Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Standard

Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice. / Cokorinos, Emily C; Delmore, Jake; Reyes, Allan R; Albuquerque, Bina; Kjøbsted, Rasmus; Jørgensen, Nicolas Oldenburg; Tran, Jean-Luc; Jatkar, Aditi; Cialdea, Katherine; Esquejo, Ryan M; Meissen, John; Calabrese, Matthew F; Cordes, Jason; Moccia, Robert; Tess, David; Salatto, Christopher T; Coskran, Timothy M; Opsahl, Alan C; Flynn, Declan; Blatnik, Matthew; Li, Wenlin; Kindt, Erick; Foretz, Marc; Viollet, Benoit; Ward, Jessica; Kurumbail, Ravi G; Kalgutkar, Amit S; Wojtaszewski, Jørgen; Cameron, Kimberly O; Miller, Russell A.

I: Cell Metabolism, Bind 25, Nr. 5, 2017, s. 1147-1159, e1-e10.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Cokorinos, EC, Delmore, J, Reyes, AR, Albuquerque, B, Kjøbsted, R, Jørgensen, NO, Tran, J-L, Jatkar, A, Cialdea, K, Esquejo, RM, Meissen, J, Calabrese, MF, Cordes, J, Moccia, R, Tess, D, Salatto, CT, Coskran, TM, Opsahl, AC, Flynn, D, Blatnik, M, Li, W, Kindt, E, Foretz, M, Viollet, B, Ward, J, Kurumbail, RG, Kalgutkar, AS, Wojtaszewski, J, Cameron, KO & Miller, RA 2017, 'Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice', Cell Metabolism, bind 25, nr. 5, s. 1147-1159, e1-e10. https://doi.org/10.1016/j.cmet.2017.04.010

APA

Cokorinos, E. C., Delmore, J., Reyes, A. R., Albuquerque, B., Kjøbsted, R., Jørgensen, N. O., Tran, J-L., Jatkar, A., Cialdea, K., Esquejo, R. M., Meissen, J., Calabrese, M. F., Cordes, J., Moccia, R., Tess, D., Salatto, C. T., Coskran, T. M., Opsahl, A. C., Flynn, D., ... Miller, R. A. (2017). Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice. Cell Metabolism, 25(5), 1147-1159, e1-e10. https://doi.org/10.1016/j.cmet.2017.04.010

Vancouver

Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO o.a. Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice. Cell Metabolism. 2017;25(5):1147-1159, e1-e10. https://doi.org/10.1016/j.cmet.2017.04.010

Author

Cokorinos, Emily C ; Delmore, Jake ; Reyes, Allan R ; Albuquerque, Bina ; Kjøbsted, Rasmus ; Jørgensen, Nicolas Oldenburg ; Tran, Jean-Luc ; Jatkar, Aditi ; Cialdea, Katherine ; Esquejo, Ryan M ; Meissen, John ; Calabrese, Matthew F ; Cordes, Jason ; Moccia, Robert ; Tess, David ; Salatto, Christopher T ; Coskran, Timothy M ; Opsahl, Alan C ; Flynn, Declan ; Blatnik, Matthew ; Li, Wenlin ; Kindt, Erick ; Foretz, Marc ; Viollet, Benoit ; Ward, Jessica ; Kurumbail, Ravi G ; Kalgutkar, Amit S ; Wojtaszewski, Jørgen ; Cameron, Kimberly O ; Miller, Russell A. / Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice. I: Cell Metabolism. 2017 ; Bind 25, Nr. 5. s. 1147-1159, e1-e10.

Bibtex

@article{0b87adfebc804ad1a9bf39091b900bb3,

title = "Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice",

abstract = "The AMP-activated protein kinase (AMPK) is a potential therapeutic target for metabolic diseases based on its reported actions in the liver and skeletal muscle. We evaluated two distinct direct activators of AMPK: a non-selective activator of all AMPK complexes, PF-739, and an activator selective for AMPK β1-containing complexes, PF-249. In cells and animals, both compounds were effective at activating AMPK in hepatocytes, but only PF-739 was capable of activating AMPK in skeletal muscle. In diabetic mice, PF-739, but not PF-249, caused a rapid lowering of plasma glucose levels that was diminished in the absence of skeletal muscle, but not liver, AMPK heterotrimers and was the result of an increase in systemic glucose disposal with no impact on hepatic glucose production. Studies of PF-739 in cynomolgus monkeys confirmed translation of the glucose lowering and established activation of AMPK in skeletal muscle as a potential therapeutic approach to treat diabetic patients.",

