Understanding the Role of Cereblon in Hematopoiesis Through Structural and Functional Analyses

AA Akuffo - 2020 - digitalcommons.usf.edu
The discovery and implementation of immunomodulatory drugs (IMiD® s) has revolutionized
the treatment of many hematological malignancies due to the plethora of IMiD®-induced …

Targeting cereblon in hematologic malignancies

O Fuchs - Blood Reviews, 2023 - Elsevier
The protein cereblon (CRBN) is a substrate receptor of the cullin 4-really interesting new
gene (RING) E3 ubiquitin ligase complex CRL4 CRBN. Targeting CRBN mediates selective …

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

AEA Lopez-Girona, D Mendy, T Ito, K Miller, AK Gandhi… - Leukemia, 2012 - nature.com
Thalidomide and the immunomodulatory drug, lenalidomide, are therapeutically active in
hematological malignancies. The ubiquitously expressed E3 ligase protein cereblon …

Characterization of RING finger E3-ubiquitin ligase cereblon in hematopoietic regulation

Y Han, AM Rajadhyaksha, AW Mailloux, J Painter… - Blood, 2013 - Elsevier
Abstract Characterization of RING finger E3-Ubiquitin Ligase Cereblon in Hematopoietic
Regulation Cereblon is a RING-domain E3 ubiquitin ligase (UbL) that is the direct protein …

[HTML][HTML] Cereblon and its downstream substrates as molecular targets of immunomodulatory drugs

T Ito, H Handa - International journal of hematology, 2016 - Springer
Thalidomide was first developed as a sedative around 60 years ago, but exhibited
teratogenicity, leading to serious defects such as limb deformities. Nevertheless, thalidomide …

[PDF][PDF] Immunomodulatory drugs and their therapeutic effect in hematological malignancies through cereblon

O Fuchs - Hematology & Medical Oncology, 2017 - researchgate.net
Immunomodulatory drugs (IMiDs), today also known as cereblon (CRBN) binding drugs, are
therapeutically important anti-cancer and anti-inflammatory drugs. IMiDs are analogs of their …

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

AA Akuffo, AY Alontaga, R Metcalf, MS Beatty… - Journal of Biological …, 2018 - ASBMB
Upon binding to thalidomide and other immunomodulatory drugs, the E3 ligase substrate
receptor cereblon (CRBN) promotes proteosomal destruction by engaging the DDB1 …

Ligand Design for Cereblon Based Immunomodulatory Therapy

RB Kargbo - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
Biological Target. Cereblon (CRBN) Summary. Cereblon (CRBN) is a multifunctional protein
located in the cytoplasm, nucleus, and peripheral membrane of the human brain and other …

[引用][C] Next-generation drugs targeting the cereblon ubiquitin ligase

SA Holstein, J Hillengass, PL McCarthy - Journal of Clinical Oncology, 2018 - ascopubs.org
Despite the pervasive use of the immunomodulatory drugs (IMiDs), thalidomide,
lenalidomide, and pomalidomide, over the past 5 to 15 years for the management of multiple …

[HTML][HTML] Pomalidomide-Based Homo-Protacs for the Chemical Knockdown of Cereblon

S Lindner, C Steinebach, N Udeshi, D Mani, H Kehm… - Blood, 2018 - Elsevier
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide are all
approved for the treatment of multiple myeloma. IMiDs bind cereblon (CRBN), a substrate …