Attah, Isaac Y Neumann, Alexander Al-Hroub, Haneen Rafehi, Muhammad Baqi, Younis Namasivayam, Vigneshwaran Müller, Christa E
Published in
Biochimica et biophysica acta. General subjects
The nucleotide receptors P2Y2 and P2Y4 are the most closely related G protein-coupled receptors (GPCRs) of the P2Y receptor (P2YR) family. Both subtypes couple to Gq proteins and are activated by the pyrimidine nucleotide UTP, but only P2Y2R is also activated by the purine nucleotide ATP. Agonists and antagonists of both receptor subtypes have pote...
Girdhar, Khyati Dehury, Budheswar Kumar Singh, Mahender Daniel, Vineeth P Choubey, Abhinav Dogra, Surbhi Kumar, Sunil Mondal, Prosenjit
Published in
Journal of biomolecular structure & dynamics
The glucagon-like peptide-1 receptor (GLP-1R) is a well-known target of therapeutics industries for the treatment of various metabolic diseases like type 2 diabetes and obesity. The structural-functional relationships of small molecule agonists and GLP-1R are yet to be understood. Therefore, an attempt was made on structurally known GLP-1R agonists...
Martelli, Giulia Galletti, Paola Baiula, Monica Calcinari, Luca Boschi, Giacomo Giacomini, Daria
Published in
Bioorganic chemistry
Obtainment and testing of pure enantiomers are of great importance for bioactive compounds, because of the assessed implications of enantioselectivity in receptor-mediated responses. Herein we evaluated the use of biocatalysis to obtain enantiomerically pure β-lactam intermediates further exploited in the synthesis of novel integrin ligands as sing...
Żeromski, Jan Kaczmarek, Mariusz Boruczkowski, Maciej Kierepa, Agata Kowala-Piaskowska, Arleta Mozer-Lisewska, Iwona
Published in
Archivum Immunologiae et Therapiae Experimentalis
Pattern recognition receptors (PRRs) are members of innate immunity, playing pivotal role in several immunological reactions. They are known to act as a bridge between innate and adaptive immunity. They are expressed on several normal cell types but have been shown with increasing frequency on/in tumor cells. Significance of this phenomenon is larg...
Wold, Eric A. Wild, Christopher T. Cunningham, Kathryn A. Zhou, Jia
Published in
Current topics in medicinal chemistry
Serotonin (5-HT) 5-HT2C receptor (5-HT2CR) is recognized as a critical mediator of disease-related pathways and behaviors based upon actions in the central nervous system (CNS). Since 5-HT2CR is a class A G protein-coupled receptor (GPCR), drug discovery efforts have traditionally pursued the activation of the receptor through synthetic ligands wit...
Milienne-Petiot, Morgane Higa, Kerin K Grim, Andrea Deben, Debbie Groenink, Lucianne Twamley, Elizabeth W Geyer, Mark A Young, Jared W
Published in
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology
Cognitive impairments, e.g., reward learning, are present in various psychiatric disorders and warrant treatment. Improving reward-related learning could synergistically enhance psychosocial treatments and cognition generally. A critical first step is to understand the mechanisms underlying reward learning. The dopamine system has been implicated i...
Lebedeva, Ekaterina Bagaev, Alexander Pichugin, Alexey Chulkina, Marina Lysenko, Andrei Tutykhina, Irina Shmarov, Maxim Logunov, Denis Naroditsky, Boris Ataullakhanov, Ravshan
...
Published in
BMC Immunology
BackgroundAgonists of TLR3 and TLR4 are effective immunoadjuvants for different types of vaccines. The mechanisms of their immunostimulatory action differ significantly; these differences are particularly critical for immunization with non-replicating adenovirus vectors (rAds) based vaccines. Unlike traditional vaccines, rAd based vaccines are not ...
Badshah, Syed Lal Ullah, Asad Al-showiman, Salim S. Mabkhot, Yahia Nasser
Published in
Chemistry Central Journal
This commentary highlights the recent work published in journal Nature on the structural based discovery of novel analgesic compounds for opioid receptors with minimal effects. Manglik et al. selectively targeted the Gi based μOR pathway instead of the β-arrestin pathway of the opioids. The computational screening of millions of compounds showed a ...
Hu, Xueping Yin, Bin Cappelle, Kaat Swevers, Luc Smagghe, Guy Yang, Xinling Zhang, Li
Krasavin, Mikhail Lukin, Alexey Bagnyukova, Daria Zhurilo, Nikolay Zahanich, Ihor Zozulya, Sergey
Published in
Journal of enzyme inhibition and medicinal chemistry
A series of nine compounds based on 3-[4-(benzyloxy)phenyl]propanoic acid core containing a 1-oxa-9-azaspiro[5.5]undecane periphery was designed, synthesized and evaluated as free fatty acid 1 (FFA1 or GPR40) agonists. The spirocyclic appendages included in these compounds were inspired by LY2881835, Eli Lilly's advanced drug candidate for type II ...
