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Molecules, Vol. 26, Pages 7599: In Search of Small Molecules That Selectively Inhibit MBOAT4
trick G. Harran Ghrelin is a 28-residue peptide hormone produced by stomach P/D1 cells located in oxyntic glands of the fundus mucosa. Post-translational octanoylation of its Ser-3 residue, catalyzed by MBOAT4 (aka ghrelin O-acyl transferase (GOAT)), is essential for the binding of the hormone to its receptor in target tissues. Physiological roles of acyl ghrelin include the regulation of food intake, growth hormone secretion from the pituitary, and inhibition of insulin secretion from the pancreas. Here, we describe a medicinal chemistry campaign that led to the identification of small lipopeptidomimetics that inhibit...
Source: Molecules - December 15, 2021 Category: Chemistry Authors: Emily S. Murzinski Ishika Saha Hui Ding David Strugatsky Ryan A. Hollibaugh Haixia Liu Peter Tontonoz Patrick G. Harran Tags: Article Source Type: research

The Impact of Racial and Ethnic Health Disparities in Diabetes Management on Clinical Outcomes: A Reinforcement Learning Analysis of Health Inequity Among Youth and Young Adults in the SEARCH for Diabetes in Youth Study
CONCLUSIONSMathematically modeling an equalized distribution of T1D self-management tools and technology accounted for part of but not all disparities in glycemic control between non-White and White YYA, underscoring the complexity of race and ethnicity-based health inequity.
Source: Diabetes Care - November 2, 2021 Category: Endocrinology Source Type: research

Trends in Glycemic Control Among Youth and Young Adults With Diabetes: The SEARCH for Diabetes in Youth Study
CONCLUSIONSDespite advances in diabetes technologies, medications, and dissemination of more aggressive glycemic targets, many current YYA are less likely to achieve desired glycemic control relative to earlier cohorts.
Source: Diabetes Care - January 17, 2022 Category: Endocrinology Source Type: research

Elucidation of the Mechanisms Underlying the Rapid Antidepressant Actions of Ketamine and Search for Possible Candidates for Novel Rapid-acting Antidepressants
Yakugaku Zasshi. 2023;143(9):713-720. doi: 10.1248/yakushi.23-00111.ABSTRACTKetamine, an N-methyl-D-aspartate receptor antagonist, elicits swift antidepressant effects even in subjects with treatment-resistant depression. Nonetheless, owing to the serious adverse effects associated with ketamine, including psychotomimetic effects, the development of safer rapid-acting antidepressants is imperative. The elucidation of the mechanisms underlying the antidepressant effects of ketamine will facilitate the advancement of these alternative treatments. Previous preclinical studies have indicated that the antidepressant properties ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 4, 2023 Category: Drugs & Pharmacology Authors: Satoshi Deyama Source Type: research