Results 41 to 50 of about 8,212 (230)

Orthogonal validation of PROTAC mediated degradation of the integral membrane proteins EGFR and c-MET

Scientific Reports
Dysregulation of integral membrane proteins (IMPs) has been linked to a myriad of diseases, making these proteins an attractive target in drug research. Whilst PROTAC technology has had a significant impact in scientific research, its application to IMPs
Camilla Ruffilli, Sascha Röth, Noam Zelcer, Kevin Moreau   +3 more
doaj   +1 more source

MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53

Acta Materia Medica, 2022
Inhibition or degradation of the anti-apoptotic protein BCL-XL is a viable strategy for cancer treatment. Despite the recent development of PROTACs for degradation of BCL-XL, the choice of E3 ligase has been restricted to VHL and CRBN.
Mengyang Chang, Feng Gao, Jing Chen, Giri Gnawali, Wei Wang   +4 more
doaj   +1 more source

The ubiquitin system in normal and infected germinal center B cells

FEBS Letters, EarlyView.
The ubiquitin system plays a central role in germinal center (GC) B cells, influencing differentiation to long‐lived memory B cells. Oncogenic gammaherpesviruses gain access to memory B cells by establishing latency in GC B cells. Mapping ubiquitin mechanisms in normal and infected GC B cells will define specific molecular circuits in B cells germane ...
Destiny Davis, Lesly Mejia, Emily K Moser   +2 more
wiley   +1 more source

PROTAC-PatentDB: A PROTAC Patent Compound Dataset

Scientific Data
Proteolysis-targeting chimeras (PROTAC) are emerging and promising molecules for targeted protein degradation which have the potential to overcome critical bottlenecks in traditional small molecule drug development. However, the scarcity of publicly available data on molecular compound structures has significantly hindered computational drug discovery ...
Hong Cai, Gengyuan Yao, Yulong Shi, Tianyi Zhang, Yuanjia Hu   +4 more
openaire   +2 more sources

Characteristic roadmap of linker governs the rational design of PROTACs

Acta Pharmaceutica Sinica B
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically degrade proteins responsible for the disease.
Yawen Dong, Tingting Ma, Ting Xu, Zhangyan Feng, Yonggui Li, Lingling Song, Xiaojun Yao, Charles R. Ashby, Jr, Ge-Fei Hao   +8 more
doaj   +1 more source

Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases

Life, 2021
Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
doaj   +1 more source

Inhibition of cyclin‐dependent kinases 12/13 using CT7439 as a treatment for colorectal cancer with CDK12 upregulation

Molecular Oncology, EarlyView.
The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington, Divya L. Dayanidhi, Mohammad Zokaasadi, John B. Mantyh, Pelumi D. Olawuni, Gabrielle Rupprecht, Jeremy M. Force, Shannon McCall, Ashwani K. Bahl, David S. Hsu, Jason A. Somarelli   +10 more
wiley   +1 more source

Identification and removal of a cryptic impurity in pomalidomide-PEG based PROTAC

Beilstein Journal of Organic Chemistry
Chemically induced dimerization is a powerful tool for studying protein function, wherein the IMiD (the “immunomodulatory drug”) class of PROTAC molecules with a PEG linker is frequently used to promote targeted protein degradation. The standard protocol
Bingnan Wang, Yong Lu, Chuo Chen
doaj   +1 more source

FAK inhibition disrupts tumor growth, apoptosis, and transcriptional regulation in GI-NETs

Endocrine Oncology
Background: Gastrointestinal neuroendocrine tumors (GI-NETs) are rare neoplasms with limited therapeutic options and increasing clinical incidence. Focal adhesion kinase (FAK) has been implicated in oncogenic processes across various tumor types; however,
Lara Toffoli, Angeliki Ditsiou, Luca Triboli, Victorine Hamm, Eva Moschioni, Francesca D’Este, Teresa Gagliano   +6 more
doaj   +1 more source

Loss of E3 Ubiquitin Ligase RINES via CpG Methylation Relieves Suppression of STAT3 and MYC, Facilitating Multiple Tumorigeneses

Advanced Science, EarlyView.
Dysregulated protein modifications drive tumorigenesis. RINES, an E3 ubiquitin ligase, represses tumor cell proliferation and metastasis by facilitating RING domain‐dependent, ubiquitin–proteasome‐mediated degradation of STAT3 and MYC, which consequently restrains cancer stemness and oncogenic progression.
Lili Li, Ka Man Ng, Xingsheng Shu, Xiaoxue Chai, Kai Yau Wong, Gopesh Srivastava, Anthony T.C. Chan, Wai Yee Chan, Qian Tao   +8 more
wiley   +1 more source