Novel (2E,4E,6Z)-7-(2-Alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic Acid Retinoid X Receptor Modulators Are Active in Models of Type 2 Diabetes

2003 ◽  
Vol 46 (13) ◽  
pp. 2683-2696 ◽  
Author(s):  
P. Y. Michellys ◽  
R. J. Ardecky ◽  
J. H. Chen ◽  
D. L. Crombie ◽  
G. J. Etgen ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Retinoid X Receptor ◽  
Trienoic Acid ◽  
Receptor Modulators

scholarly journals Biological Characterization of a Heterodimer-Selective Retinoid X Receptor Modulator: Potential Benefits for the Treatment of Type 2 Diabetes

Endocrinology ◽  
2006 ◽  
Vol 147 (2) ◽  
pp. 1044-1053 ◽  
Author(s):  
Mark D. Leibowitz ◽  
Robert J. Ardecky ◽  
Marcus F. Boehm ◽  
Carol L. Broderick ◽  
Mark A. Carfagna ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Retinoid X Receptor ◽  
Biological Characterization ◽  
Receptor Modulator ◽  
Potential Benefits

Mutation screening and association of human retinoid X receptor γ variation with lipid levels in familial type 2 diabetes

2002 ◽  
Vol 76 (1) ◽  
pp. 14-22 ◽  
Author(s):  
Hua Wang ◽  
Winston Chu ◽  
Christopher Hemphill ◽  
Sandra J. Hasstedt ◽  
Steven C. Elbein
Keyword(s):  
Type 2 Diabetes ◽  
Mutation Screening ◽  
Retinoid X Receptor ◽  
Lipid Levels ◽  
Familial Type

scholarly journals Association of potential salivary biomarkers with diabetic retinopathy and its severity in type-2 diabetes mellitus: a proteomic analysis by mass spectrometry

PeerJ ◽  
2016 ◽  
Vol 4 ◽  
pp. e2022 ◽  
Author(s):  
Chin Soon Chee ◽  
Khai Meng Chang ◽  
Mun Fai Loke ◽  
Voon Pei Angela Loo ◽  
Visvaraja Subrayan
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Diabetic Retinopathy ◽  
Proliferative Diabetic Retinopathy ◽  
Pathway Analysis ◽  
Retinoid X Receptor ◽  
Differentially Expressed ◽  
Disease Group

Aim/hypothesis:The aim of our study was to characterize the human salivary proteome and determine the changes in protein expression in two different stages of diabetic retinopathy with type-2 diabetes mellitus: (1) with non-proliferative diabetic retinopathy (NPDR) and (2) with proliferative diabetic retinopathy (PDR). Type-2 diabetes mellitus without diabetic retinopathy (XDR) was designated as control.Method:In this study, 45 saliva samples were collected (15 samples from XDR control group, 15 samples from NPDR disease group and 15 samples from PDR disease group). Salivary proteins were extracted, reduced, alkylated, trypsin digested and labeled with an isobaric tag for relative and absolute quantitation (iTRAQ) before being analyzed by an Orbitrap fusion tribrid mass spectrometer. Protein annotation, fold change calculation and statistical analysis were interrogated by Proteome Discoverer. Biological pathway analysis was performed by Ingenuity Pathway Analysis. Data are available via ProteomeXchange with identifiersPXD003723–PX003725.Results:A total of 315 proteins were identified from the salivary proteome and 119 proteins were found to be differentially expressed. The differentially expressed proteins from the NPDR disease group and the PDR disease group were assigned to respective canonical pathways indicating increased Liver X receptor/Retinoid X receptor (LXR/RXR) activation, Farnesoid X receptor/Retinoid X receptor (FXR/RXR) activation, acute phase response signaling, sucrose degradation V and regulation of actin-based motility by Rho in the PDR disease group compared to the NPDR disease group.Conclusions/Interpretation:Progression from non-proliferative to proliferative retinopathy in type-2 diabetic patients is a complex multi-mechanism and systemic process. Furthermore, saliva was shown to be a feasible alternative sample source for diabetic retinopathy biomarkers.

scholarly journals Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome

PPAR Research ◽  
2007 ◽  
Vol 2007 ◽  
pp. 1-12 ◽  
Author(s):  
Jane A. Pinaire ◽  
Anne Reifel-Miller
Keyword(s):  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Metabolic Syndrome ◽  
Therapeutic Potential ◽  
Treatment Options ◽  
Additional Treatment ◽  
The Metabolic Syndrome ◽  
Prevalence Of Obesity ◽  
Receptor Modulators

The increasing prevalence of obesity is a fundamental contributor to the growing prevalence of the metabolic syndrome. Rexinoids, a class of compounds that selectively bind and activate RXR, are being studied as a potential option for the treatment of metabolic syndrome. These compounds have glucose-lowering, insulin-sensitizing, and antiobesity effects in animal models of insulin resistance and type 2 diabetes. However, undesirable side effects such as hypertriglyceridemia and suppression of the thyroid hormone axis also occur. This review examines and compares the effects of four RXR-selective ligands: LGD1069, LG100268, AGN194204, and LG101506, a selective RXR modulator. Similar to selective modulators of other nuclear receptors such as the estrogen receptor (SERMs), LG101506 binding to RXR selectively maintains the desirable characteristic effects of rexinoids while minimizing the undesirable effects. These recent findings suggest that, with continued research efforts, RXR-specific ligands with improved pharmacological profiles may eventually be available as additional treatment options for the current epidemic of obesity, insulin resistance, type 2 diabetes, and all of the associated metabolic sequelae.

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