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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
Recurrent chromosomal translocations involving the mixed lineage leukaemia (MLL) gene initiate aggressive forms of leukaemia, which are often refractory to conventional therapies. Many MLL-fusionExpand
Inhibition of BET Recruitment to Chromatin As An Effective Treatment for MLL-Fusion Leukaemia
Abstract 55 Recurrent chromosomal translocations involving the mixed lineage leukaemia (MLL) gene initiate aggressive forms of leukaemia, which confer a poor prognosis and are often refractory toExpand
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
SB-277011-A (trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolininecarboxamide), is a brain-penetrant, high-affinity, and selective dopamine D(3) receptorExpand
Characterization of SB‐269970‐A, a selective 5‐HT7 receptor antagonist
The novel 5‐HT7 receptor antagonist, SB‐269970‐A, potently displaced [3H]‐5‐CT from human 5‐HT7(a) (pKi 8.9±0.1) and 5‐HT7 receptors in guinea‐pig cortex (pKi 8.3±0.2). 5‐CT stimulated adenylylExpand
Orexin-A, an hypothalamic peptide with analgesic properties
&NA; The hypothalamic peptide orexin‐A and the orexin‐1 receptor are localized in areas of the brain and spinal cord associated with nociceptive processing. In the present study, localization wasExpand
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
The bromo and extra C-terminal domain (BET) family of bromodomains are involved in binding epigenetic marks on histone proteins, more specifically acetylated lysine residues. This paper describes theExpand
Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.
The selective, brain penetrant, 5-HT(1B/D) (formerly 5-HT(1D beta/alpha)) receptor agonist SKF-99101H (3-(2-dimethylaminoethyl)-4-chloro-5-propoxyindole hemifumarate) (30 mg/kg i.p.) causes a doseExpand
The Practice of Medicinal Chemistry
Toward an improved prediction of human in vivo brain penetration
The penetration of drugs into the central nervous system is a composite of both the rate of drug uptake across the blood–brain barrier and the extent of distribution into brain tissue compartments.Expand
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