Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.

The bromodomain and extra terminal (BET) family of bromodomain-containing proteins are important epigenetic regulators that elicit their effect through binding histone tail -acetyl lysine (KAc) post-translational modifications. Recognition of such markers has been implicated in a range of oncology and immune diseases and, as such, small-molecule inhibition of the BET family bromodomain-KAc protein-protein interaction has received significant interest as a therapeutic strategy, with several potential medicines under clinical evaluation. This work describes the structure- and property-based optimization of a ligand and lipophilic efficient pan-BET bromodomain inhibitor series to deliver candidate I-BET787 () that demonstrates efficacy in a mouse model of inflammation and suitable properties for both oral and intravenous (IV) administration.

Concurrent Exercise Training: Long-Term Changes in Body Composition and Motives for Continued Participation in Women with Obesity.

The purpose of this project was to examine the effect of a concurrent exercise program (sprint interval training and resistance exercise) on body composition in women with obesity and factors associated with continued exercise participation following the program. Twenty women (37.1 ± 7.

Adaptations to a Concurrent Exercise Training Program in Inactive Aging Women.

Wadsworth, DD, Rodriguez-Hernandez, M, Huffman, LS, McDonald, JR, Spring, KE, and Pascoe, DD. Adaptations to a concurrent exercise training program in inactive aging women. J Strength Cond Res 36(11): 3217-3223, 2022-This study assessed the effect of a 10-week, sprint interval concurrent exercise training program on body composition and muscular strength in aging women.

Functional Performance of Firefighters After Exposure to Environmental Conditions and Exercise.

Context: Slips, trips, and falls are leading causes of musculoskeletal injuries in firefighters. Researchers have hypothesized that heat stress is the major contributing factor to these fireground injuries.

Objective: To examine the effect of environmental conditions, including hot and ambient temperatures, and exercise on functional and physiological outcome measures, including balance, rectal temperature, and perceived exertion.

Ischemic preconditioning has no effect on maximal arm cycling exercise in women.

Purpose: We investigated the effect of ischemic preconditioning (IPC) on performance of a 3 min maximal effort arm ergometer test in young women.

Methods: Twenty healthy women (23.1 (SD 3.

Correction to: Ten weeks of branched-chain amino acid supplementation improves select performance and immunological variables in trained cyclists.

For the author R. Mac Thompson, the first name should be R. Mac and the last name should be Thompson.

Red Spinach Extract Increases Ventilatory Threshold during Graded Exercise Testing.

We examined the acute effect of a red spinach extract (RSE) (1000 mg dose; ~90 mg nitrate (NO 3 - )) on performance markers during graded exercise testing (GXT). For this randomized, double-blind, placebo (PBO)-controlled, crossover study, 15 recreationally-active participants (aged 23.1 ± 3.

Unilateral application of an external pneumatic compression therapy improves skin blood flow and vascular reactivity bilaterally.

Background: We sought to determine the effects of unilateral lower-limb external pneumatic compression (EPC) on bilateral lower-limb vascular reactivity and skin blood flow.

Methods: Thirty-two participants completed this two-aim study. In AIM1 ( = 18, age: 25.

Multiple Short Bouts of Walking Activity Attenuate Glucose Response in Obese Women.

Background: We sought to determine the effect of multiple walking breaks from sedentary behavior (SED) on glucose responses in sedentary obese women.

Materials And Methods: Ten women [aged = 36 (5) y, body mass index = 38.0 (1.

Concomitant external pneumatic compression treatment with consecutive days of high intensity interval training reduces markers of proteolysis.

Purpose: To compare the effects of external pneumatic compression (EPC) and sham when used concurrently with high intensity interval training (HIIT) on performance-related outcomes and recovery-related molecular measures.

Methods: Eighteen recreationally endurance-trained male participants (age: 21.6 ± 2.

Thermographic imaging in sports and exercise medicine: A Delphi study and consensus statement on the measurement of human skin temperature.

The importance of using infrared thermography (IRT) to assess skin temperature (t) is increasing in clinical settings. Recently, its use has been increasing in sports and exercise medicine; however, no consensus guideline exists to address the methods for collecting data in such situations. The aim of this study was to develop a checklist for the collection of t using IRT in sports and exercise medicine.

Molecular, neuromuscular, and recovery responses to light versus heavy resistance exercise in young men.

Recent evidence suggests that resistance training with light or heavy loads to failure results in similar adaptations. Herein, we compared how both training modalities affect the molecular, neuromuscular, and recovery responses following exercise. Resistance-trained males (mean ± SE: 22 ± 2 years, 84.

Effects of a pre-workout supplement on hyperemia following leg extension resistance exercise to failure with different resistance loads.

