Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.

We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure-activity relationship of the high-throughput screening (HTS) lead compound provided potent and selective SMYD3 inhibitors. The SAR optimization, cocrystal structures of small molecules with SMYD3, and mode of inhibition (MOI) characterization of compounds are described.

Predators of monarch butterfly eggs and neonate larvae are more diverse than previously recognised.

Conserving threatened organisms requires knowledge of the factors impacting their populations. The Eastern monarch butterfly (Danaus plexippus L.) has declined by as much as 80% in the past two decades and conservation biologists are actively seeking to understand and reverse this decline.

Insurance-mandated preoperative diet and outcomes after bariatric surgery.

Background: Despite a lack of demonstrated patient benefit, many insurance providers mandate a physician-supervised diet before financial coverage for bariatric surgery.

Objectives: To compare weight loss between patients with versus without insurance mandating a preoperative diet.

Setting: University hospital, United States.

Outcomes associated with preoperative weight loss after laparoscopic Roux-en-Y gastric bypass.

Background: Laparoscopic Roux-en-Y gastric bypass (LRYGB) is an effective treatment for achieving and maintaining weight loss and for improving obesity-related comorbidities. As part of the approval process for bariatric surgery, many insurance companies require patients to have documented recent participation in a supervised weight loss program. The goal of this study was to evaluate the relationship of preoperative weight changes with outcomes following LRYGB.