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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
It is shown that a novel small molecule inhibitor of the BET family, GSK1210151A (I-BET151), has profound efficacy against human and murine MLL-fusion leukaemic cell lines, through the induction of early cell cycle arrest and apoptosis, establishing the displacement of BET proteins from chromatin as a promising epigenetic therapy for these aggressive leukaemias.
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
- C. Reavill, S. Taylor, J. Hagan
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 September 2000
The effect of SB-277011-A on isolation-induced prepulse inhibition deficit suggests that blockade of dopamine D(3) receptors may benefit the treatment of schizophrenia.
Characterization of SB‐269970‐A, a selective 5‐HT7 receptor antagonist
A role for 5‐HT7 receptor stimulation in 5‐CT induced hypothermia in guinea‐pigs is suggested, and time spent in Paradoxical Sleep (PS) during the first 3 h of EEG recording in conscious rats is significantly reduced.
Orexin-A, an hypothalamic peptide with analgesic properties
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.
Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Toward an improved prediction of human in vivo brain penetration
- S. Summerfield, A. Lucas, A. Ruffo
- BiologyXenobiotica; the fate of foreign compounds in…
- 21 November 2008
Examination of two of the major influences on the extent of brain penetration across species, namely plasma protein binding and brain tissue binding, suggest that passive diffusion across the blood–brain barrier is an important process for many drugs in humans and highlights the possibility for improved prediction of brain Penetration across species.