Results 121 to 130 of about 823,777 (226)

PROTACs in Oncology: Emerging Frontiers for Next-Generation Cancer Therapeutics

Onco
PROTACs represent a cutting-edge approach to the discovery of innovative cancer therapies. By exploiting the cell’s ubiquitin–proteasome system, PROTACs induce the selective degradation of target proteins, providing a distinct advantage over conventional
Salahuddin, Renu Sharma, Mohamed Jawed Ahsan, Avijit Mazumder, Kavita Rana, Rajnish Kumar, Chandana Majee   +6 more
doaj   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Conditional protein degradation with novel PROteolysis-TArgeting Chimeras (PROTACs)

, 2023
PROteolysis-TArgeting Chimeras (PROTACs) are novel heterobifunctional degraders that catalytically induce targeted protein degradation through the Ubiquitin-Proteasome System (UPS). Offering unique advantages over conventional small molecule inhibitors, PROTACs have successfully degraded a wide range of oncogenic proteins and showed potential as a ...
openaire   +2 more sources

Discovery of a potent proteolysis targeting chimera enables targeting the scaffolding functions of FK506‐binding protein 51 (FKBP51) [PDF]

The FK506‐binding protein 51 (FKBP51) is a promising target in a variety of disorders including depression, chronic pain, and obesity. Previous FKBP51‐targeting strategies were restricted to occupation of the FK506‐binding site, which does not affect ...
Walz, Michael, Lermyte, Frederik, Dreizler, Johannes K., Kuehn, Angela, Sugiarto, Wisely O., Meyners, Christian, Maciel, Edvaldo V. S., Hausch, Felix, Geiger, Thomas M., Zheng, Min   +9 more
core   +2 more sources

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Proteolysis-Targeting Chimera (PROTAC) Delivery into the Brain across the Blood-Brain Barrier. [PDF]

Antibodies (Basel), 2023
Tashima T.
europepmc   +1 more source

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Vepdegestrant, a PROTAC Estrogen Receptor Degrader, in Advanced Breast Cancer.

International audienceVepdegestrant is an oral proteolysis-targeting chimera (PROTAC) estrogen receptor (ER) degrader that directly harnesses the ubiquitin-proteasome ...
Ladoire, Sylvain, Hamilton, Erika, Molckovsky, Andrea, Lu, Dongrui, Fontana, Andrea, Zhang, Yongqiang, Cui, Jiuwei, Cil, Timucin, Martignoni, Marcella, Zamagni, Claudio, de Laurentiis, Michelino, Zhi, Xin, Rodriguez-Lescure, Alvaro, Guarneri, Valentina, Cazzaniga, Marina, Sezer, Ahmet, Demirci, Umut, Patsouris, Anne, Jerzak, Katarzyna, Parameswaran, Janaki, Fuentes, Christian, Jhaveri, Komal, Yoshinami, Tetsuhiro, Valota, Olga, Campone, Mario, Hu, Xichun, Mouret-Reynier, Marie-Ange   +26 more
core   +1 more source

BRD3 PROTAC degrader targets H3K18ac to alleviate retinal microglia-driven uveitis

iScience
Summary: Uveitis is a sight-threatening intraocular inflammation in which the proinflammatory immune response driven by retinal microglia is a key contributor.
Zhi Zhang, Tianlong Lan, Yongbo Liu, Hui Yang, Nan Shu, Ruonan Li, Wanqian Li, Qian Zhou, Peizeng Yang, Yu Rao, Shengping Hou   +10 more
doaj   +1 more source

Daraxonrasib and Beyond: Pan‐RAS Inhibition, Resistance, and Next‐Generation Strategies

Cancer Science, EarlyView.
ABSTRACT RAS proteins have long been considered difficult therapeutic targets, but allele‐selective inhibitors established the clinical tractability of mutant RAS. Daraxonrasib (RMC‐6236), an oral pan‐RAS inhibitor, has now extended this concept by targeting multiple mutant and wild‐type RAS proteins.
Ryo Honda
wiley   +1 more source