Results 151 to 160 of about 827,025 (271)

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

CD93—An emerging vascular target in cancer therapy

British Journal of Pharmacology, EarlyView.
Abstract CD93 is a single‐pass transmembrane glycoprotein that belongs to the C‐type lectin domain group XIV family of proteins. Although it is known to be expressed in other cell types, namely, in some subsets of immune cells, CD93 is primarily expressed on endothelial cells, where it acts as a crucial regulator of angiogenesis.
Beatriz de Alves Pereira, Stefano Barbera, Roberta Lugano, Anna Dimberg   +3 more
wiley   +1 more source

Extracellular vesicles in pharmacology: Innovations in drug delivery and therapeutic applications in cancer

British Journal of Pharmacology, EarlyView.
Extracellular vesicles (EVs) are a diverse population of membrane nanoparticles secreted by nearly all cell types, playing a key role in intercellular communication by transferring bioactive macromolecular cargo. In cancer, EVs shape both the local tumour microenvironment and distant premetastatic niches.
Evangelia Pantazaka, Georgios Sivvas, Evangelia Papadimitriou, Constantinos M. Mikelis   +3 more
wiley   +1 more source

Population Pharmacokinetics and Exposure-Response Analyses of Vepdegestrant, a First-in-Class PROteolysis-TArgeting Chimera Estrogen Receptor Degrader. [PDF]

J Clin Pharmacol
Yang DZ, Masters JC, Wang H, Tran L, Zhang Y, Lee KC, Tan W, Jermain B.   +7 more
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

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

Identification of Clofibric Acid as a Synoviolin (SYVN1) Ligand for Proteolysis-Targeting Chimera (PROTAC) Development. [PDF]

ACS Med Chem Lett
Warren J, Munakala A, Zientek KD, Kim K, Wilmarth PA, Reddy AP, Li BX, Xiao X.   +7 more
europepmc   +1 more source

TRIM59 Drives Bladder Cancer Progression Through E3 Ligase‐Dependent K48‐Linked Degradation of PTRF

Cancer Science, EarlyView.
Schematic model of TRIM59‐driven BLCA progression through K48‐linked ubiquitination and proteasomal degradation of PTRF, leading to AKT activation and c‐Myc upregulation. ABSTRACT Tripartite motif‐containing 59 (TRIM59) is an E3 ubiquitin ligase implicated in multiple malignancies, but its role in bladder cancer (BLCA) remains incompletely understood ...
Junlin Gan, Xuesong Bai, Aijie Zhang, Fei Lin, Hang Tong, Tinghao Li, Ning Xu, Xinyuan Li, Zhou Yu, Hubin Yin   +9 more
wiley   +1 more source

Chromatin Remodeller BRD9 Orchestrates Odontoblastic Differentiation via Coordinating RUNX2‐KLF4

Cell Proliferation, EarlyView.
During odontoblast lineage commitment, the chromatin remodeller BRD9 acts as a critical epigenetic coordinator, orchestrating the chromatin landscape to facilitate synergistic binding of key transcription factors RUNX2 and KLF4 to target loci for odontogenesis.
Wenrui Zeng, Yuxiu Lin, Yongyan Gao, Delan Huang, Yuanyuan Li, Honglei Ruan, Guohua Yuan, Huan Liu, Zhi Chen   +8 more
wiley   +1 more source

Targeted, receptor‐mediated delivery of a masked d‐amino acid cell‐penetrating peptide for cell‐specific phototoxicity

The FEBS Journal, EarlyView.
A targeted phototoxic peptide selectively accumulates in cells expressing chemokine‐like receptor 1 (CMKLR1). Phototoxicity of the native peptide is low, but cleavage by lysosomal protease cathepsin B releases a 6‐tetramethylrhodamine (TMR) labeled nona‐ᴅ‐arginine which mediates lysosomal rupture and cell death upon irradiation.
Moritz List, Eva‐Maria Jülke, Annette G. Beck‐Sickinger   +2 more
wiley   +1 more source