User profiles for Tarsis F. Brust
Tarsis BrustNeurocrine Biosciences Verified email at neurocrine.com Cited by 1404 |
Polydopamine-based simple and versatile surface modification of polymeric nano drug carriers
The surface of a polymeric nanoparticle (NP) is often functionalized with cell-interactive
ligands and/or additional polymeric layers to control NP interaction with cells and proteins. …
ligands and/or additional polymeric layers to control NP interaction with cells and proteins. …
Biased agonism: An emerging paradigm in GPCR drug discovery
G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors, G …
cellular proteins. The members of this large receptor gene family couple to primary effectors, G …
Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria
TF Brust, J Morgenweck, SA Kim, JH Rose, JL Locke… - Science …, 2016 - science.org
Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic
candidates because of their efficacy for treating intractable itch and relieving pain. Unlike typical …
candidates because of their efficacy for treating intractable itch and relieving pain. Unlike typical …
[HTML][HTML] A “Genome-to-Lead” Approach for Insecticide Discovery: Pharmacological Characterization and Screening of Aedes aegypti D1-like Dopamine Receptors
…, GI Giraldo-Calderón, TF Brust… - PLoS neglected …, 2012 - journals.plos.org
Background Many neglected tropical infectious diseases affecting humans are transmitted
by arthropods such as mosquitoes and ticks. New mode-of-action chemistries are urgently …
by arthropods such as mosquitoes and ticks. New mode-of-action chemistries are urgently …
Physiological roles of mammalian transmembrane adenylyl cyclase isoforms
KF Ostrom, JE LaVigne, TF Brust… - Physiological …, 2022 - journals.physiology.org
Adenylyl cyclases (ACs) catalyze the conversion of ATP to the ubiquitous second messenger
cAMP. Mammals possess nine isoforms of transmembrane ACs, dubbed AC1–9, that serve …
cAMP. Mammals possess nine isoforms of transmembrane ACs, dubbed AC1–9, that serve …
Gαi/o-coupled receptor-mediated sensitization of adenylyl cyclase: 40 years later
Heterologous sensitization of adenylyl cyclase (also referred to as superactivation, sensitization,
or supersensitization of adenylyl cyclase) is a cellular adaptive response first described …
or supersensitization of adenylyl cyclase) is a cellular adaptive response first described …
Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties
TF Brust, D Alongkronrusmee, M Soto-Velasquez… - Science …, 2017 - science.org
Adenylyl cyclase 1 (AC1) belongs to a group of adenylyl cyclases (ACs) that are stimulated
by calcium in a calmodulin-dependent manner. Studies with AC1 knockout mice suggest that …
by calcium in a calmodulin-dependent manner. Studies with AC1 knockout mice suggest that …
Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways
G protein–coupled receptors (GPCRs) often activate multiple signaling pathways, and ligands
may evoke functional responses through individual pathways. These unique responses …
may evoke functional responses through individual pathways. These unique responses …
New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling
The dopamine D 2 receptor (DRD2) is a G protein-coupled receptor (GPCR) that is generally
considered to be a primary target in the treatment of schizophrenia. First generation …
considered to be a primary target in the treatment of schizophrenia. First generation …
Bisamidate Prodrugs of 2‐Substituted 9‐[2‐(Phosphonomethoxy) ethyl] adenine (PMEA, adefovir) as Selective Inhibitors of Adenylate Cyclase Toxin from Bordetella …
…, M Dračínský, TF Brust, P Pávek, F Trejtnar… - …, 2015 - Wiley Online Library
Novel small‐molecule agents to treat Bordetella pertussis infections are highly desirable, as
pertussis (whooping cough) remains a serious health threat worldwide. In this study, a …
pertussis (whooping cough) remains a serious health threat worldwide. In this study, a …