Hoguet, Vanessa Lasalle, Manuel Maingot, Mathieu Dequirez, Geoffroy Boulahjar, Rajaa Leroux, Florence Piveteau, Catherine Herledan, Adrien Biela, Alexandre Dumont, Julie
...
PEGylation of therapeutic agents is known to improve the pharmacokinetic behavior of macromolecular drugs and nanoparticles. In this work, we performed the conjugation of polyethylene glycols (220-5000 Da) to a series of non-steroidal small agonists of the bile acids receptor TGR5. A suitable anchoring position on the agonist was identified to reta...
Balachandran, Subin Binitha, R. N.
Published in
In Silico Pharmacology
Antioxidant food additives were routinely used for increasing the keeping quality of packaged food items. Butylated Hydroxyanisole (BHA) is one of the most widely used synthetic phenolic antioxidants of such kind. Although quantity of antioxidants in packaged eatables and admissible daily intake (ADI) per person per day are limited by laws, the urb...
Liu, Jianfeng Wu, Ruyan Li, Jun-Xu
Published in
Cellular and molecular neurobiology
Trace amine-associated receptor 1 is one of the best-characterized receptors of trace amines. Growing evidence shows that TAAR1 negatively regulates the monoaminergic activity, including dopamine transmission in the mesocorticolimbic system. Neurochemical assays demonstrated that selective TAAR1 full and partial agonists were effective to prevent p...
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...
Martínez, Claudio Souto, José A de Lera, Angel R
Published in
Methods in molecular biology (Clifton, N.J.)
Retinoid X receptors (RXRs) are promiscuous partners of heterodimeric associations with other members of the Nuclear Receptor (NR) superfamily. RXR ligands ("rexinoids") either transcriptionally activate the "permissive" subclass of heterodimers or synergize with partner ligands in the "nonpermissive" subclass of heterodimers. The rationale for rex...
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...