In vivo and in vitro characterization of skeletal muscle metabolism in patients with statin-induced adverse effects

2006 ◽  
Vol 55 (4) ◽  
pp. 551-557 ◽  
Author(s):  
S. Guis ◽  
D. Figarella-branger ◽  
J. P. Mattei ◽  
F. Nicoli ◽  
Y. Le Fur ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Adverse Effects ◽  
Muscle Metabolism ◽  
Skeletal Muscle Metabolism ◽  
In Vitro Characterization

scholarly journals Skeletal muscle metabolism in sea-acclimatized king penguins. I. Thermogenic mechanisms

2020 ◽  
Vol 223 (21) ◽  
pp. jeb233668
Author(s):  
Damien Roussel ◽  
Marion Le Coadic ◽  
Jean-Louis Rouanet ◽  
Claude Duchamp
Keyword(s):  
Skeletal Muscle ◽  
Muscle Metabolism ◽  
Exact Nature ◽  
Skeletal Muscle Metabolism ◽  
Energy Demands ◽  
Skeletal Muscle Contraction ◽  
Drastic Increase ◽  
Shivering Thermogenesis

ABSTRACTAt fledging, king penguin juveniles undergo a major energetic challenge to overcome the intense and prolonged energy demands for thermoregulation and locomotion imposed by life in cold seas. Among other responses, sea acclimatization triggers fuel selection in skeletal muscle metabolism towards lipid oxidation in vitro, which is reflected by a drastic increase in lipid-induced thermogenesis in vivo. However, the exact nature of skeletal muscle thermogenic mechanisms (shivering and/or non-shivering thermogenesis) remains undefined. The aim of the present study was to determine in vivo whether the capacity for non-shivering thermogenesis was enhanced by sea acclimatization. We measured body temperature, metabolic rate, heart rate and shivering activity in fully immersed king penguins (Aptenodytes patagonicus) exposed to water temperatures ranging from 12 to 29°C. Results from terrestrial pre-fledging juveniles were compared with those from sea-acclimatized immature penguins (hereafter ‘immatures’). The capacity for thermogenesis in water was as effective in juveniles as in immatures, while the capacity for non-shivering thermogenesis was not reinforced by sea acclimatization. This result suggests that king penguins mainly rely on skeletal muscle contraction (shivering or locomotor activity) to maintain endothermy at sea. Sea-acclimatized immature penguins also exhibited higher shivering efficiency and oxygen pulse (amount of oxygen consumed or energy expended per heartbeat) than pre-fledging juvenile birds. Such increase in shivering and cardiovascular efficiency may favor a more efficient activity–thermoregulatory heat substitution providing penguins with the aptitude to survive the tremendous energetic challenge imposed by marine life in cold circumpolar oceans.

scholarly journals Protein kinase N2 regulates AMP kinase signaling and insulin responsiveness of glucose metabolism in skeletal muscle

2017 ◽  
Vol 313 (4) ◽  
pp. E483-E491 ◽  
Author(s):  
Maxwell A. Ruby ◽  
Isabelle Riedl ◽  
Julie Massart ◽  
Marcus Åhlin ◽  
Juleen R. Zierath
Keyword(s):  
Skeletal Muscle ◽  
Protein Kinase ◽  
Glucose Metabolism ◽  
Glucose Uptake ◽  
Muscle Metabolism ◽  
Whole Body ◽  
Skeletal Muscle Metabolism ◽  
Ampk Signaling

Insulin resistance is central to the development of type 2 diabetes and related metabolic disorders. Because skeletal muscle is responsible for the majority of whole body insulin-stimulated glucose uptake, regulation of glucose metabolism in this tissue is of particular importance. Although Rho GTPases and many of their affecters influence skeletal muscle metabolism, there is a paucity of information on the protein kinase N (PKN) family of serine/threonine protein kinases. We investigated the impact of PKN2 on insulin signaling and glucose metabolism in primary human skeletal muscle cells in vitro and mouse tibialis anterior muscle in vivo. PKN2 knockdown in vitro decreased insulin-stimulated glucose uptake, incorporation into glycogen, and oxidation. PKN2 siRNA increased 5′-adenosine monophosphate-activated protein kinase (AMPK) signaling while stimulating fatty acid oxidation and incorporation into triglycerides and decreasing protein synthesis. At the transcriptional level, PKN2 knockdown increased expression of PGC-1α and SREBP-1c and their target genes. In mature skeletal muscle, in vivo PKN2 knockdown decreased glucose uptake and increased AMPK phosphorylation. Thus, PKN2 alters key signaling pathways and transcriptional networks to regulate glucose and lipid metabolism. Identification of PKN2 as a novel regulator of insulin and AMPK signaling may provide an avenue for manipulation of skeletal muscle metabolism.

Asymmetric synthesis and in vivo/in vitro characterization of new hybrid anticonvulsants derived from (2,5-dioxopyrrolidin-1-yl)phenylacetamides

2021 ◽  
Vol 109 ◽  
pp. 104751
Author(s):  
Michał Abram ◽  
Anna Rapacz ◽  
Gniewomir Latacz ◽  
Bartłomiej Szulczyk ◽  
Justyna Kalinowska-Tłuścik ◽  
...  
Keyword(s):  
Asymmetric Synthesis ◽  
In Vitro Characterization

scholarly journals In vivo and in vitro characterization of overproduced colicin E9 immunity protein

1992 ◽  
Vol 207 (2) ◽  
pp. 687-695 ◽  
Author(s):  
Russell WALLIS ◽  
Ann REILLY ◽  
Arthur ROWE ◽  
Geoffrey R. MOORE ◽  
Richard JAMES ◽  
...  
Keyword(s):  
Immunity Protein ◽  
In Vitro Characterization ◽  
Colicin E9

scholarly journals Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7236
Author(s):  
Yazan J. Meqbil ◽  
Hongyu Su ◽  
Robert J. Cassell ◽  
Kendall L. Mores ◽  
Anna M. Gutridge ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Clinical Drug Development ◽  
In Vitro Characterization ◽  
Opioid Receptor Agonist ◽  
Negative Allosteric Modulator ◽  
Δ Opioid Receptor ◽  
Clinical Drug

The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed. It has increasingly become apparent that the SNC80 scaffold carries with it potent and efficacious β-arrestin recruitment. Here, we screened a relatively small (5120 molecules) physical drug library to identify δOR agonists that underrecruit β-arrestin, as it has been suggested that compounds that efficaciously recruit β-arrestin are proconvulsant. The screen identified a hit compound and further characterization using cellular binding and signaling assays revealed that this molecule (R995045, compound 1) exhibited ten-fold selectivity over µ- and κ-opioid receptors. Compound 1 represents a novel chemotype at the δOR. A subsequent characterization of fourteen analogs of compound 1, however did not identify a more potent δOR agonist. Computational modeling and in vitro characterization of compound 1 in the presence of the endogenous agonist leu-enkephalin suggest compound 1 may also bind allosterically and negatively modulate the potency of Leu-enkephalin to inhibit cAMP, acting as a ‘NAM-agonist’ in this assay. The potential physiological utility of such a class of compounds will need to be assessed in future in vivo assays.

In vivo and in vitro characterization of rifampicine suppositories

2009 ◽  
Vol 19 (3) ◽  
pp. 217-221
Author(s):  
H.M. El-Nahas ◽  
F.S. Ghazy ◽  
H.A. El-Ghamry ◽  
A.M. El-Wsaby
Keyword(s):  
In Vitro Characterization
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