Results 41 to 50 of about 2,283,209 (217)

Dual‐Target Nectin‐4/FAP Heterobivalent Probe 68Ga/177Lu‐FZ‐NF‐1 for Triple‐Negative Breast Cancer: Preclinical Theranostic Evaluation and First‐in‐Human Translation

Advanced Science, EarlyView.
A novel hetero‐bivalent agent, 68Ga/177Lu‐FZ‐NF‐1, concurrently targets Nectin‐4 and FAP in triple‐negative breast cancer. It yields significant preclinical tumor regression and clinically identifies additional metastatic lesions missed by 18F‐FDG PET, demonstrating promising theranostic potential for personalized management.
Ye Li, Li Sun, Xiaoyu Pan, Shuyi Lin, Dongliang Wang, Jianping Zhang, Fengshuang Qiu, Bin Zhu, Lingzhou Zhao, Fengsheng Zhang, Liyan Bai, Bingxin Gu, Xiaoping Xu, Shaoli Song   +13 more
wiley   +1 more source

Analyzing Radioligand Binding Data [PDF]

, 2002
Radioligand binding experiments are easy to perform, and provide useful data in many fields. They can be used to study receptor regulation, discover new drugs by screening for compounds that compete with high affinity for radioligand binding to a ...
Neubig, Richard, Richard Neubig, Harvey Motulsky, Motulsky, Harvey   +3 more
core   +1 more source

Development of Plate Reader and On-Line Microfluidic Screening to Identify Ligands of the 5-Hydroxytryptamine Binding Protein in Venoms

Toxins, 2015
The 5-HT3 receptor is a ligand-gated ion channel, which is expressed in the nervous system. Its antagonists are used clinically for treatment of postoperative- and radiotherapy-induced emesis and irritable bowel syndrome.
Reka A. Otvos, Janaki Krishnamoorthy Iyer, René van Elk, Chris Ulens, Wilfried M. A. Niessen, Govert W. Somsen, R. Manjunatha Kini, August B. Smit, Jeroen Kool   +8 more
doaj   +1 more source

Interleukin‐39 is a Prognostic Biomarker and Therapy Target for Sepsis

Advanced Science, EarlyView.
Sepsis triggers a significant increase in IL‐39 production, with circulating levels markedly elevated and positively correlated with disease severity and poor clinical prognosis in sepsis patients. Mechanistically, macrophage‐derived IL‐39 activates the GP130 signaling pathway via a ligand‐receptor interaction, thereby fueling the pro‐inflammatory ...
Feng‐zhi Zhang, Hai‐jun Liu, Yan Yue, Jun‐jie Gao, Jin Zhang, Wen‐wu Zhang, Yun‐long Zhang, Wei‐hua Lu, Sheng‐wei Jin, Pu‐hong Zhang   +9 more
wiley   +1 more source

Partial characterization of thyroid stimulating hormone in thyroid tumors using radioligand binding assay techniques [PDF]

Thyroid Stimulating Hormone (TSH) plays a crucial role in regulating thyroid function and is implicated in various thyroid disorders, including tumors.
Hassan, A. N. M. A.
core   +2 more sources

Mechanistic Studies of the Antiallergic Activity of Phyllanthus amarus Schum. & Thonn. and Its Compounds

Molecules, 2021
Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds.
Nur Zahirah Abd Rani, Kok Wai Lam, Juriyati Jalil, Hazni Falina Mohamad, Mohd Shukri Mat Ali, Khairana Husain   +5 more
doaj   +1 more source

Innovative Approach Reveals How Receptors Control G Protein State Equilibria

Advanced Science, EarlyView.
Using conformational specific trFRET biosensors of the Gi protein (depicted at the bottom), the authors show that receptor activation can not only release GDP from the inactive G protein, but can also release GTP from the activated G protein, leading to the reformation of the RG ternary complex.
Alexandre Bouyssou, Mélanie Da Silva, Julien Soulé, Ludovic Fabre, Laurent Lamarque, Rémy Sounier, Thierry Durroux, Sébastien Granier, Thomas Roux, Elodie Dupuis, Eric Trinquet, Philippe Rondard, Jean‐Philippe Pin   +12 more
wiley   +1 more source

Paltusotine versus octreotide: different effects on radioligand uptake in neuroendocrine tumours

Endocrine Oncology
Objective: Somatostatin receptor analogues are well-established in the treatment of metastatic gastro-enteropancreatic neuroendocrine tumours (GEP-NETs), especially for symptom control in patients with the carcinoid syndrome, and to control tumour growth.
Katharina Wang, Christoph J Auernhammer, Simon Lindner, Mathias Zacherl, Rudolf A Werner, Julian Maurer, Lea Peischer, Julia Hamati, Maximilian P Hungbauer, Thomas Knösel, Astrid Reul, Elena Kuzmenko, Diana Vetter, José Oberholzer, Umberto Maccio, Felix Beuschlein, Martin Reincke, Constanze Hantel, Karel Pacak, Ashley B Grossman, Kathrin Zitzmann, Svenja Nölting   +21 more
doaj   +1 more source

Discovery of benzothiazolylquinoline conjugates as novel human A3 receptor antagonists: biological evaluations and molecular docking studies [PDF]

Royal Society Open Science, 2018
Adenosine is known as an endogenous purine nucleoside and it modulates a wide variety of physiological responses by interacting with adenosine receptors. Among the four adenosine receptor subtypes, the A3 receptor is of major interest in this study as it
Bidisha Sarkar, Santanu Maiti, Gajanan Raosaheb Jadhav, Priyankar Paira   +3 more
doaj   +1 more source

Comparative Evaluation of Chelator‐Conjugated Peptides for Lead‐Labeled SSTR2‐Targeted Theranostics: Integrated Computational Modeling and Preclinical Validation

Advanced Science, EarlyView.
The study integrates density functional theory with radiochemical and biological validation to compare DOTA‐, PSC‐, and DOTAM‐based chelator‐conjugates for 203Pb/212Pb theranostic applications. Distinct differences in metal coordination, electrostatic properties, conformational flexibility, cellular uptake, biodistribution, and dosimetry are identified
Jeongyun Kim, Na Yeon Han, Ayman Muzammal, Jae Hun Ahn, Changkeun Im, Sujin Kim, Sairan Eom, Choong Mo Kang, Ku Kang, Yong Jin Lee, Kyo Chul Lee, Michael K. Schultz, Dongyoul Lee   +12 more
wiley   +1 more source