The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]
, 2013 G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D. +2 more
core +1 more source
TRP Channels as Drug Targets to Relieve Itch
Pharmaceuticals, 2018 Although acute itch has a protective role by removing irritants to avoid further damage, chronic itch is debilitating, significantly impacting quality of life.
Zili Xie, Hongzhen Hu
doaj +1 more source
A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias [PDF]
, 2017 Free Fatty Acid Receptor 2 is a GPCR activated by short chain fatty acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates.
Aoki, Junken +9 more
core +3 more sources
The state-of-the-art of emergency contraception with the cutting edge drug
GMS German Medical Science, 2011 The objective of this study is to evaluate and elucidated the potential of selective progesterone receptor modulators (SPRMs) to be an effective emergency contraception (EC). The data are extracted from the literature through the MEDLINE database service
Sarkar, Narendra Nath
doaj
An opioid-like system regulating feeding behavior in C. elegans [PDF]
, 2015 Neuropeptides are essential for the regulation of appetite. Here we show that neuropeptides could regulate feeding in mutants that lack neurotransmission from the motor neurons that stimulate feeding muscles. We identified nlp-24 by an RNAi screen of 115
Artyukhin, Alexander B. +3 more
core +3 more sources
Could dopamine agonists aid in drug development for anorexia nervosa? [PDF]
, 2014 Anorexia nervosa is a severe psychiatric disorder most commonly starting during the teenage-years and associated with food refusal and low body weight. Typically there is a loss of menses, intense fear of gaining weight, and an often delusional quality ...
Frank, Guido KW
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Structure of human GPR119-Gs complex binding APD597 and characterization of GPR119 binding agonists
Frontiers in PharmacologyThe rhodopsin-like receptor GPR119 plays a crucial role in glucose homeostasis and is an emerging target for the treatment of type 2 diabetes mellitus. In this study, we analyzed the structure of GPR119 with the agonist APD597 bound and in complex with ...
Ruixue Li +6 more
doaj +1 more source
Frontiers in Physiology, 2018 Recently, two alternative targets in insect periphery nerve system have been explored for environmentally-friendly approaches in insect pest management, namely odorant-binding proteins (OBPs) and odorant receptors (ORs).
Herbert Venthur +3 more
doaj +1 more source
The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120) [PDF]
, 2014 The long-chain fatty acid receptor FFA4(previously GPR120) is receiving substantial interest as a novel target for the treatment of metabolic and inflammatory disease.
Hudson, Brian D. +3 more
core +1 more source
Cholinergic suppression: A postsynaptic mechanism of long-term associative learning [PDF]
, 1986 Food avoidance learning in the mollusc Pleurobranchaea entails reduction in the responsiveness of key brain interneurons in the feeding neural circuitry, the paracerebral feeding command interneurons (PCNs), to the neurotransmitter acetylcholine (AcCho).
Davis, W. Jackson +5 more
core +2 more sources