keywords = "AMPK, Diabetes, Glucose uptake, Pharmacology",

author = "Cokorinos, {Emily C} and Jake Delmore and Reyes, {Allan R} and Bina Albuquerque and Rasmus Kj{\o}bsted and J{\o}rgensen, {Nicolas Oldenburg} and Jean-Luc Tran and Aditi Jatkar and Katherine Cialdea and Esquejo, {Ryan M} and John Meissen and Calabrese, {Matthew F} and Jason Cordes and Robert Moccia and David Tess and Salatto, {Christopher T} and Coskran, {Timothy M} and Opsahl, {Alan C} and Declan Flynn and Matthew Blatnik and Wenlin Li and Erick Kindt and Marc Foretz and Benoit Viollet and Jessica Ward and Kurumbail, {Ravi G} and Kalgutkar, {Amit S} and J{\o}rgen Wojtaszewski and Cameron, {Kimberly O} and Miller, {Russell A}",

note = "CURIS 2017 NEXS 124",

year = "2017",

doi = "10.1016/j.cmet.2017.04.010",

language = "English",

volume = "25",

pages = "1147--1159, e1--e10",

journal = "Cell Metabolism",

issn = "1550-4131",

publisher = "Cell Press",

number = "5",

}

RIS

TY - JOUR

T1 - Activation of skeletal muscle AMPK promotes glucose disposal and glucose lowering in non-human primates and mice

AU - Cokorinos, Emily C

AU - Delmore, Jake

AU - Reyes, Allan R

AU - Albuquerque, Bina

AU - Kjøbsted, Rasmus

AU - Jørgensen, Nicolas Oldenburg

AU - Tran, Jean-Luc

AU - Jatkar, Aditi

AU - Cialdea, Katherine

AU - Esquejo, Ryan M

AU - Meissen, John

AU - Calabrese, Matthew F

AU - Cordes, Jason

AU - Moccia, Robert

AU - Tess, David

AU - Salatto, Christopher T

AU - Coskran, Timothy M

AU - Opsahl, Alan C

AU - Flynn, Declan

AU - Blatnik, Matthew

AU - Li, Wenlin

AU - Kindt, Erick

AU - Foretz, Marc

AU - Viollet, Benoit

AU - Ward, Jessica

AU - Kurumbail, Ravi G

AU - Kalgutkar, Amit S

AU - Wojtaszewski, Jørgen

AU - Cameron, Kimberly O

AU - Miller, Russell A

N1 - CURIS 2017 NEXS 124

PY - 2017

Y1 - 2017

N2 - The AMP-activated protein kinase (AMPK) is a potential therapeutic target for metabolic diseases based on its reported actions in the liver and skeletal muscle. We evaluated two distinct direct activators of AMPK: a non-selective activator of all AMPK complexes, PF-739, and an activator selective for AMPK β1-containing complexes, PF-249. In cells and animals, both compounds were effective at activating AMPK in hepatocytes, but only PF-739 was capable of activating AMPK in skeletal muscle. In diabetic mice, PF-739, but not PF-249, caused a rapid lowering of plasma glucose levels that was diminished in the absence of skeletal muscle, but not liver, AMPK heterotrimers and was the result of an increase in systemic glucose disposal with no impact on hepatic glucose production. Studies of PF-739 in cynomolgus monkeys confirmed translation of the glucose lowering and established activation of AMPK in skeletal muscle as a potential therapeutic approach to treat diabetic patients.

AB - The AMP-activated protein kinase (AMPK) is a potential therapeutic target for metabolic diseases based on its reported actions in the liver and skeletal muscle. We evaluated two distinct direct activators of AMPK: a non-selective activator of all AMPK complexes, PF-739, and an activator selective for AMPK β1-containing complexes, PF-249. In cells and animals, both compounds were effective at activating AMPK in hepatocytes, but only PF-739 was capable of activating AMPK in skeletal muscle. In diabetic mice, PF-739, but not PF-249, caused a rapid lowering of plasma glucose levels that was diminished in the absence of skeletal muscle, but not liver, AMPK heterotrimers and was the result of an increase in systemic glucose disposal with no impact on hepatic glucose production. Studies of PF-739 in cynomolgus monkeys confirmed translation of the glucose lowering and established activation of AMPK in skeletal muscle as a potential therapeutic approach to treat diabetic patients.

KW - AMPK

KW - Diabetes

KW - Glucose uptake

KW - Pharmacology

U2 - 10.1016/j.cmet.2017.04.010

DO - 10.1016/j.cmet.2017.04.010

M3 - Journal article

C2 - 28467931

VL - 25

SP - 1147-1159, e1-e10

JO - Cell Metabolism

JF - Cell Metabolism

SN - 1550-4131

IS - 5

ER -

ID: 177383146