Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs

Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators

(2021) Gisele Nishiguchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Clinical Activity of CC-90009, a Cereblon E3 Ligase Modulator and First-in-Class GSPT1 Degrader, As a Single Agent in Patients with Relapsed or Refractory Acute Myeloid Leukemia (R/R AML): First Results from a Phase I Dose-Finding Study

(2020) Geoffrey L. Uy et al.   BLOOD

Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality

(2020) Milka Kostic et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay

(2020) Wenwei Lin et al.   BIOCONJUGATE CHEMISTRY

A novel cereblon modulator for targeted protein degradation

(2019) Sung Ah Kim et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Targeted protein degradation: elements of PROTAC design

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

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature 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

CC-90009, a Novel Cereblon E3 Ligase Modulator, Targets GSPT1 for Degradation to Induce Potent Tumoricidal Activity Against Acute Myeloid Leukemia (AML)

(2019) Antonia Lopez-Girona et al.   BLOOD

Targeted protein degradation: expanding the toolbox

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

Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure-Degradation Relationships

(2018) George M. Burslem et al.   ChemMedChem

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

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

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

(2018) Chong Qin 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

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

(2018) Quinlan L. Sievers et al.   SCIENCE

Structural basis of PROTAC cooperative recognition for selective protein degradation

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

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL

(2015) P. R. Hagner et al.   BLOOD

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma

(2015) Sujatha Venataraman et al.   Oncotarget

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

(2014) Eric S. Fischer et al.   NATURE

HD-MB03 is a novel Group 3 medulloblastoma model demonstrating sensitivity to histone deacetylase inhibitor treatment

(2012) Till Milde et al.   JOURNAL OF NEURO-ONCOLOGY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE