Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon

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

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

(2017) D T Saenz et al.   LEUKEMIA

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

(2016) Xin Wang et al.   BIOCHEMICAL PHARMACOLOGY

The molecular mechanism of thalidomide analogs in hematologic malignancies

(2016) Stefanie Lindner et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

A calcium- and calpain-dependent pathway determines the response to lenalidomide in myelodysplastic syndromes

(2016) Jing Fang et al.   NATURE MEDICINE

Immunomodulatory drugs disrupt the cereblon–CD147–MCT1 axis to exert antitumor activity and teratogenicity

(2016) Ruth Eichner et al.   NATURE 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

Antibody therapy alone and in combination with targeted drugs in chronic lymphocytic leukemia

(2016) Tadeusz Robak et al.   SEMINARS IN ONCOLOGY

Cereblon negatively regulates TLR4 signaling through the attenuation of ubiquitination of TRAF6

(2016) Yoon Min et al.   Cell Death & Disease

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

(2016) Honorine Lebraud et al.   ACS Central Science

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

BET bromodomain inhibition suppresses graft-versus-host disease after allogeneic bone marrow transplantation in mice

(2015) Y. Sun et al.   BLOOD

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

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

(2015) Jan Krönke et al.   NATURE

Immunomodulatory drugs target IKZF1-IRF4-MYC axis in primary effusion lymphoma in a cereblon-dependent manner and display synergistic cytotoxicity with BRD4 inhibitors

(2015) R Gopalakrishnan et al.   ONCOGENE

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Rate of CRL4CRBN substrate Ikaros and Aiolos degradation underlies differential activity of lenalidomide and pomalidomide in multiple myeloma cells by regulation of c-Myc and IRF4

(2015) C C Bjorklund et al.   Blood Cancer Journal

The IMiDs targets IKZF-1/3 and IRF4 as novel negative regulators of NK cell-activating ligands expression in multiple myeloma

(2015) Cinzia Fionda et al.   Oncotarget

Lenalidomide enhances antitumor functions of chimeric antigen receptor modified T cells

(2015) Pavel Otáhal et al.   OncoImmunology

Ikaros Imposes a Barrier to CD8+ T Cell Differentiation by Restricting Autocrine IL-2 Production

(2014) S. O'Brien et al.   JOURNAL OF IMMUNOLOGY

Thalidomide mimics uridine binding to an aromatic cage in cereblon

(2014) Marcus D. Hartmann et al.   JOURNAL OF STRUCTURAL BIOLOGY

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

(2014) Eric S. Fischer et al.   NATURE

Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs

(2014) Philip P Chamberlain et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Measuring cereblon as a biomarker of response or resistance to lenalidomide and pomalidomide requires use of standardized reagents and understanding of gene complexity

(2013) Anita K. Gandhi et al.   BRITISH JOURNAL OF HAEMATOLOGY

Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4CRBN

(2013) Anita K. Gandhi et al.   BRITISH JOURNAL OF HAEMATOLOGY

Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments

(2013) G. Madhavi Sastry et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

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

(2013) J. Kronke et al.   SCIENCE

Drug response in a genetically engineered mouse model of multiple myeloma is predictive of clinical efficacy

(2012) M. Chesi et al.   BLOOD

A Novel Approach to the Discovery of Small-Molecule Ligands of CDK2

(2012) Mathew P. Martin et al.   CHEMBIOCHEM

Expansion of Effector Memory Regulatory T Cells Represents a Novel Prognostic Factor in Lower Risk Myelodysplastic Syndrome

(2012) A. W. Mailloux et al.   JOURNAL OF IMMUNOLOGY

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Behavioral characterization of cereblon forebrain-specific conditional null mice: A model for human non-syndromic intellectual disability

(2011) Anjali M. Rajadhyaksha et al.   BEHAVIOURAL BRAIN RESEARCH

Functional modulation of AMP-activated protein kinase by cereblon

(2011) Kwang Min Lee et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

The Transcription Factor Myc Controls Metabolic Reprogramming upon T Lymphocyte Activation

(2011) Ruoning Wang et al.   IMMUNITY

Reversal of T-cell tolerance in myelodysplastic syndrome through lenalidomide immune modulation

(2011) J M McDaniel et al.   LEUKEMIA

Protacs for Treatment of Cancer

(2010) Kathleen M Sakamoto   PEDIATRIC RESEARCH

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

A spectrophotometric method for the determination of zinc, copper, and cobalt ions in metalloproteins using Zincon

(2009) Crystal E. Säbel et al.   ANALYTICAL BIOCHEMISTRY