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1.
J Dance Med Sci ; : 1089313X241288998, 2024 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-39392612

RESUMO

INTRODUCTION: In 2012, the Standard Measures Consensus Initiative (SMCI) of the International Association for Dance Medicine and Science (IADMS) presented 6 recommendations regarding dance injury surveillance, definitions of injury and exposure, dance-specific screening, risk reduction strategies, and collaborative data management. The aim was to standardize risk factor measurement and injury reporting by researchers in dance medicine and science. Since then, numerous reports on the recording and reporting of injury data in sport and performing arts have been published. METHODS: IADMS commissioned SMCI to update the 2012 recommendations, a process that involved 3 stages: (1) current field experts were invited to join SMCI, (2) SMCI members reviewed recent and relevant sport and performing arts literature, then drafted, discussed, and revised section updates, (3) IADMS invited individuals representing diverse backgrounds in the IADMS community to critically review drafted updates. The final update serves as a bridge from the 6 recommendations in the 2012 report to the current state of evidence. RESULTS: We continue to encourage use of dance injury surveillance systems and support that surveillance protocols be fit-for-purpose, and that failure to use clear and consistent injury definitions perpetuates a lack of rigor in dance injury research. Based on new evidence, we recommend that some aspects of injury surveillance be self-reported, that the choice of dance exposure measures be dependent on the research question, contextual factors, and type of injury/health problem(s) of interest, and that studies using dance-specific screening articulate specific objectives, validity, and reliability of each protocol. CONCLUSIONS: Future studies should focus on the development, implementation, and evaluation of strategies to minimize injury risk to improve consistency and rigor in data collection and research reporting on the health and wellness of dancer populations, thus facilitating a future dance injury consensus statement similar to recent statements published for sports and circus arts.

2.
Nat Commun ; 12(1): 1052, 2021 02 16.
Artigo em Inglês | MEDLINE | ID: mdl-33594070

RESUMO

The parasitic protist Trypanosoma brucei is the causative agent of Human African Trypanosomiasis, also known as sleeping sickness. The parasite enters the blood via the bite of the tsetse fly where it is wholly reliant on glycolysis for the production of ATP. Glycolytic enzymes have been regarded as challenging drug targets because of their highly conserved active sites and phosphorylated substrates. We describe the development of novel small molecule allosteric inhibitors of trypanosome phosphofructokinase (PFK) that block the glycolytic pathway resulting in very fast parasite kill times with no inhibition of human PFKs. The compounds cross the blood brain barrier and single day oral dosing cures parasitaemia in a stage 1 animal model of human African trypanosomiasis. This study demonstrates that it is possible to target glycolysis and additionally shows how differences in allosteric mechanisms may allow the development of species-specific inhibitors to tackle a range of proliferative or infectious diseases.


Assuntos
Glicólise/efeitos dos fármacos , Fosfofrutoquinases/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Trypanosoma/enzimologia , Tripanossomíase Africana/metabolismo , Tripanossomíase Africana/parasitologia , Doença Aguda , Regulação Alostérica/efeitos dos fármacos , Animais , Células Hep G2 , Humanos , Concentração Inibidora 50 , Estimativa de Kaplan-Meier , Camundongos , Parasitos/efeitos dos fármacos , Fosfofrutoquinases/química , Fosfofrutoquinases/metabolismo , Ligação Proteica/efeitos dos fármacos , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacocinética , Inibidores de Proteínas Quinases/uso terapêutico , Multimerização Proteica , Relação Estrutura-Atividade , Trypanosoma/efeitos dos fármacos , Tripanossomíase Africana/tratamento farmacológico
3.
ACS Cent Sci ; 2(10): 687-701, 2016 Oct 26.
Artigo em Inglês | MEDLINE | ID: mdl-27800551

RESUMO

The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate, and patents were not sought. One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility. As an open source research project, unexplored avenues are clearly identified and may be explored further by the community; new findings may be cumulatively added to the present work.

4.
Chem Cent J ; 1: 2, 2007 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-17880736

RESUMO

Chemistry Central is a new open access website for chemists publishing peer-reviewed research in chemistry from a range of open access journals. A new addition, Chemistry Central Journal, will cover all of chemistry and will be broken down into discipline-specific sections, and Im delighted that Medicinal Chemistry will be a key discipline in this new journal.

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