Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice

Zhao, Lei; Pan, Yong; Peng, Kesong; Wang, Zhe; Li, Jieli; Li, Dan; Tong, Chao; Wang, Yichuan; Liang, Guang

doi:10.1530/jme-14-0268

Cited by 10 publications

(8 citation statements)

References 41 publications

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“…Several inhibitors of 11-βHSD type 1 have consequently been tested in animals, obtaining an improvement in glucose control and lipid profile (47,50).…”

Section: Diabetes Mellitus Obesity and Metabolic Syndromementioning

confidence: 99%

Approach to patients with pseudo-Cushing’s states

Scaroni

Albiger

Palmieri

et al. 2020

Endocrine Connections

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The distinction between pseudo-Cushing’s states (PCS) and Cushing’s syndrome (CS) poses a significant clinical challenge even for expert endocrinologists. A patient’s clinical history can sometimes help to distinguish between them (as in the case of alcoholic individuals), but the overlap in clinical and laboratory findings makes it difficult to arrive at a definitive diagnosis. We aim to describe the most common situations that can give rise to a condition resembling overt endogenous hypercortisolism and try to answer questions that physicians often face in clinical practice. It is important to know the relative prevalence of these different situations, bearing in mind that most of the conditions generating PCS are relatively common (such as metabolic syndrome and polycystic ovary syndrome), while CS is rare in the general population. Physicians should consider CS in the presence of additional features. Appropriate treatment of underlying conditions is essential as it can reverse the hormonal abnormalities associated with PCS. Close surveillance and a thorough assessment of a patient’s hormone status will ultimately orient the diagnosis and treatment options over time.

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“…Several inhibitors of 11-βHSD type 1 have consequently been tested in animals, obtaining an improvement in glucose control and lipid profile (47,50).…”

Section: Diabetes Mellitus Obesity and Metabolic Syndromementioning

confidence: 99%

Approach to patients with pseudo-Cushing’s states

Scaroni

Albiger

Palmieri

et al. 2020

Endocrine Connections

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“…Several structurally diverse and selective 11 β -HSD1 inhibitors, such as HIS-388, LG13, and PF-915275, have thus been designed [92, 93]. The antidiabetic activity of these inhibitors has been confirmed to be comparable to that of the classical insulin sensitizer pioglitazone in different insulin-resistant and/or diabetic rodent models [92, 94, 95], where the inhibitors significantly suppressed the levels of plasma and local tissue cortisol, plasma insulin, and fasting or postprandial blood glucose, and improved glucose intolerance and IR.…”

Section: Pparγ-sparing Compoundsmentioning

confidence: 99%

Discovery of Novel Insulin Sensitizers: Promising Approaches and Targets

Chen

Zhu

et al. 2017

PPAR Research

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Insulin resistance is the undisputed root cause of type 2 diabetes mellitus (T2DM). There is currently an unmet demand for safe and effective insulin sensitizers, owing to the restricted prescription or removal from market of certain approved insulin sensitizers, such as thiazolidinediones (TZDs), because of safety concerns. Effective insulin sensitizers without TZD-like side effects will therefore be invaluable to diabetic patients. The specific focus on peroxisome proliferator-activated receptor γ- (PPARγ-) based agents in the past decades may have impeded the search for novel and safer insulin sensitizers. This review discusses possible directions and promising strategies for future research and development of novel insulin sensitizers and describes the potential targets of these agents. Direct PPARγ agonists, selective PPARγ modulators (sPPARγMs), PPARγ-sparing compounds (including ligands of the mitochondrial target of TZDs), agents that target the downstream effectors of PPARγ, along with agents, such as heat shock protein (HSP) inducers, 5′-adenosine monophosphate-activated protein kinase (AMPK) activators, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) selective inhibitors, biguanides, and chloroquines, which may be safer than traditional TZDs, have been described. This minireview thus aims to provide fresh perspectives for the development of a new generation of safe insulin sensitizers.

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“…11β-HSD1 catalyses the intracellular conversion of cortisone to cortisol. Inhibition of 11β-HSD1 has therapeutic benefits in type 2 diabetes 35 . Disadvantagemineralocorticoid induced side effects 12 .…”

Section: Fig 6: Mechanism Of Action Of Dgat-1mentioning

confidence: 99%

Untitled

2020

IJPSR

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Diabetes mellitus (DM) is a globally spreading metabolic disorder with a high incidence rate. About 425 million cases took place in 2017 and expected to rise up to 693 million by 2045. In diabetes, the patient elevation of blood glucose level occurs due to the deformation of insulin receptor action/secretion or both. Long term increases in blood glucose level causes chronic effects such as dysfunction and damage of various organs such as eyes, nerves, kidney heart and blood vessels. There are many treatment regimens available in market, but do not able to provide complete relief and cause severe side effects. To overcome these types of problems it becomes important to find different therapeutic targets and use it in combination with conventional medicine for the treatment of diabetes. To surmount the side effect of presently available treatments, now researchers relay on herbal plants. In this review, we discussed the diabetes occurrence, epidemiology, types, different target receptors, and available treatments and describe briefly role of different plant constituents in diabetes management and focused on a main plant, Moringa oleifera.

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Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice

Cited by 10 publications

References 41 publications

Approach to patients with pseudo-Cushing’s states

Approach to patients with pseudo-Cushing’s states

Discovery of Novel Insulin Sensitizers: Promising Approaches and Targets

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