Essential role for cholesterol in entry of mycobacteria into macrophages

J Gatfield, J Pieters - Science, 2000 - science.org
Mycobacteria are intracellular pathogens that can invade and survive within host
macrophages, thereby creating a major health problem worldwide. The molecular mechanisms …

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

…, C Binkert, K Morrison, W Fischli, J Gatfield… - … of Pharmacology and …, 2008 - ASPET
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N′-propylaminosulfonamide],
is a new dual ET A /ET …

Ancestral antibiotic resistance in Mycobacterium tuberculosis

RP Morris, L Nguyen, J Gatfield… - Proceedings of the …, 2005 - National Acad Sciences
Chemotherapeutic options to treat tuberculosis are severely restricted by the intrinsic
resistance of Mycobacterium tuberculosis to the majority of clinically applied antibiotics. Such …

[HTML][HTML] Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells

J Gatfield, C Mueller Grandjean, T Sasse, M Clozel… - 2012 - journals.plos.org
Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently
approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease …

2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1 Receptor Agonists

…, R Bravo, S Buchmann, D Bur, J Gatfield… - Journal of medicinal …, 2010 - ACS Publications
Sphingosine-1-phosphate (S1P) is a widespread lysophospholipid which displays a wealth
of biological effects. Extracellular S1P conveys its activity through five specific G-protein …

Regulation of T cell survival through coronin-1–mediated generation of inositol-1, 4, 5-trisphosphate and calcium mobilization after T cell receptor triggering

…, B Combaluzier, I Albrecht, J Gatfield… - Nature …, 2008 - nature.com
T cell homeostasis is essential for the functioning of the vertebrate immune system, but the
intracellular signals required for T cell homeostasis are largely unknown. We here report that …

Evaluation of tert‐Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities

…, BT Wolfstädter, JM Plancher, J Gatfield… - …, 2015 - Wiley Online Library
The tert‐butyl group is a common motif in medicinal chemistry. Its incorporation into bioactive
compounds is often accompanied by unwanted property modulation, such as increased …

Association of the leukocyte plasma membrane with the actin cytoskeleton through coiled coil-mediated trimeric coronin 1 molecules

J Gatfield, I Albrecht, B Zanolari… - Molecular biology of …, 2005 - Am Soc Cell Biol
Coronin 1 is a member of the coronin protein family specifically expressed in leukocytes and
accumulates at sites of rearrangements of the F-actin cytoskeleton. Here, we describe that …

Hijacking the host: survival of pathogenic mycobacteria inside macrophages

J Pieters, J Gatfield - Trends in microbiology, 2002 - cell.com
Mycobacteria are among the most persistent pathogens known today: one-third of the
global population is latently infected with Mycobacterium tuberculosis, an organism that is …

Selexipag: an oral and selective IP prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension

T Asaki, K Kuwano, K Morrison, J Gatfield, T Hamamoto… - 2015 - ACS Publications
Prostacyclin controls cardiovascular function via activation of the prostacyclin receptor.
Decreased prostacyclin production occurs in several cardiovascular diseases. However, the …