Novel immunomodulatory drugs and neo-substrates

S Gao, S Wang, Y Song - Biomarker Research, 2020 - Springer
Thalidomide, lenalidomide and pomalidomide are immunomodulatory drugs (IMiDs)
effective in the treatment of multiple myeloma, myelodysplastic syndrome (MDS) with …

CRL4CRBN E3 Ligase Complex as a Therapeutic Target in Multiple Myeloma

J Barankiewicz, A Salomon-Perzyński… - Cancers, 2022 - mdpi.com
Simple Summary Immunomodulatory drugs (IMiDs) are effective in the treatment of multiple
myeloma (MM) and other hematological malignancies. Cereblon (CRBN), a target of IMiDs …

pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase

J An, CM Ponthier, R Sack, J Seebacher… - Nature …, 2017 - nature.com
Thalidomide and its derivatives lenalidomide and pomalidomide (IMiDs) are effective
treatments of haematologic malignancies. It was shown that IMiDs impart gain-of-function …

Homo-PROTACs for the chemical knockdown of cereblon

C Steinebach, S Lindner, ND Udeshi… - ACS chemical …, 2018 - ACS Publications
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …

A novel cereblon modulator for targeted protein degradation

SA Kim, A Go, SH Jo, SJ Park, YU Jeon, JE Kim… - European Journal of …, 2019 - Elsevier
Immunomodulatory drugs (IMiDs) exert anti-myeloma activity by binding to the protein
cereblon (CRBN) and subsequently degrading IKZF1/3. Recently, their ability to recruit E3 …

Lenalidomide derivatives and proteolysis-targeting chimeras for controlling neosubstrate degradation

S Yamanaka, H Furihata, Y Yanagihara, A Taya… - Nature …, 2023 - nature.com
Lenalidomide, an immunomodulatory drug (IMiD), is commonly used as a first-line therapy in
many haematological cancers, such as multiple myeloma (MM) and 5q myelodysplastic …

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 …

[HTML][HTML] A novel effect of thalidomide and its analogs: suppression of cereblon ubiquitination enhances ubiquitin ligase function

Y Liu, X Huang, X He, Y Zhou, X Jiang… - The FASEB …, 2015 - ncbi.nlm.nih.gov
The immunomodulatory drug (IMiD) thalidomide and its structural analogs lenalidomide and
pomalidomide are highly effective in treating clinical indications. Thalidomide binds to …

Crbn I391V is sufficient to confer in vivo sensitivity to thalidomide and its derivatives in mice

EC Fink, M McConkey, DN Adams… - Blood, The Journal …, 2018 - ashpublications.org
Thalidomide and its derivatives, lenalidomide and pomalidomide, are clinically effective
treatments for multiple myeloma and myelodysplastic syndrome with del (5q). These …

Immunomodulatory drugs activate NK cells via both Zap-70 and cereblon-dependent pathways

T Hideshima, D Ogiya, J Liu, T Harada, K Kurata, J Bae… - Leukemia, 2021 - nature.com
Immunomodulatory drugs (IMiDs) lenalidomide and pomalidomide show remarkable
antitumor activity in multiple myeloma (MM) via directly inhibiting MM-cell growth in the bone …