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The Immune Modulator FTY720 Targets Sphingosine 1-Phosphate Receptors*
The results suggest that FTY720, after phosphorylation, acts through sphingosine 1-phosphate signaling pathways to modulate chemotactic responses and lymphocyte trafficking. Expand
SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile.
A novel short synthetic SRIF peptidomimetic, which exhibits high affinity binding to four of the five human SRIF receptor subtypes and has potent, long lasting inhibitory effects on GH and IGF-I release, is identified. Expand
Opportunities in somatostatin research: biological, chemical and therapeutic aspects
Recent advances in SRIF biology, the chemistry of SRIF agonists and antagonists, and the therapeutic potential of such compounds in a wide range of established and novel indications are reviewed. Expand
Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site
Targeting of the statin-binding site of LFA-1 could be used to treat diseases such as psoriasis, rheumatoid arthritis, ischemia/reperfusion injury and transplant rejection. Expand
The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate
The immunomodulatory potential of BAF312 and the S1P receptor‐mediated effects on heart rate are characterized using preclinical and human data. Expand
Somatostatin analogue octreotide and inhibition of tumour growth in metastatic endocrine gastroenteropancreatic tumours.
The results suggest that octreotide inhibits tumour growth in patients with metastasised endocrine GEP tumours and the antiproliferative effect is, at least in some patients, longlasting. Expand
The multi-ligand somatostatin analogue SOM230 inhibits ACTH secretion by cultured human corticotroph adenomas via somatostatin receptor type 5.
The preferential inhibition of ACTH release by human corticotroph adenoma cells by SOM230 in vitro, suggest that SOM230 may have potential in the treatment of patients with pituitary-dependent Cushing's disease. Expand
[111In-DTPA-D-Phe1]-octreotide, a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumors: synthesis, radiolabeling and in vitro validation.
Results suggest that [111In-DTPA-D-Phe1]-octreotide is a promising radiopharmaceutical for scintigraphic imaging of somatostatin receptor-positive tumors. Expand
A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis.
NIBR-0213 showed comparable therapeutic efficacy to fingolimod in experimental autoimmune encephalomyelitis (EAE), a model of human MS, providing convincing evidence that S1P(1) antagonists are effective in EAE. Expand
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.
A rational drug design approach, capitalizing on structure-activity relationships and involving transposition of functional groups from somatotropin release inhibitory factor (SRIF) into a reducedExpand