Publications by authors named "R B Lobell"

Introduction: Volleyball and handball have typical overhead throwing motion that can generate adaptations in the athlete's kinetic chain predisposing to injuries and pain. Considering the importance of the trunk and shoulder in overhead throwing motion and the particularities of these action in different sports, this study aimed to compare the trunk and shoulder muscle strength and mobility in young female volleyball and handball athletes.

Design: Cross-sectional study with 70 female volleyball and handball athletes between 13 and 18 years old.

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Context: Volleyball and handball players have usually been studied collectively as "overhead athletes," since throwing present similarities in the proximal to distal movement sequencing and upper limb joints ranges of motion. However, each sport presents specificities in the objectives when accelerating the ball and a variety of possible throwing techniques. Therefore, it is expected there may be differences in the shoulder and upper body physical performance between sports.

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Pyridyl aminothiazoles comprise a novel class of ATP-competitive Chk1 inhibitors with excellent inhibitory potential. Modification of the core with ethylenediamine amides provides compounds with low picomolar potency and very high residence times. Investigation of binding parameters of such compounds using X-ray crystallography and molecular dynamics simulations revealed multiple hydrogen bonds to the enzyme backbone as well as stabilization of the conserved water molecules network in the hydrophobic binding region.

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Translation of significant biochemical activity of pyridyl aminothiazole class of Chk1 inhibitors into functional CEA potency required analysis and adjustment of both physical properties and kinase selectivity profile of the series. The steps toward optimization of cellular potency included elimination of CDK7 activity, reduction of molecular weight and polar surface area and increase in lipophilicity of the molecules in the series.

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We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stability when incubated in human and rat microsomes.

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