Results 71 to 80 of about 827,025 (271)

Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders. [PDF]

ACS Med Chem Lett
Dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) has been identified as a promising oncogenic driver of several types of cancer and is considered to be a critical cancer therapeutic target.
Chen J, Zhu W, Zhang W, Tong Y, Xu F, Pang J.   +5 more
europepmc   +3 more sources

The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents

Molecules, 2020
The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez, Antonio Delgado, Bernat Crosas   +2 more
doaj   +1 more source

Analisi del protocollo chimera per la protezione di integrità dei segnali GNSS. [PDF]

, 2022
Questo lavoro di tesi è incentrato sull'analisi del protocollo Chimera per la protezione di integrità dei segnali GNSS, proposto all'International Technical Meeting of The Satellite Division of the Institute of Navigation, ION GNSS+, (Portland ...
Poltronieri, Anna
core  

DataSheet1_The proteolysis targeting chimera GMB-475 combined with dasatinib for the treatment of chronic myeloid leukemia with BCR::ABL1 mutants.pdf

, 2022
Patients with chronic myeloid leukemia (CML) show resistance to tyrosine kinase inhibitors (TKIs) targeting ABL1 due to the emergence of BCR::ABL1 mutants, especially compound mutants during the treatment, which brings great challenges to clinical ...
Wu Ye (11397215), Xia Wu (203682), Xiaoyu Wei (2794636), Xiaojia Wang (218810), Yuqian Tang (4528789), Yuping Gong (790038), Xianfeng Ouyang (13896624)   +6 more
core   +1 more source

A Second Pathogenic Protein, PolyGN2C‐iso2, Reveals a Dual‐Protein Pathology in Neuronal Intranuclear Inclusion Disease

Advanced Science, EarlyView.
This study reveals that NOTCH2NLC transcript variant 2 generates PolyGN2C‐iso2, an aggregating protein present within intranuclear inclusions of NIID patient tissues. A novel mouse model expressing PolyGN2C‐iso2 recapitulates white matter abnormalities and cognitive deficits, mechanistically linked to mitochondrial dysfunction. These findings support a
Kang Zhang, Wenhao Ma, Yi Zhou, Zhijie Wu, Pan Gao, Hongze Niu, Hongfei Tai, Tianyi Zhao, Zheyue Dong, Li Li, Yan Zhang, An Wang, Si Shen, Yueyang Li, Sifei Yu, Yan Peng, Wang Sheng, Xiaoyan Dong, Hua Pan, Kaibin Shi, Magdalena J. Koziol, Xiaobing Wu, Zaiqiang Zhang   +22 more
wiley   +1 more source

HaloTag-Targeted Sirtuin Rearranging Ligand (SirReal) for the Development of Proteolysis Targeting Chimeras (PROTACs) Against the Lysine Deacetylase Sirtuin 2 (Sirt2) [PDF]

, 2020
We have discovered the sirtuin rearranging ligands (SirReals) as a novel class of highly potent and selective inhibitors of the NAD+-dependent lysine deacetylase sirtuin 2 (Sirt2).
Sándor, Szunyogh, Dina, Robaa, Manfred, Jung, Attila, Lehotzky, Oliver, Einsle, Sören, Hammelmann, Nathalie, Wössner, Wolfgang, Sippl, Judit, Ovádi, Matthias, Schiedel, Judit, Oláh   +10 more
core   +2 more sources

Trafficking Deficiency of TMEM175 Variants in Parkinson's Disease Pathogenesis and the Prospects of Precision Medicine

Advanced Science, EarlyView.
This study identifies that the PD‐associated TMEM175‐L156P variant disrupts lysosomal ion channel trafficking by causing aberrant endoplasmic reticulum retention. A “chaperone–agonist” bifunctional small molecule restores TMEM175‐L156P lysosomal localization and channel function, thereby alleviating PD‐relevant cellular phenotypes and highlighting a ...
Ting Luo, Yu He, Shuyao Li, Haoyu Guan, Ruili Cui, Yu Shi, Zhongwen Jiang, Siyu Wang, Xuan Li, Jiyuan Li, Mei Hu, Yupeng Zhou, Beisha Tang, Yanyan Zhang, Zhaobing Gao, Yu Zhou, Zhenhua Liu, Ping Li   +17 more
wiley   +1 more source

Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera. [PDF]

FEBS J
Cyclic AMP (cAMP) has a crucial role in many vital cellular processes and there has been much effort expended in the discovery of inhibitors against the enzyme superfamily that degrades this second messenger, namely phosphodiesterases (PDEs). The journey
Sin YY, Giblin A, Judina A, Rujirachaivej P, Corral LG, Glennon E, Tai ZX, Feng T, Torres E, Zorn A, Gorelik J, Kyurkchieva E, Yenchitsomanus PT, Swindlehurst C, Chan K, Stirling D, Baillie GS.   +16 more
europepmc   +2 more sources

Proteolysis-Targeting Chimeras (PROTACs) Based on Macrocyclic Tetrapeptides Selectively Degrade Class I Histone Deacetylases 1–3 [PDF]

, 2020
Histone deacetylases (HDACs) remove acetyl groups from histone proteins and are implicated in gene regulation. They have been recognized as drug targets for treatment of cancer and other human diseases and several inhibitors are already clinically used ...
Martin, Roatsch, Christian Adam, Olsen, Manfred, Jung, Daniel, Herp, Anja, Vogelmann   +4 more
core   +2 more sources

A Single‐Amino‐Acid Ligand for LAT1: A Minimalist and Modular Platform for Lysosome‐Targeted Degradation of Membrane Proteins

Advanced Science, EarlyView.
LA‐LYTAC repurposes the cancer‐enriched amino acid transporter LAT1 as a lysosomal trafficking receptor for targeted membrane‐protein degradation. A single phenylalanine‐derived ligand, modularly linked to antibodies or small‐molecule binders, recruits PD‐L1, EGFR, or integrins to LAT1, triggering transporter‐mediated internalization, lysosomal ...
Liquan Zhu, Ke Liu, Haotian Liu, Chaoqi He, Xiaozhen Liu, Xin Zeng, Misha Mao, Yuxiao Mu, Ying Li, Qinghui Zheng, Hongchao Tang, Da Qian, Xuli Meng   +12 more
wiley   +1 more source