From history to reality: sodium glucose co‐transporter 2 inhibitors – a novel therapy for type 2 diabetes mellitus

Nair, Sunil; Joseph, Franklin; Ewins, David; Wilding, John; Goenka, Niru

doi:10.1002/pdi.1509

Cited by 14 publications

(6 citation statements)

References 36 publications

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“…SGLT transports sodium and glucose into the cells using sodium gradient created by Na + /K + ATPase pumps at the basolateral border of the cell membranes. Glucose is then transported passively by GLUT-2 along its concentration gradient into the interstitium[ 1 2 ] [ Figure 2 ]. The affinity of phlorizin, the prototype drug of the group, is about 1 uM for hSGLT-1 and 20 nM for hSGLT-2.…”

Section: P Harmacology Of S Odium mentioning

confidence: 99%

Sodium glucose co-transporter inhibitors – A new class of old drugs

Malhotra

Kudyar

Gupta

et al. 2015

Int J App Basic Med Res

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Sodium glucose co-transporter (SGLT) inhibitors are a new class of drugs which are used in the pharmacotherapy of Type-II diabetes, which happens to be a major risk factor for developing both micro as well as macro-vascular complications. These drugs inhibit the glucose reabsorption by inhibiting SGLT, which exhibits a novel and promising mechanism of action by promoting the urinary glucose excretion hence providing a basis of therapeutic intervention. Results of SGLT-II inhibitors are very encouraging as there is a significant elevation of GLP-1 level, which forms the basis of relevance in treatment of diabetes. It targets the HbA1C and keeps a check on its levels. It also exerts other positive benefits such as weight loss, reduction in blood glucose levels, reduction in blood pressure and improvement in insulin resistance and β-cell dysfunction: All contributing to effective glycemic control. SGLT inhibition will develop as effective modality as it has the capability of inhibiting reabsorption of greater percentage of filtered glucose load.

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Section: P Harmacology Of S Odium mentioning

confidence: 99%

Sodium glucose co-transporter inhibitors – A new class of old drugs

Malhotra

Kudyar

Gupta

et al. 2015

Int J App Basic Med Res

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“…[94][95][96][97][98][99][100] Since dapagliflozin has progressed so much further than the other candidates, these reviews focused primarily on the phase 2/3 results obtained with dapagliflozin. In addition to reviewing the major studies completed with dapagliflozin, selected clinical results disclosed at the 2011 annual meetings of the American Diabetes Association and European Association for the Study of Diabetes for each of the other eight C-glucosides will be summarized.…”

Section: Clinical Studies With Sglt2 Inhibitorsmentioning

confidence: 99%

Chapter 3. SGLT2 Inhibitors in Development

Washburn¹

2012

Drug Discovery

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“…Indeed, in Auyrvedic and Chinese medicine, taste was used as a guide for the therapeutic potential of a compound . An example of bitter taste as a pointer of medicinal qualities is Phlorizin—a bitter glycoside isolated for antimalarial use following the discovery of its bitter taste (typical for known antimalarial treatments) .…”

Section: Introductionmentioning

confidence: 99%

The taste of toxicity: A quantitative analysis of bitter and toxic molecules

2017

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The role of bitter taste-one of the few basic taste modalities-is commonly assumed to signal toxicity and alert animals against consuming harmful compounds. However, it is known that some toxic compounds are not bitter and that many bitter compounds have negligible toxicity while having important health benefits. Here we apply a quantitative analysis of the chemical space to shed light on the bitterness-toxicity relationship. Using the BitterDB dataset of bitter molecules, The BitterPredict prediction tool, and datasets of toxic compounds, we quantify the identity and similarity between bitter and toxic compounds. About 60% of the bitter compounds have documented toxicity and only 56% of the toxic compounds are known or predicted to be bitter. The LD value distributions suggest that most of the bitter compounds are not very toxic, but there is a somewhat higher chance of toxicity for known bitter compounds compared to known nonbitter ones. Flavonoids and alpha acids are more common in the bitter dataset compared with the toxic dataset. In contrast, alkaloids are more common in the toxic datasets compared to the bitter dataset. Interestingly, no trend linking LD values with the number of activated bitter taste receptors (TAS2Rs) subtypes is apparent in the currently available data. This is in accord with the newly discovered expression of TAS2Rs in several extra-oral tissues, in which they might be activated by yet unknown endogenous ligands and play non-gustatory physiological roles. These results suggest that bitter taste is not a very reliable marker for toxicity, and is likely to have other physiological roles. © 2017 IUBMB Life, 69(12):938-946, 2017.

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From history to reality: sodium glucose co‐transporter 2 inhibitors – a novel therapy for type 2 diabetes mellitus

Cited by 14 publications

References 36 publications

Sodium glucose co-transporter inhibitors – A new class of old drugs

Sodium glucose co-transporter inhibitors – A new class of old drugs

Chapter 3. SGLT2 Inhibitors in Development

The taste of toxicity: A quantitative analysis of bitter and toxic molecules

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