Background: We sought to determine if a pre-workout supplement (PWS), containing multiple ingredients thought to enhance blood flow, increases hyperemia associated with resistance training compared to placebo (PBO). Given the potential interaction with training loads/time-under-tension, we evaluated the hyperemic response at two different loads to failure.

Methods: Thirty males participated in this double-blinded study.

Effects of Whey, Soy or Leucine Supplementation with 12 Weeks of Resistance Training on Strength, Body Composition, and Skeletal Muscle and Adipose Tissue Histological Attributes in College-Aged Males.

We sought to determine the effects of L-leucine (LEU) or different protein supplements standardized to LEU (~3.0 g/serving) on changes in body composition, strength, and histological attributes in skeletal muscle and adipose tissue. Seventy-five untrained, college-aged males (mean ± standard error of the mean (SE); age = 21 ± 1 years, body mass = 79.

Effects of a Sprint Interval and Resistance Concurrent Exercise Training Program on Aerobic Capacity of Inactive Adult Women.

Salom Huffman, L, Wadsworth, DD, McDonald, JR, Foote, SJ, Hyatt, H, and Pascoe, DD. Effects of a sprint interval and resistance concurrent exercise training program on aerobic capacity of inactive adult women. J Strength Cond Res 33(6): 1641-1648, 2019-The purpose of this investigation was to examine the effects of high-intensity concurrent exercise training (CET) consisting of sprint intervals (sprint interval training [SIT]) and resistance exercise (RET) protocols on aerobic capacity in recreationally active, adult women.

Does external pneumatic compression treatment between bouts of overreaching resistance training sessions exert differential effects on molecular signaling and performance-related variables compared to passive recovery? An exploratory study.

Purpose: We sought to compare the effects of external pneumatic compression (EPC) and sham when used concurrently with resistance training on performance-related outcomes and molecular measures related to recovery.

Methods: Twenty (N = 20) resistance-trained male participants (aged 21.6±2.

Elementary School Teachers' Vocal Dose: Muscle Bioenergetics and Training Implications.

Purpose: Translating exercise-science methodology for determination of muscle bioenergetics, we hypothesized that the temporal voice-use patterns for classroom and music teachers would indicate a reliance on the immediate energy system for laryngeal skeletal-muscle metabolism. It was hypothesized that the music-teacher group would produce longer voiced segments than the classroom teachers.

Method: Using a between- and within-group multivariate analysis-of-variance design (5 classroom teachers; 7 music teachers), we analyzed fundamental-frequency data-collected via an ambulatory phonation monitor-for length (seconds) of voiced and nonvoiced intervals.

Impact of external pneumatic compression target inflation pressure on transcriptome-wide RNA expression in skeletal muscle.

Next-generation RNA sequencing was employed to determine the acute and subchronic impact of peristaltic pulse external pneumatic compression (PEPC) of different target inflation pressures on global gene expression in human vastus lateralis skeletal muscle biopsy samples. Eighteen (N = 18) male participants were randomly assigned to one of the three groups: (1) sham (n = 6), 2) EPC at 30-40 mmHg (LP-EPC; n = 6), and 3) EPC at 70-80 mmHg (MP-EPC; n = 6). One hour treatment with sham/EPC occurred for seven consecutive days.

Evaluation of Performance Improvements After Either Resistance Training or Sprint Interval-Based Concurrent Training.

Laird IV, RH, Elmer, DJ, Barberio, MD, Salom, LP, Lee, KA, and Pascoe, DD. Evaluation of performance improvements after either resistance training or sprint interval-based concurrent training. J Strength Cond Res 30(11): 3057-3065, 2016-The purpose of this investigation was to examine the effects of concurrent sprint interval and resistance training (CST) vs.

Differential vascular reactivity responses acutely following ingestion of a nitrate rich red spinach extract.

Introduction: Inorganic nitrate ingestion has been posited to affect arterial blood pressure and vascular function.

Purpose: We sought to determine the acute effect of a red spinach extract (RSE) high in inorganic nitrate on vascular reactivity 1-h after ingestion in peripheral conduit and resistance arteries.

Methods: Fifteen (n = 15; males 8, females 7) apparently healthy subjects (aged 23.

Inflammatory, lipid, and body composition responses to interval training or moderate aerobic training.

Purpose: The goal of this study was to compare the effect of work- and duration-matched interval training (HIIT) versus moderate aerobic endurance training (ET) on acute and chronic inflammation, along with changes in the lipid profile, to determine which may be more beneficial for improving cardiovascular health.

Methods: Twelve sedentary males (maximal oxygen consumption = 41.6 ± 5.

Ten weeks of branched-chain amino acid supplementation improves select performance and immunological variables in trained cyclists.

We examined if supplementing trained cyclists (32 ± 2 year, 77.8 ± 2.6 kg, and 7.