Results 41 to 50 of about 1,238 (123)

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

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

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

Development and Characterization of a Noncovalent Stimulator of Interferon Genes Proteolysis‐Targeting Chimeras

ChemMedChem, Volume 21, Issue 1, January 2026.
The design, synthesis, and initial biological evaluation of noncovalent stimulator of interferon genes degraders are presented. The lead from this series, BH690L, exhibits an effective concentration for half‐maximal degradation (DC50) of 11.3 nM and a maximum level of degradation (Dmax) of 0.67.
Bo Hu, Adam S. Duerfeldt
wiley   +1 more source

Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time

Scientific Reports, 2017
Bioluminescence resonance energy transfer (BRET) has been a vital tool for understanding G protein-coupled receptor (GPCR) function. It has been used to investigate GPCR-protein and/or -ligand interactions as well as GPCR oligomerisation.
Carl W. White, Hannah K. Vanyai, Heng B. See, Elizabeth K. M. Johnstone, Kevin D. G. Pfleger   +4 more
doaj   +1 more source

Fluorescent ligands for dopamine D2/D3 receptors

Scientific Reports, 2020
Fluorescent ligands are versatile tools for the study of G protein-coupled receptors. Depending on the fluorophore, they can be used for a range of different applications, including fluorescence microscopy and bioluminescence or fluorescence resonance ...
Anni Allikalt, Nirupam Purkayastha, Khajidmaa Flad, Maximilian F. Schmidt, Alina Tabor, Peter Gmeiner, Harald Hübner, Dorothee Weikert   +7 more
doaj   +1 more source

Dual Targeting Approach Using 4‐Hydroxytamoxifen Neuropeptide Y Conjugates for Selective Addressing of Adipose Tissue

ChemMedChem, Volume 20, Issue 24, December 15, 2025.
The [F7,P34]‐pNPY based peptide‐drug conjugate targets the Y1 receptor and induces internalization. Once inside the cell, 4‐hydroxytamoxifen is cleaved from the peptide and is released into the cytosol, where it activates the estrogen receptor α. This dual‐targeting mechanism aims to promote body weight loss and offers a potential therapeutic strategy ...
Anna Kohler, Eva‐Maria Jülke, Luke C. Darveniza, Jan Stichel, Annette G. Beck‐Sickinger   +4 more
wiley   +1 more source