Results 21 to 30 of about 5,540 (198)

Molecular Mechanisms of the Teratogenic Effects of Thalidomide

Pharmaceuticals, 2020
Thalidomide was sold worldwide as a sedative over 60 years ago, but it was quickly withdrawn from the market due to its teratogenic effects. Thalidomide was later found to have therapeutic effects in several diseases, although the molecular mechanisms ...
Tomoko Asatsuma-Okumura, Takumi Ito, Hiroshi Handa   +2 more
doaj   +1 more source

Activity of a Novel Anti-Inflammatory Agent F-3,6′-dithiopomalidomide as a Treatment for Traumatic Brain Injury

Biomedicines, 2022
Traumatic brain injury (TBI) is a major risk factor for several neurodegenerative disorders, including Parkinson’s disease (PD) and Alzheimer’s disease (AD).
Shih Chang Hsueh, Michael T. Scerba, David Tweedie, Daniela Lecca, Dong Seok Kim, Abdul Mannan Baig, Yu Kyung Kim, Inho Hwang, Sun Kim, Warren R. Selman, Barry J. Hoffer, Nigel H. Greig   +11 more
doaj   +1 more source

UDP-Glucose: A Cereblon-Dependent Glucokinase Protein Degrader [PDF]

, 2022
We previously reported that glucokinase is ubiquitinated and degraded by cereblon with an unknown endogenous glucokinase protein degrader. Here, we show that UDP-glucose is a glucokinase protein degrader.
Abe, Wakana, Jaeyong Cho, Yamamura, Hatsuo, Hatsuo Yamamura, Miyagawa, Atsushi, Yamaguchi, Kazuki, Wakana Abe, Atsushi Miyagawa, Tsugawa, Yusuke, Kazuki Yamaguchi, Tsugawa, Yoji, Imai, Takeshi, Yoji Tsugawa, Takeshi Imai, Cho, Jaeyong   +14 more
core   +1 more source

Cereblon Deficiency Contributes to the Development of Elastase-Induced Emphysema by Enhancing NF-κB Activation

Antioxidants, 2022
Cereblon (CRBN) has been shown to play an essential role in regulating inflammatory response and endoplasmic reticulum stress, thus mediating the development of various diseases.
Eun-Young Heo, Kyoung-Hee Lee, Jisu Woo, Jiyeon Kim, Chang-Hoon Lee, Kyung-Jin Lee, Yun-Kyu Kim, Chul-Gyu Yoo   +7 more
doaj   +1 more source

Supplementary Figure from Interactome of Aiolos/Ikaros Reveals Combination Rationale of Cereblon Modulators with HDAC Inhibitors in DLBCL

, 2022
Supplementary Figure from Interactome of Aiolos/Ikaros Reveals Combination Rationale of Cereblon Modulators with HDAC Inhibitors in ...
Anita K. Gandhi (14891744), Vivek S. Chopra (15045122), Maria Ortiz Estevez (15045125), Hsiling Chiu (15045119), Patrick R. Hagner (15045116), Fadi Towfic (394366), Martino Colombo (3298965), Nisha Patel (336148), Michelle F. Waldman (15045128), Remco Loos (5791577)   +9 more
core   +6 more sources

A MedChem toolbox for cereblon-directed PROTACs [PDF]

MedChemComm, 2019
A modular chemistry toolbox was developed for cereblon-directed PROTACs.
Christian Steinebach, Izidor Sosič, Stefanie Lindner, Aleša Bricelj, Franziska Kohl, Yuen Lam Dora Ng, Marius Monschke, Karl G. Wagner, Jan Krönke, Michael Gütschow   +9 more
openaire   +2 more sources

Regulation of AMPK Activity by CRBN Is Independent of the Thalidomide-CRL4^CRBN Protein Degradation Axis

Pharmaceuticals, 2021
Cereblon (CRBN), a primary target of immune-modulatory imide drugs (IMiDs), functions as a substrate receptor in the CUL4-RBX1-DDB1-CRBN (known as CRL4CRBN) E3 ubiquitin ligase complex.
Seung-Joo Yang, Seungje Jeon, Jeong Won Baek, Kwang Min Lee, Chul-Seung Park   +4 more
doaj   +1 more source

Caspase-8 Inhibition Prevents the Cleavage and Degradation of E3 Ligase Substrate Receptor Cereblon and Potentiates Its Biological Function

Frontiers in Cell and Developmental Biology, 2020
Cereblon (CRBN), a substrate receptor of cullin 4-RING E3 ligase (CRL4), mediates the ubiquitination and degradation of constitutive substrates and immunomodulatory drug-induced neo-substrates including MEIS2, c-Jun, CLC1, IKZF1/3, CK1α, and SALL4.
Liang Zhou, Wenjun Yu, David S. Jayabalan, Ruben Niesvizky, Samie R. Jaffrey, Xiangao Huang, Guoqiang Xu   +6 more
doaj   +1 more source

A New Generation of IMiDs as Treatments for Neuroinflammatory and Neurodegenerative Disorders

Biomolecules, 2023
The immunomodulatory imide drug (IMiD) class, which includes the founding drug member thalidomide and later generation drugs, lenalidomide and pomalidomide, has dramatically improved the clinical treatment of specific cancers, such as multiple myeloma ...
Katherine O. Kopp, Margaret E. Greer, Elliot J. Glotfelty, Shih-Chang Hsueh, David Tweedie, Dong Seok Kim, Marcella Reale, Neil Vargesson, Nigel H. Greig   +8 more
doaj   +1 more source

Cereblon-Recruiting PROTACs: Will New Drugs Have to Face Old Challenges?

Pharmaceutics, 2023
The classical low-molecular-weight drugs are designed to bind with high affinity to the biological targets endowed with receptor or enzymatic activity, and inhibit their function.
Marcin Cieślak, Marta Słowianek
doaj   +1 more source