Results 111 to 120 of about 31,985 (308)

The calcilytic agent NPS 2143 rectifies hypocalcemia in a mouse model with an activating calcium-sensing-receptor (CaSR) mutation:relevance to autosomal dominant hypocalcemia type 1 (ADH1) [PDF]

, 2015
Autosomal dominant hypocalcemia type 1 (ADH1) is caused by germline gain-of-function mutations of the calcium-sensing receptor (CaSR) and may lead to symptomatic hypocalcemia, inappropriately low serum parathyroid hormone (PTH) concentrations and ...
Allen M. Spiegel, Breitwieser, Dong, Drude, Enikö Kallay, Fadil M. Hannan, Gerard V. Walls, Gowen, Hannan, Hannan, Harding, Hofer, Hough, Hu, Hu, Huang, Jianxin Hu, John, Kinoshita, Kumar, Leach, Leach, Letz, Letz, Lia-Baldini, Loupy, M. Andrew Nesbit, Miedlich, Nemeth, Nemeth, Nesbit, Pearce, Pearce, Petrel, Rajesh V. Thakker, Raue, Roger D. Cox, Stechman, Tertius A. Hough, Thim, Valerie N. Babinsky, Vargas-Poussou, Watanabe, William D. Fraser, Yamamoto   +44 more
core   +1 more source

A Metal‐Free Carbon Monoxide Prodrug Suppresses Metastasis of Pancreatic and Breast Cancer

Advanced Science, EarlyView.
A metal‐free carbon monoxide (CO) prodrug, CO‐116, delivers controlled systemic CO without inhalation. CO suppresses the HRG1–heme axis, reducing intracellular heme availability. Attenuation of this pathway inhibits metastatic progression in pancreatic and triple‐negative breast cancer models.
Tiantian Zhang, Xiang Chen, Xiaoxiao Yang, Muskan Gori, Rohit Kumar Varshnaya, Dongning Liu, Cheryl Zhang, Michelle Yi Qin Chen, Zhengming Chen, George Zhang, Erika Patel, Qiyue Mao, Tan A. Ince, Chalet Tan, Binghe Wang, Yi‐Chieh Nancy Du   +15 more
wiley   +1 more source

Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.

PLoS ONE, 2017
S 47445 is a novel positive allosteric modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors (AMPA-PAM). S 47445 enhanced glutamate's action at AMPA receptors on human and rat receptors and was inactive at NMDA and ...
Sylvie Bretin, Caroline Louis, Laure Seguin, Stéphanie Wagner, Jean-Yves Thomas, Sylvie Challal, Nathalie Rogez, Karine Albinet, Fabrice Iop, Nadège Villain, Sonia Bertrand, Ali Krazem, Daniel Bérachochéa, Stéphanie Billiald, Charles Tordjman, Alex Cordi, Daniel Bertrand, Pierre Lestage, Laurence Danober   +18 more
doaj   +1 more source

Chimeric glutamate receptor subunits reveal the transmembrane domain is sufficient for NMDA receptor pore properties but some positive allosteric modulators require additional domains [PDF]

, 2016
NMDA receptors are ligand-gated ion channels that underlie transmission at excitatory synapses and play an important role in regulating synaptic strength and stability.
Huettner, Jmaes E, Lopez, Melany N, Wilding, Timothy J   +2 more
core   +2 more sources

Endothelial GPR68 Is Essential for Arteriogenesis and Represents a Therapeutic Target in a Model of Peripheral Artery Disease

Advanced Science, EarlyView.
Endothelial GPR68 is identified as a critical regulator of collateral artery growth in peripheral artery disease. Genetic and pharmacological evidence demonstrates that GPR68 integrates hemodynamic cues to drive monocyte recruitment and inflammatory remodeling, thereby promoting collateral arteriogenesis and tissue perfusion after ischemia ...
Yiyan Song, Senyi Peng, Zhilei Huang, Miao Yu, Mingyue Wu, Yuexin Zhu, Zeyi Zhou, Yongshan Liu, Yalin Zhang, Yu Huang, Zhongxing Wang, Fu‐Li Xiang, Jie Xu   +12 more
wiley   +1 more source

Development and Structural Characterization of UTE‐156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase

Advanced Science, EarlyView.
The AAA+ ATPase Valosin‐containing protein (VCP/p97) regulates protein homeostasis by unfolding ubiquitinated substrates. Here, we describe UTE‐156, a novel irreversible covalent inhibitor that modifies Cys522 in the D2 ATPase motor domain. Although its pharmacochemical limitations preclude immediate therapeutic use, UTE‐156 serves as a valuable ...
Daniela Tamayo‐Jaramillo, Subramanya Hegde, Xuan Jia, Kimberly Coffman, Hariprasad Vankayalapati, David Bearss, Kevin B. Jones, Alex W. Stark, Peter S. Shen   +8 more
wiley   +1 more source

Heteroreceptor complexes and their allosteric receptor-receptor interactions in the central nervous system. Focus on examples from Dopamine D2 and Serotonin 5-HT1a receptors [PDF]

, 2018
GPCR interacting proteins (specially β- arrestin) and their receptor-protein interactions are also covered but their interactions with the allosteric receptor-receptor interactions in heteroreceptor complexes remain to be elucidated.
Corrales Ferro, Fidel
core   +1 more source

Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization [PDF]

, 2013
Keywords:adenosine;allosterism;receptor;GPCR;dimerization;biased signalling The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It is released under a variety of physiological and pathophysiological conditions to
Albrecht-Kupper, Alexander, Amoah-Apraku, Aurelio, Aurelio, Avlani, Azzi, Baker, Baker, Bar-Yehuda, Bar-Yehuda, Baraldi, Baraldi, Barbhaiya, Briddon, Bruns, Bruns, Carr, Casadó, Chandrasekera, Chen, Chiavegatta, Chien, Christopoulos, Christopoulos, Chung, Ciruela, Clark, Cohen, Cordeaux, Corriden, Corriden, Cristovao-Ferreira, Dowling, Du, Dubey, Ellis, Fishman, Franco, Fredholm, Gao, Gao, Gao, Gao, Ge, Gessi, Goedeke, Goldman, Graaf, Gracia, Gracia, Griffin, Göblyös, Göblyös, Han, Harrison, Heitman, Hern, Hu, Ilien, Jaakola, Jacobson, Jacobson, Janusz, Kenakin, Kenakin, Keov, Kimatrai-Salvador, Klaft, Klein, Knapp, Kostenis, Kourounakis, Kuszak, Langemeijer, Lazareno, Lee, Lee, Lee, Limbird, Liu, Madi, Mares, Matherne, May, May, May, May, McCrea, Meno, Merighi, Morrison, Muller, Nikolakopoulos, Park, Peeters, Pisterzi, Rasmussen, Romagnoli, Roth, Salvatore, Smith, Sowa, Springael, Street, Suzuki, Swaminath, Tendera, Tinney, Uematsu, Urizar, Valant, Whalen, Williams, Xu   +114 more
core   +2 more sources

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

Advanced Science, EarlyView.
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

Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.

PLoS ONE, 2017
There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity.
Mustafa Nazıroğlu, Bilal Çiğ, Walter Blum, Csaba Vizler, Andrea Buhala, Annamária Marton, Róbert Katona, Katalin Jósvay, Beat Schwaller, Zoltán Oláh, László Pecze   +10 more
doaj   +1 more source