A protein kinase C α and β inhibitor blunts hyperphagia to halt renal function decline and reduces adiposity in a rat model of obesity-driven type 2 diabetes.


Journal

Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288

Informations de publication

Date de publication:
07 10 2023
Historique:
received: 28 12 2022
accepted: 28 09 2023
medline: 1 11 2023
pubmed: 8 10 2023
entrez: 7 10 2023
Statut: epublish

Résumé

Type 2 diabetes (T2D) and its complications can have debilitating, sometimes fatal consequences for afflicted individuals. The disease can be difficult to control, and therapeutic strategies to prevent T2D-induced tissue and organ damage are needed. Here we describe the results of administering a potent and selective inhibitor of Protein Kinase C (PKC) family members PKCα and PKCβ, Cmpd 1, in the ZSF1 obese rat model of hyperphagia-induced, obesity-driven T2D. Although our initial intent was to evaluate the effect of PKCα/β inhibition on renal damage in this model setting, Cmpd 1 unexpectedly caused a marked reduction in the hyperphagic response of ZSF1 obese animals. This halted renal function decline but did so indirectly and indistinguishably from a pair feeding comparator group. However, above and beyond this food intake effect, Cmpd 1 lowered overall animal body weights, reduced liver vacuolation, and reduced inguinal adipose tissue (iWAT) mass, inflammation, and adipocyte size. Taken together, Cmpd 1 had strong effects on multiple disease parameters in this obesity-driven rodent model of T2D. Further evaluation for potential translation of PKCα/β inhibition to T2D and obesity in humans is warranted.

Identifiants

pubmed: 37805649
doi: 10.1038/s41598-023-43759-7
pii: 10.1038/s41598-023-43759-7
pmc: PMC10560236
doi:

Substances chimiques

Protein Kinase C-alpha EC 2.7.11.13

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

16919

Informations de copyright

© 2023. Springer Nature Limited.

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Auteurs

Ju Wang (J)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA. ju.wang@pfizer.com.

Agustin Casimiro-Garcia (A)

Medicine Design, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Bryce G Johnson (BG)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Jennifer Duffen (J)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Michael Cain (M)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Mediar Therapeutics, Boston, MA, USA.

Leigh Savary (L)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Instem Life Science Systems Ltd, Mount Ida College, South Hadley, MA, USA.

Stephen Wang (S)

Pharmacokinetics and Drug Metabolism, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Novartis Gene Therapies, Novartis Institute for Biomedical Research, Cambridge, MA, USA.

Prashant Nambiar (P)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Strand Therapeutics, Cambridge, MA, USA.

Matthew Lech (M)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Shanrong Zhao (S)

Clinical Genetics and Bioinformatics, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Amunix Pharmaceuticals, San Francisco, CA, USA.

Li Xi (L)

Early Clinical Development, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Yutian Zhan (Y)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Jennifer Olson (J)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Groton, CT, USA.

James A Stejskal (JA)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Groton, CT, USA.
Charles River Laboratories, Shrewsbury, MA, USA.

Hank Lin (H)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Sunovion Pharmaceuticals Inc., Marlborough, MA, USA.

Baohong Zhang (B)

Clinical Genetics and Bioinformatics, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Data Sciences, Biogen, Cambridge, MA, USA.

Robert V Martinez (RV)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.
Center for Technological Innovation, Pfizer Worldwide Research and Development, San Francisco, CA, USA.

Katherine Masek-Hammerman (K)

Drug Safety Research and Development, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Franklin J Schlerman (FJ)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA.

Ken Dower (K)

Inflammation and Immunology, Pfizer Worldwide Research and Development, Cambridge, MA, USA. ken.dower@pfizer.com.

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Classifications MeSH