• Publications
  • Influence
Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors.
TLDR
Cinacalcet is the first allosteric GPCR modulator to enter the market, which demonstrates that the therapeutic principle of allosterics modulation can also be extended to this important drug target class. Expand
The Agonist-binding Domain of the Calcium-sensing Receptor Is Located at the Amino-terminal Domain*
TLDR
A chimeric receptor named Ca/1a is constructed consisting of the ATD of CaR and the seven transmembrane region and C terminus of mGlu1a, which demonstrates that Ser-170 and to some extent Ser-147 are involved in the Ca2+ activation of the CaR, and reveals a close resemblance of the activation mechanism between the CaGlu receptors. Expand
Excitatory amino acid transporters as potential drug targets
TLDR
Not until subtype-selective enhancers, inhibitors and substrates for all five EAAT subtypes have been discovered can a full and detailed understanding of EAATs be obtained, so collaboration between organic chemists and molecular pharmacologists, together, may pave the way for new EAAT ligands of importance. Expand
Allosteric Modulation of the Calcium-Sensing Receptor
TLDR
The recent approval of the calcimimetic cinacalcet for the treatment of certain forms of primary and secondary hyperparathyroidism constitutes an important proof-of-concept for future development of allosteric modulators on other GPCR drug targets. Expand
The four human gamma-aminobutyric acid (GABA) transporters: pharmacological characterization and validation of a highly efficient screening assay.
TLDR
It is found that the [3H]GABA uptake assay is categorized by high Z'-factors (Z' > 0.5) for all four GAT subtypes, demonstrating that the assay is excellent for a high throughput screen, and enables future high throughput screening of compound libraries at the four human GATs. Expand
Cloning and Characterization of a Functional Human γ-Aminobutyric Acid (GABA) Transporter, Human GAT-2*
TLDR
The finding of the human GAT-2 demonstrates for the first time that the four plasma membrane GABA transporters identified in several mammalian species are all conserved in human and enables the use of all human clones of the GABA transporter in drug development programs and functional characterization of novel inhibitors of GABA transport. Expand
Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors
TLDR
A detailed electrophysiological characterization of NS9283 is presented, a potent positive allosteric modulator acting selectively at 3α:2β stoichiometry of α2* and α4* nAChRs. Expand
No evidence for a bone phenotype in GPRC6A knockout mice under normal physiological conditions.
TLDR
The data do not support a role for GPRC6A in normal bone physiology, and assessment of bone mineral density, histomorphometry, and bone metabolism demonstrated no significant differences between 13-week-old knockout and wild-type mice. Expand
Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay.
TLDR
The FMP assay was capable of distinguishing between substrates and non-substrate inhibitors and to discriminate between "full" and "partial" substrates at the transporters, and it is proposed that the assay will be of great use in future studies of thetransporters. Expand
...
1
2
3
4
5
...