) Julianty Frost et al.   Nature Communications

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

Catalytic in vivo protein knockdown by small-molecule PROTACs

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

Glycogen synthase kinase-3 beta (GSK-3β) signaling: Implications for Parkinson's disease

(2015) Mojtaba Golpich et al.   PHARMACOLOGICAL RESEARCH

Glycogen synthase kinase-3 (GSK3): Regulation, actions, and diseases

(2015) Eleonore Beurel et al.   PHARMACOLOGY & THERAPEUTICS

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Glutamine and cancer: cell biology, physiology, and clinical opportunities

(2013) Christopher T. Hensley et al.   JOURNAL OF CLINICAL INVESTIGATION

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

(2012) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface

(2012) Inge Van Molle et al.   CHEMISTRY & BIOLOGY

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 Leukemogenicity of AML1-ETO Is Dependent on Site-Specific Lysine Acetylation

(2011) L. Wang et al.   SCIENCE

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Q's next: the diverse functions of glutamine in metabolism, cell biology and cancer

(2009) R J DeBerardinis et al.   ONCOGENE

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS