Application of combinatorial chemistry science on modern drug discovery
JP Kennedy, L Williams, TM Bridges… - Journal of …, 2008 - ACS Publications
The science that established combinatorial chemistry as important new discipline in the
1980s and 1990s has re-emerged and infiltrated every sub-discipline within modern drug …
1980s and 1990s has re-emerged and infiltrated every sub-discipline within modern drug …
G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms
TM Bridges, CW Lindsley - ACS chemical biology, 2008 - ACS Publications
… GPCRs all have a common core composed of seven transmembrane helices (the 7TM domain
composed of TM-I−TM-VII) with an extracellular N-terminal domain and an intracellular C-…
composed of TM-I−TM-VII) with an extracellular N-terminal domain and an intracellular C-…
Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors
…, KA Emmitte, CR Hopkins, TM Bridges… - Chemical …, 2016 - ACS Publications
… A positive allosteric modulator of the GABA B receptor, termed CGP7930 (17), has been
shown to bind within the GABA B2 TM domain to potentiate the effects of GABA. (119) As the …
shown to bind within the GABA B2 TM domain to potentiate the effects of GABA. (119) As the …
Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats
…, MN Tantawy, AS Kane, TM Bridges… - Journal of …, 2008 - Soc Neuroscience
Recent studies suggest that subtype-selective activators of M 1 /M 4 muscarinic acetylcholine
receptors (mAChRs) may offer a novel approach for the treatment of psychotic symptoms …
receptors (mAChRs) may offer a novel approach for the treatment of psychotic symptoms …
A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in …
…, PJ Jones, AA Davis, TM Bridges… - Journal of …, 2009 - Soc Neuroscience
M 1 muscarinic acetylcholine receptors (mAChRs) may represent a viable target for treatment
of disorders involving impaired cognitive function. However, a major limitation to testing …
of disorders involving impaired cognitive function. However, a major limitation to testing …
Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats
Previous clinical and animal studies suggest that selective activators of M 1 and/or M 4
muscarinic acetylcholine receptors (mAChRs) have potential as novel therapeutic agents for …
muscarinic acetylcholine receptors (mAChRs) have potential as novel therapeutic agents for …
Split‐face comparison of photodynamic therapy with 5‐aminolevulinic acid and intense pulsed light versus intense pulsed light alone for photodamage
…, VL Bradshaw, MM Boring, TM Bridges… - Dermatologic …, 2006 - Wiley Online Library
BACKGROUND Photodynamic therapy (PDT) with a 5‐aminolevulinic acid (ALA)
photosensitizing agent and a variety of lasers and light sources has been shown to enhance the …
photosensitizing agent and a variety of lasers and light sources has been shown to enhance the …
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity
JE Marlo, CM Niswender, EL Days, TM Bridges… - Molecular …, 2009 - ASPET
Activators of M 1 muscarinic acetylcholine receptors (mAChRs) may provide novel treatments
for schizophrenia and Alzheimer's disease. Unfortunately, the development of M 1 -active …
for schizophrenia and Alzheimer's disease. Unfortunately, the development of M 1 -active …
Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents
Positive allosteric modulators (PAMs) of the M 4 muscarinic acetylcholine receptor (mAChR)
represent a novel approach for the treatment of psychotic symptoms associated with …
represent a novel approach for the treatment of psychotic symptoms associated with …
A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning
DJ Sheffler, R Williams, TM Bridges, Z Xiang… - Molecular …, 2009 - ASPET
Previous studies suggest that selective antagonists of specific subtypes of muscarinic
acetylcholine receptors (mAChRs) may provide a novel approach for the treatment of certain …
acetylcholine receptors (mAChRs) may provide a novel approach for the treatment of certain …