A series of novel 8-amino-1,3-disubstituted-imidazo[1,5-a]pyrazines was designed and synthesized as IGF-IR inhibitors.
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| http://dx.doi.org/10.1016/j.bmcl.2006.11.016 | DOI Listing |
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Gene deletion of Pregnancy-associated Plasma Protein-A (PAPP-A) improves pathology and cognition in an Alzheimer's disease mouse model.
Exp Neurol
December 2024
Department of Endocrinology, Mayo Clinic, Rochester, MN 55905, United States of America. Electronic address:
Article Synopsis
- Alzheimer's disease (AD) is a worsening brain condition without effective treatments, linked to the buildup of toxic β-amyloid peptides and amyloid plaques.
- Previous studies have connected the insulin-like growth factor (IGF) system to AD, and reduced IGF-I receptor (IGFIR) signaling can alleviate plaque formation and neurodegeneration in mice.
- Research highlighted that deleting PAPP-A, a protein involved in regulating IGF-I, in a mouse model of AD resulted in less plaque, improved brain function, and suggests that targeting PAPP-A could be a new treatment option for AD.
Opposite effects of acute and chronic IGF1 on rat dorsal root ganglion neuron excitability.
Front Cell Neurosci
June 2024
Department of Physiology and Pharmacology, Faculty of Medicine and Health Sciences and Sagol School of Neurosciences-Tel Aviv University, Tel Aviv, Israel.
Insulin-like growth factor-1 (IGF-1) is a polypeptide hormone with a ubiquitous distribution in numerous tissues and with various functions in both neuronal and non-neuronal cells. IGF-1 provides trophic support for many neurons of both the central and peripheral nervous systems. In the central nervous system (CNS), IGF-1R signaling regulates brain development, increases neuronal firing and modulates synaptic transmission.
View Article and Find Full Text PDFPAPP-A as a Potential Target in Thyroid Eye Disease.
J Clin Endocrinol Metab
November 2024
Division of Endocrinology, Mayo Clinic, Rochester, MN 55905, USA.
Context: Proptosis in thyroid eye disease (TED) can result in facial disfigurement and visual dysfunction. Treatment with insulin-like growth factor I receptor (IGF-IR) inhibitors has been shown to be effective in reducing proptosis but with side effects.
Objective: To test the hypothesis that inhibition of IGF-IR indirectly and more selectively with PAPP-A inhibitors attenuates IGF-IR signaling in TED.
Establishment and Characterization of Amitrole-Induced Mouse Thyroid Adenomatous Nodule-Derived Cell Lines.
Thyroid
April 2024
Cancer Innovation Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Thyroid cancer cell lines have been of great value for the study of thyroid cancer. However, the availability of benign thyroid adenoma cell lines is limited. Cell lines were established from thyroid adenomatous nodules that developed in mice treated with the goitrogen amitrole.
View Article and Find Full Text PDFFibrocyte Participation in Thyroid-Associated Ophthalmopathy Suggests New Approaches to Therapy.
Ophthalmic Plast Reconstr Surg
December 2023
Department of Ophthalmology and Visual Sciences.
Purpose: Review the historical context of research and changing therapeutic landscape of thyroid-associated ophthalmopathy (TAO) by focusing on the relationship between TAO, CD34+ fibrocytes, thyrotropin receptor (TSHR), and insulin-like growth factor-I receptor (IGF-IR).
Methods: A literature review using search terms, including fibrocytes, IGF-IR, TSHR, TAO, and thyroid eye disease.
Results: The mechanisms involved in TAO have been partially identified.
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