Results 71 to 80 of about 37,460 (168)

Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera

The FEBS Journal, EarlyView.
Here, we report KTX207, a previously undescribed cereblon‐based PDE4 PROTAC that can specifically target PDE4D shortform for degradation. We showed that KTX207 could improve selectivity, potency and enable a long‐lasting effect when used at a sub‐nanomolar concentration.
Yuan Yan Sin, Aoife Giblin, Aleksandra Judina, Punchita Rujirachaivej, Laura G. Corral, Eliza Glennon, Zhi Xian Tai, Tian Feng, Eduardo Torres, Alina Zorn, Julia Gorelik, Elka Kyurkchieva, Pa Thai Yenchitsomanus, Cathy Swindlehurst, Kyle Chan, David Stirling, George S. Baillie   +16 more
wiley   +1 more source

Characterization of the Huntingtin gene promoter and Huntingtin transcriptional regulation

, 2015
Huntington’s disease (HD) is a late onset, neurological, autosomal dominant genetic disorder. Despite being associated to a defined genetic mutation within the huntingtin gene (HTT), little is known about its transcriptional regulation. HTT is expressed, at varying levels, throughout the body.
De Souza, Rebecca Anne Grace
openaire   +2 more sources

Transcriptional Regulation of the Huntingtin Gene

Journal of Huntington's Disease, 2018
Huntington's disease (HD) is an autosomal dominant neurodegenerative disorder caused by a CAG trinucleotide expansion in the HTT gene, which encodes for an abnormal polyglutamine tract in the huntingtin protein (HTT). This review examines the known mechanisms of HTT gene regulation.
Sarah B. Thomson, Blair R. Leavitt
openaire   +3 more sources

Identification of hepta-histidine as a candidate drug for Huntington's disease by in silico-in vitro- in vivo-integrated screens of chemical libraries. [PDF]

, 2016
We identified drug seeds for treating Huntington's disease (HD) by combining in vitro single molecule fluorescence spectroscopy, in silico molecular docking simulations, and in vivo fly and mouse HD models to screen for inhibitors of abnormal ...
Chen, Xigui, Finkbeiner, Steven, Fujita, Kyota, Homma, Hidenori, Ikura, Teikichi, Imamura, Tomomi, Ito, Nobutoshi, Kaye, Julia, Mao, Ying, Motoki, Kazumi, Nakabayashi, Makoto, Okano, Hideyuki, Okazawa, Hitoshi, Tagawa, Kazuhiko, Tamura, Takuya, Taniguchi, Juliana Bosso, Tomii, Kentaro, Yamada, Kazunori   +17 more
core   +2 more sources

PI5P4K inhibitors: promising opportunities and challenges

The FEBS Journal, EarlyView.
Developing inhibitors is like climbing a steep, challenging mountain. PI5P4K inhibitors hold significant promise for the treatment of cancer, immune disorders, and neurological diseases. However, the path to success is fraught with hurdles, and researchers are therefore required to apply their expertise to overcome critical “checkpoints.” While some ...
Koh Takeuchi, Lisa Nagase, Shun Kageyama, Hirotaka Kanoh, Masashi Oshima, Aki Ogawa‐Iio, Yoshiki Ikeda, Yuki Fujii, Sei Kondo, Natsuki Osaka, Takeshi Masuda, Tsukasa Ishihara, Yoshikazu Nakamura, Yoshihisa Hirota, Takehiko Sasaki, Toshiya Senda, Atsuo T. Sasaki   +16 more
wiley   +1 more source

A guide to heat shock factors as multifunctional transcriptional regulators

The FEBS Journal, EarlyView.
The heat shock factors (HSFs) are evolutionarily conserved transcription factors best known as regulators of molecular chaperone genes in response to heat shock and other protein‐damaging stresses. Vertebrate HSFs, HSF1‐5, HSFX, and HSFY, are implicated in various physiological and pathological processes, including organismal development and cancer ...
Hendrik S. E. Hästbacka, Alejandro J. Da Silva, Lea Sistonen, Eva Henriksson   +3 more
wiley   +1 more source

Cdk5 protects huntingtin

The Journal of Cell Biology, 2005
![Graphic][1] Cdk5 (red) phosphorylates htt (green) and protects it from caspases.A cyclin-dependent kinase protects neurons from toxic fragments of huntingtin (htt), according to Luo et al.
openaire   +3 more sources

Profiling Swallowing Safety and Physiology in People With Huntington's Disease

Neurogastroenterology &Motility, EarlyView.
We assessed swallowing in HD using the PAS and MBSImP. Safety profiles: 65% safe, 7.5% penetration, and 27.5% aspiration. Oral phase: 85% none‐to‐mild and 15% moderate severity. Pharyngeal phase: 97.5% none‐to‐mild and 2.5% moderate. Findings showed increased impairments in swallowing efficiency and the oral phase.
Claudia Raines, Makenna Clark, Cara Donohue   +2 more
wiley   +1 more source

A Systems Biology Approach towards Deciphering the Unfolded Protein Response in Huntington's Disease [PDF]

, 2012
Although the disease causing gene huntingtin has been known for some time, the exact cause of neuronal cell death during _Huntington's disease_ (HD) remains unknown.
Kameshwar R. Ayasolla, Matthias E. Futschik, Ravi K. R. Kalathur   +2 more
core   +2 more sources

The causative role of amyloidosis in the cardiac complications of Alzheimer's disease: a comprehensive systematic review

The Journal of Physiology, EarlyView.
Abstract figure legend Schematic illustration of the bidirectional causative link between cerebral amyloid‐beta (Aβ) angiopathy and cardiovascular disease in Alzheimer's disease (AD). Common cardiovascular risk factors like microvascular thrombosis, diabetes, atrial fibrillation, hypertension and atherosclerosis lead to cerebral hypoperfusion and ...
Samuel Parker, James Andrew, Mastitskaya Svetlana   +2 more
wiley   +1 more source