Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 1380089-33-7, Name is (4-Bromo-3-methylisoxazol-5-yl)methyl acetate, molecular formula is C7H8BrNO3, 1380089-33-7, In a Article, authors is Nordqvist, Anneli£¬once mentioned of 1380089-33-7
Structure-Based Drug Design of Mineralocorticoid Receptor Antagonists to Explore Oxosteroid Receptor Selectivity
The mineralocorticoid receptor (MR) is a nuclear hormone receptor involved in the regulation of body fluid and electrolyte homeostasis. In this study we explore selectivity triggers for a series of nonsteroidal MR antagonists to improve selectivity over other members of the oxosteroid receptor family. A biaryl sulfonamide compound was identified in a high-throughput screening (HTS) campaign. The compound bound to MR with pKi=6.6, but displayed poor selectivity over the glucocorticoid receptor (GR) and the progesterone receptor (PR). Following X-ray crystallography of MR in complex with the HTS hit, a compound library was designed that explored an induced-fit hypothesis that required movement of the Met852 side chain. An improvement in MR selectivity of 11- to 79-fold over PR and 23- to 234-fold over GR was obtained. Given the U-shaped binding conformation, macrocyclizations were explored, yielding a macrocycle that bound to MR with pKi=7.3. Two protein?ligand X-ray structures were determined, confirming the hypothesized binding mode for the designed compounds.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.1380089-33-7. In my other articles, you can also check out more blogs about 1380089-33-7
Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem