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Crystal Structures and Structure-Activity Relationships of Imidazothiazole Derivatives as IDO1 Inhibitors.
TLDR
The crystal structures of two IDO1/IDO1 inhibitor complexes are reported, one of which shows that Amg-1 is directly bound to the heme iron of IDO2 with a clear induced fit, which is very valuable for understanding the mechanism of IDo1 activation.
Isolation and synthesis of TNF-alpha release inhibitors from Fijian kawa (Piper methysticum).
TLDR
5,6-Dehydrokawain (desmethoxyyangonin) and yangonin (4) significantly inhibited TNF-alpha release with IC50 values of 17 microM and 40 microM; a potency as great as (-)-epigallocatechin gallate (EGCG) isolated from green tea extract.
High-resolution NMR study of a GdAGA tetranucleotide loop that is an improved substrate for ricin, a cytotoxic plant protein.
TLDR
It appears that the 2'-hydroxyl group of adenosine at the depurination site (6A) does not participate in the recognition by ricin of the substrate, while the amino group of 7G is essential for substrate recognition the ricin A-chain.
Synthesis of possible metabolites of chlorpromazine. I. 7-hydroxy derivatives of chlorpromazine, nor1-chlorpromazine and nor2-chlorpromazine
The title compounds and various derivatives have been prepared as analytical standards for the identification of chlorpromazine metabolites in biological materials. Additional evidence is presented
Crystal structures of the catalytic domain of human stromelysin-1 (MMP-3) and collagenase-3 (MMP-13) with a hydroxamic acid inhibitor SM-25453.
TLDR
The results revealed that the binding modes for this inhibitor to MMP-3 and -13 were quite similar, however, subtle comparative differences were observed at the bottom of S1' pockets, which were occupied with the guanidinomethyl moiety of the inhibitor.
Catechin production in cultured Polygonum hydropiper cells
TLDR
The (+)-catechin production of suspension-cultured cells increased with cell growth and reached the maximal value (29.0 mg g −1 dry wt) after 6 days from the start of subculture, which is the highest value of (+)-Catechin content among reports on catechinProduction in vitro so far published.
Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.
TLDR
The sodium salt of 9 (9Na) demonstrated potent efficacy in lowering both blood glucose and lipids in an animal model without causing significant body weight gain, a well-known side effect associated with PPARγ full agonists.
Synthesis, structure and α-olefin polymerization activity of group 4 metal complexes with [OSSO]-type bis(phenolate) ligands
Abstract The tetradentate [OSSO]-type bis(phenol) ligands, [{2,2′-(HOC6H2-4,6-R2)2CH2SCH2CH2SCH2}] (R = tBu, 2; Br, 3) react with MBz4 (M = Zr, Hf) to yield the corresponding dibenzyl complexes,
Pharmacokinetics of 9α‐fluoromedroxyprogesterone acetate in rats: comparison with medroxyprogesterone acetate
TLDR
The physico‐chemical properties of FMPA and MPA and their pharmacokinetics in female rats were investigated and the free fraction ofFMPA in blood is estimated to be higher than that of MPA, which may explain the higher anti‐tumour activity.
Crystallization and preliminary X-ray crystallographic analysis of human phosphodiesterase 12.
Phosphodiesterase PDE12 is a medically important esterase-family member that hydrolyzes 2'-5'-linked oligoadenylates (2-5A), which are involved in the regulation of biological processes related to
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