Folate-Guided Protein Degradation by Immunomodulatory Imide Drug-Based Molecular Glues and Proteolysis Targeting Chimeras

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cancer Selective Target Degradation by Folate-Caged PROTACs

(2021) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Light-induced control of protein destruction by opto-PROTAC

(2020) Jing Liu et al.   Science Advances

Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

(2020) Marı́a Maneiro et al.   ACS Chemical Biology

Exploiting the folate receptor α in oncology

(2020) Mariana Scaranti et al.   Nature Reviews Clinical Oncology

Skp2 dictates cell cycle-dependent metabolic oscillation between glycolysis and TCA cycle

(2020) Jing Liu et al.   CELL RESEARCH

The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

(2020) Mikołaj Słabicki et al.   NATURE

Rational discovery of molecular glue degraders via scalable chemical profiling

(2020) Cristina Mayor-Ruiz et al.   Nature Chemical Biology

ARID2 is a pomalidomide-dependent CRL4CRBN substrate in multiple myeloma cells

(2020) Junichi Yamamoto et al.   Nature Chemical Biology

Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation

(2020) Lu Lv et al.   eLife

Folate receptors and transporters: biological role and diagnostic/therapeutic targets in cancer and other diseases

(2019) Barbara Frigerio et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

(2019) Thomas H. Pillow et al.   ChemMedChem

p63 is a cereblon substrate involved in thalidomide teratogenicity

(2019) Tomoko Asatsuma-Okumura et al.   Nature Chemical Biology

Targeted protein degradation: expanding the toolbox

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

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

(2019) Peter S. Dragovich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders

(2018) Mette Ishoey et al.   ACS Chemical Biology

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

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

Striking a Balance between Carbonate/Carbamate Linkage Bond- and Reduction-Sensitive Disulfide Bond-Bearing Linker for Tailored Controlled Release: In Situ Covalent-Albumin-Binding Gemcitabine Prodrugs Promote Bioavailability and Tumor Accumulation

(2018) Huicong Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expression of functional folate receptors in multiple myeloma

(2018) Ying Zhou et al.   LEUKEMIA & LYMPHOMA

Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome

(2018) Katherine A Donovan et al.   eLife

Selective degradation of splicing factor CAPERα by anticancer sulfonamides

(2017) Taisuke Uehara et al.   Nature Chemical Biology

Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15

(2017) Ting Han et al.   SCIENCE

Blurring the Role of Oligonucleotides: Spherical Nucleic Acids as a Drug Delivery Vehicle

(2016) Xuyu Tan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Induced protein degradation: an emerging drug discovery paradigm

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

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

(2015) Jan Krönke et al.   NATURE

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

Cell-Specific, Activatable, and Theranostic Prodrug for Dual-Targeted Cancer Imaging and Therapy

(2011) Santimukul Santra et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Prodrug Approach for Increasing Cellular Glutathione Levels

(2010) Ivana Cacciatore et al.   MOLECULES

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Antibody−Drug Conjugates: Linking Cytotoxic Payloads to Monoclonal Antibodies

(2009) Laurent Ducry et al.   BIOCONJUGATE CHEMISTRY

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

(2009) Teresa A. Soucy et al.   NATURE