Results 51 to 60 of about 488 (104)

Application of Fluorescence- and Bioluminescence-Based Biosensors in Cancer Drug Discovery

Biosensors
Recent advances in drug discovery have established biosensors as indispensable tools, particularly valued for their precision, sensitivity, and real-time monitoring capabilities.
Tynan Kelly, Xiaolong Yang
doaj   +1 more source

The GPCR Connection: Linking Alzheimer's Disease and Glioblastoma

Journal of Cellular and Molecular Medicine, Volume 30, Issue 7, April 2026.
ABSTRACT Alzheimer's disease (AD) and glioblastoma multiforme (GBM) are biologically distinct age‐related brain disorders with opposing clinical phenotypes. AD is characterised by progressive neurodegeneration and cognitive decline, whereas GBM is characterised by aggressive cellular proliferation and a poor prognosis.
Ana B. Caniceiro, Sofia P. Agostinho, Luiz F. Piochi, Nícia Rosário‐Ferreira, Irina S. Moreira   +4 more
wiley   +1 more source

Targeted Degradation of eEF2K by a Structure‐Guided PROTAC Strategy for the Treatment of Triple‐Negative Breast Cancer

Advanced Science, Volume 13, Issue 18, 27 March 2026.
This study developed an eEF2K‐targeting PROTAC, A6, that efficiently degrades eEF2K in TNBC cells, inhibiting tumor growth in vitro and in vivo. To enhance tumor‐specific delivery, we engineered A6@ZIF‐8, a pH‐sensitive nanocarrier, which improved drug accumulation at tumor sites, offering a promising therapeutic strategy for TNBC through targeted ...
Shijun Cao, Changxin Zhong, Shilong Jiang, Yungui Li, Yang Xi, Mingxuan Xiao, Ting Jiang, Xiaoya Wan, Zonglin Chen, Xiaohui Yu, Yan Cheng   +10 more
wiley   +1 more source

Light‐Based Molecular Tools to Precisely Monitor and Operate β‐Adrenoceptors

Medicinal Research Reviews, Volume 46, Issue 2, Page 445-474, March 2026.
ABSTRACT β‐Adrenoceptors are important G protein–coupled receptors involved in cardiovascular, metabolic, and neurological regulation. To study their function with high precision, light‐based molecular tools have been developed offering precise spatiotemporal control.
Ignazzitto Maria Tindara, Gómez‐Santacana Xavier, Llebaria Amadeu, Rovira Xavier   +3 more
wiley   +1 more source

The role of accessory proteins and co‐factors in regulation of melanocortin‐4 receptor signalling: An update

Journal of Neuroendocrinology, Volume 38, Issue 3, March 2026.
Abstract The melanocortin‐4 receptor (MC4R) is a G protein‐coupled receptor with an essential role in appetite suppression and energy homeostasis. Genetic mutations in the receptor and components of its signalling pathway that cause obesity in humans, dogs and rodent models have revealed important insights into how the receptor signals and what ...
Aqfan Jamaluddin, Alyce McClellan, Eleanor Raffan, Caroline M. Gorvin   +3 more
wiley   +1 more source

Determining the nanoBRET AL2K IC50 values of 24 new ACVR1/ALK2 inhibitors

, 2018
In an effort to develop clinical compounds for Diffused Intrinsic Pontine Glioma (DIPG) treatment, new analogues of ACVR1/ALK2 inhibitors are continuously synthesised by Ontario Institute for Cancer Research (OICR) and Charles River Laboratories (CRL). I
Alex, Jong Fu Wong, Jong Fu Wong (4949545), Alex (6929108)   +3 more
core   +1 more source

NanoBRET and NanoBiT/BRET-Based Ligand Binding Assays Permit Quantitative Assessment of Small Molecule Ligand Binding to Smoothened

, 2021
Smoothened (SMO) is a G protein-coupled receptor (GPCR) that mediates Hedgehog (Hh) signaling. SMO activity is regulated following the binding of Hh to the transmembrane protein Patched. Overactive SMO signaling is oncogenic, and hence this receptor is a
Paweł Kozielewicz, Schulte, G,, Gunnar Schulte, Kozielewicz, P,   +3 more
core   +1 more source

A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova, Thomas M. Geiger, Lorenzo Cianni, Dominika E. Pieńkowska, Jan Gerhartz, Lina Read, Aleša Bricelj, Alexander Herrmann, Maurice Leon Nelles, Yuen Lam Dora Ng, Marcus D. Hartmann, Jan Krönke, Izidor Sosič, Radosław P. Nowak, Michael Gütschow, Christian Steinebach   +15 more
wiley   +1 more source

A novel approach to target skin photodamage: Topical application of salt inducible kinase inhibitors

International Journal of Cosmetic Science, Volume 48, Issue 1, Page 1-15, February 2026.
UV‐induced photodamage leads to increased DNA damage and elevated MMP levels, which degrade collagen and contribute to wrinkle formation. SLT‐001 and SLT‐008, novel cosmetic ingredients that target salt‐inducible kinase, help reverse this effect by enhancing DNA repair, reducing MMP expression and decreasing erythema, thereby mitigating photodamage ...
Inbal Rachmin, Béatrice Le Varlet, Claire Regazzetti, Thierry Passeron, Jinhua Wang, David E. Fisher, Philippe Schaison, Braham Shroot   +7 more
wiley   +1 more source

Identification of low-molecular compounds that inhibit envelope formation of hepatitis B virus

Scientific Reports
Agents with novel mechanisms are clinically needed for the functional cure of chronic hepatitis B virus (HBV) infection. This study aimed to identify compounds that inhibit an interaction between large hepatitis B surface (LHBs) and hepatitis B core (HBc)
Kosuke Sato, Jun Inoue, Masashi Ninomiya, Akitoshi Sano, Mio Tsuruoka, Masazumi Onuki, Satoko Sawahashi, Keishi Ouchi, Kotaro Doi, Kengo Watanabe, Atsushi Masamune   +10 more
doaj   +1 more source