Molecular mechanism of 7TM receptor activation—a global toggle switch model

TW Schwartz, TM Frimurer, B Holst… - Annu. Rev …, 2006 - annualreviews.org
… -III constitutes a central, highly tilted rod in the 7TM receptor structure as it reaches from
the extracellular end of TM-II to the intracellular end of TM-V, with TM-IV being located as a …

Ligand binding and micro-switches in 7TM receptor structures

R Nygaard, TM Frimurer, B Holst… - Trends in …, 2009 - cell.com
… (TM-I to TM-VII) and helix VII in addition to the extracellular loops (ECL) highlighted. The highly
conserved disulfide bridge from the extracellular end of TM-… ’ see-saw movement of TM-VI …

The minor binding pocket: a major player in 7TM receptor activation

MM Rosenkilde, T Benned-Jensen, TM Frimurer… - Trends in …, 2010 - cell.com
… is defined by a highly conserved kink in TM-II that is induced by a … TM-II and TM-VII being
of particular significance. Importantly, the minor binding pocket, especially the proline-kink in TM

[HTML][HTML] GPR40 (FFAR1)–combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

…, M Lückmann, MW Miller, ME Trujillo, TM Frimurer… - Molecular …, 2015 - Elsevier
… anchor point, ie an elongated pocket extending between TM-III and TM-VII over towards
TM-I and TM-II (pocket#3) and a smaller pocket located between TM-V, -VI and -VII (pocket #4). …

[PDF][PDF] Extracellular succinate hyperpolarizes M2 macrophages through SUCNR1/GPR91-mediated Gq signaling

…, B Breton, AS Husted, SA Hjorth, A Inoue, TM Frimurer… - Cell reports, 2021 - cell.com
Succinate functions both as a classical TCA cycle metabolite and an extracellular metabolic
stress signal sensed by the mainly Gi-coupled succinate receptor SUCNR1. In the present …

[HTML][HTML] A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors 2

…, MS Engelstoft, PS Petersen, TM Frimurer… - Journal of Biological …, 2010 - ASBMB
The conserved tryptophan in position 13 of TM-VI (Trp-VI:13 or Trp-6.48) of the CWXP motif
located at the bottom of the main ligand-binding pocket in TM-VI is believed to function as a …

Improving the odds in discriminating “drug-like” from “non drug-like” compounds

TM Frimurer, R Bywater, L Nĉrum… - Journal of chemical …, 2000 - ACS Publications
We have used a feed-forward neural network technique to classify chemical compounds
into potentially “drug-like” and “non drug-like” candidates. The neural network was trained to …

Ghrelin receptor inverse agonists: identification of an active peptide core and its interaction epitopes on the receptor

…, M Lang, E Brandt, A Bach, A Howard, TM Frimurer… - Molecular …, 2006 - ASPET
TM-III, TM-VI, and TM-VII (ie, where the ghrelin hits are found in the present study) (Elling et
al., 1999, 2006; Buck and Wells, 2005). In the case of the relatively large ghrelin peptide, we …

[HTML][HTML] Biosynthesis of natural and halogenated plant monoterpene indole alkaloids in yeast

…, L Ding, Y Qiao, TM Frimurer… - Nature Chemical …, 2023 - nature.com
Monoterpenoid indole alkaloids (MIAs) represent a large class of plant natural products with
marketed pharmaceutical activities against a wide range of indications, including cancer, …

Electrostatic Evaluation of the Signature Motif (H/V)CX5R(S/T) in Protein−Tyrosine Phosphatases

GH Peters, TM Frimurer, OH Olsen - Biochemistry, 1998 - ACS Publications
The catalytic activity of protein−tyrosine phosphatases (PTPs) is mediated by a cysteine
side chain which carries out a nucleophilic attack initiating the phosphate cleavage. …