Results 51 to 60 of about 7,381 (220)

Evidence that 5‐HT2A receptor signalling efficacy and not biased agonism differentiates serotonergic psychedelic from non‐psychedelic drugs

British Journal of Pharmacology, EarlyView.
Background and Purpose Serotonergic psychedelic drugs are under investigation as therapies for various psychiatric disorders, including major depression. Although serotonergic psychedelic drugs are 5‐HT2A receptor agonists, some such agonists are not psychedelic, potentially due to differences in 5‐HT2A receptor ligand bias or signalling efficacy. Here,
Aurelija Ippolito, Sridhar Vasudevan, Shaun Hurley, Gary Gilmour, Frederick Westhorpe, Grant Churchill, Trevor Sharp   +6 more
wiley   +1 more source

PARP inhibitors: polypharmacology versus selective inhibition [PDF]

The FEBS Journal, 2013
Inhibition of ADP‐ribosyltransferases with diphtheria toxin homology (ARTD), widely known as the poly(ADP‐ribose) polymerase (PARP) family, is a strategy under development for treatment of various conditions, including cancers and ischemia. Here, we give a brief summary of ARTD enzyme functions and the implications for their potential as therapeutic ...
Torun Ekblad, CAMAIONI, Emidio, Herwig Schüler, MACCHIARULO, Antonio   +3 more
openaire   +2 more sources

Chemoinformatic Database Building and in Silico Hit-Identification of Potential Multi-Targeting Bioactive Compounds Extracted from Mushroom Species

Molecules, 2017
Mushrooms are widely-consumed fungi which contain natural compounds that can be used both for their nutritive and medicinal properties, i.e., taking advantage of their antimicrobial, antiviral, antitumor, anti-allergic, immunomodulation, anti ...
Annalisa Maruca, Federica Moraca, Roberta Rocca, Fulvia Molisani, Francesca Alcaro, Maria Concetta Gidaro, Stefano Alcaro, Giosuè Costa, Francesco Ortuso   +8 more
doaj   +1 more source

A New Quantitative Cell-Based Assay Reveals Unexpected Microtubule Stabilizing Activity of Certain Kinase Inhibitors, Clinically Approved or in the Process of Approval

Frontiers in Pharmacology, 2020
Agents able to modify microtubule dynamics are important anticancer drugs. The absence of microtubules resulting from drug-induced depolymerization is easy to detect.
Sacnicte Ramirez-Rios, Sophie Michallet, Leticia Peris, Caroline Barette, Clotilde Rabat, Yangbo Feng, Marie-Odile Fauvarque, Annie Andrieux, Karin Sadoul, Laurence Lafanechère   +9 more
doaj   +1 more source

Exploring Protein-Protein Interactions as Drug Targets for Anti-cancer Therapy with In Silico Workflows [PDF]

, 2017
We describe a computational protocol to aid the design of small molecule and peptide drugs that target protein-protein interactions, particularly for anti-cancer therapy. To achieve this goal, we explore multiple strategies, including finding binding hot
A Goncearenco, A Goncearenco, A Marchler-Bauer, A Truszkowski, AA Bogan, B Graves, B Ma, BA Shoemaker, BA Shoemaker, BA Shoemaker, BJ Smith, CA Goble, CM Yates, D Petrey, E Cukuroglu, FP Davis, H Perez-Sanchez, HS Haase, J Bhagat, J Cinatl, JA Wells, K Wolstencroft, M Guharoy, M Li, M Li, M Li, M Petukh, M Tyagi, MK Gilson, MP Mazanetz, N Estrada-Ortiz, P Aloy, P Aloy, P Filippakopoulos, R Mosca, RR Thangudu, S Beisken, S Kim, S Shangary, S Teng, T Rolland, W Yang, WS Valdar, Y Wang, Y Zhao   +44 more
core   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Utility of the Biosynthetic Folate Pathway for Targets in Antimicrobial Discovery

Antibiotics, 2014
The need for new antimicrobials is great in face of a growing pool of resistant pathogenic organisms. This review will address the potential for antimicrobial therapy based on polypharmacological activities within the currently utilized bacterial ...
Christina R. Bourne
doaj   +1 more source

Unveiling the Multitarget Anti-Alzheimer Drug Discovery Landscape: A Bibliometric Analysis

Pharmaceuticals, 2022
Multitarget anti-Alzheimer agents are the focus of very intensive research. Through a comprehensive bibliometric analysis of the publications in the period 1990–2020, we have identified trends and potential gaps that might guide future directions.
Anna Sampietro, F. Javier Pérez-Areales, Paula Martínez, Elsa M. Arce, Carles Galdeano, Diego Muñoz-Torrero   +5 more
doaj   +1 more source

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. [PDF]

, 2008
The clinical success of multitargeted kinase inhibitors has stimulated efforts to identify promiscuous drugs with optimal selectivity profiles. It remains unclear to what extent such drugs can be rationally designed, particularly for combinations of ...
Aizenstein, Brian, Apsel, Beth, Blair, Jimmy A, Feldman, Morri E, Gonzalez, Beatriz, Hoffman, Randy, Knight, Zachary A, Nazif, Tamim M, Shokat, Kevan M, Williams, Roger L   +9 more
core  

Comprehensive transduceromic profiling of NOP receptor ligands at different Gα subunits

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) is an opioid receptor family member with distinct pharmacology and broad therapeutic potential. NOP receptors regulate functions such as nociception, stress reactivity, reward, mood, autonomic tone, immunity and sleep/wake cycle.
Davide Malfacini, Riccardo Camilotto, Michele Maritan, Erika Morrone, Stephen Afriyie Boateng, Anna Vacilotto, Salvatore Pacifico, Remo Guerrini, Nurulain T. Zaveri, Girolamo Calo'   +9 more
wiley   +1 more source