A–C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions [PDF]
Estrogen receptor-beta (ERβ) is a drug target for memory consolidation in postmenopausal women. Herein is reported a series of potent and selective ERβ agonists (SERBAs) with in vivo efficacy that are A–C estrogens, lacking the B and D estrogen rings ...
Donaldson, William A. +12 more
core +4 more sources
Structural and Functional Insights into CRF Peptides and Their Receptors
Corticotropin-releasing factor or hormone (CRF or CRH) and the urocortins regulate a plethora of physiological functions and are involved in many pathophysiological processes.
Minos-Timotheos Matsoukas +5 more
doaj +1 more source
Similarity-based virtual screening using 2D fingerprints [PDF]
This paper summarises recent work at the University of Sheffield on virtual screening methods that use 2D fingerprint measures of structural similarity. A detailed comparison of a large number of similarity coefficients demonstrates that the well-known ...
Willett, P.
core +1 more source
Atopic dermatitis (AD) is an immune-mediated inflammatory dermatosis characterized by epidermal barrier dysfunction, immune dysregulation, and cutaneous microbial dysbiosis.
Yuting Bao +7 more
doaj +1 more source
Beta-agonist stimulation ameliorates the phenotype of spinal and bulbar muscular atrophy mice and patient-derived myotubes [PDF]
Spinal and bulbar muscular atrophy (SBMA) is a neuromuscular disease characterized by the loss of lower motor neurons. SBMA is caused by expansions of a polyglutamine tract in the gene coding for androgen receptor (AR).
Blaauw, Bert +18 more
core +3 more sources
Historical narratives of conflict typically revolve around heroes and villains or perpetrators and victims. However, this dichotomy of events and people into good and evil greatly reduces the extent to which the past can be analysed, explained, and understood.
De Angeli, Daniela +4 more
openaire +1 more source
Novel 2-amino-isoflavones exhibit aryl hydrocarbon receptor agonist or antagonist activity in a species/cell-specific context [PDF]
The aryl hydrocarbon receptor (AhR) mediates the induction of a variety of xenobiotic metabolism genes. Activation of the AhR occurs through binding to a group of structurally diverse compounds, most notably dioxins, which are exogenous ligands ...
BALBONI, GIANFRANCO +10 more
core +1 more source
Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David +17 more
core +1 more source
In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
Dynaflow ™ 48, a microfluidic chip solution for increasing throughput and data quality in patch-clamp-based drug screening [PDF]
Ion channels are transm embrane proteins, found in virtually all cell types throughout the human body. Ion channels underlie neural communication, memory, behavior, every movement and heartbeat, and are as such prone to cause disease if malfunctioning.
Granfeldt, Daniel +4 more
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