Sulfonyl(thio)urea derivative induction of insulin secretion is mediated by potassium, calcium, and sodium channel signal transduction

Sulis, Paola Miranda; Dambrós, Betina Fernanda; Mascarello, Alessandra; Santos, Adair R.S.; Yunes, Rosendo A.; Nunes, Ricardo José; Frederico, Marisa Jádna Silva; Silva, Fátima Regina Mena Barreto

doi:10.1002/jcp.27680

Cited by 11 publications

(4 citation statements)

References 52 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As a result, the intracellular concentration of potassium cations increases, leading to plasma membrane depolarization. These conditions stimulate the opening of voltage-gated calcium channels, and an increased concentration of cytosolic calcium cations leads to a surge in insulin secretion ( Sulis et al, 2019 ).…”

Section: Established Drug Classes For the Treatment Of Diabetesmentioning

confidence: 99%

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

et al. 2022

View full text Add to dashboard Cite

Type 2 diabetes mellitus (T2DM) continues to be a substantial medical problem due to its increasing global prevalence and because chronic hyperglycemic states are closely linked with obesity, liver disease and several cardiovascular diseases. Since the early discovery of insulin, numerous antihyperglycemic drug therapies to treat diabetes have been approved, and also discontinued, by the United States Food and Drug Administration (FDA). To provide an up-to-date account of the current trends of antidiabetic pharmaceuticals, this review offers a comprehensive analysis of the main classes of antihyperglycemic compounds and their mechanisms: insulin types, biguanides, sulfonylureas, meglitinides (glinides), alpha-glucosidase inhibitors (AGIs), thiazolidinediones (TZD), incretin-dependent therapies, sodium-glucose cotransporter type 2 (SGLT2) inhibitors and combinations thereof. The number of therapeutic alternatives to treat T2DM are increasing and now there are nearly 60 drugs approved by the FDA. Beyond this there are nearly 100 additional antidiabetic agents being evaluated in clinical trials. In addition to the standard treatments of insulin therapy and metformin, there are new drug combinations, e.g., containing metformin, SGLT2 inhibitors and dipeptidyl peptidase-4 (DPP4) inhibitors, that have gained substantial use during the last decade. Furthermore, there are several interesting alternatives, such as lobeglitazone, efpeglenatide and tirzepatide, in ongoing clinical trials. Modern drugs, such as glucagon-like peptide-1 (GLP-1) receptor agonists, DPP4 inhibitors and SGLT2 inhibitors have gained popularity on the pharmaceutical market, while less expensive over the counter alternatives are increasing in developing economies. The large heterogeneity of T2DM is also creating a push towards more personalized and accessible treatments. We describe several interesting alternatives in ongoing clinical trials, which may help to achieve this in the near future.

show abstract

Section: Established Drug Classes For the Treatment Of Diabetesmentioning

confidence: 99%

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Activators of the TRPA1 channel induce membrane currents, membrane depolarization, action potentials, and insulin secretion in primary rat β-cells, and all these can be blocked by selective TRPA1 inhibitors [146]. The antidiabetic sulphonylurea drug glibenclamide and its derivatives activate the TRPA1 channel by interacting with some reactive cysteines, and stimulate insulin secretion from rat islets [149,150].…”

Section: Trpa1mentioning

confidence: 99%

Molecular Regulations and Functions of the Transient Receptor Potential Channels of the Islets of Langerhans and Insulinoma Cells

Islam

2020

Cells

View full text Add to dashboard Cite

Insulin secretion from the β-cells of the islets of Langerhans is triggered mainly by nutrients such as glucose, and incretin hormones such as glucagon-like peptide-1 (GLP-1). The mechanisms of the stimulus-secretion coupling involve the participation of the key enzymes that metabolize the nutrients, and numerous ion channels that mediate the electrical activity. Several members of the transient receptor potential (TRP) channels participate in the processes that mediate the electrical activities and Ca2+ oscillations in these cells. Human β-cells express TRPC1, TRPM2, TRPM3, TRPM4, TRPM7, TRPP1, TRPML1, and TRPML3 channels. Some of these channels have been reported to mediate background depolarizing currents, store-operated Ca2+ entry (SOCE), electrical activity, Ca2+ oscillations, gene transcription, cell-death, and insulin secretion in response to stimulation by glucose and GLP1. Different channels of the TRP family are regulated by one or more of the following mechanisms: activation of G protein-coupled receptors, the filling state of the endoplasmic reticulum Ca2+ store, heat, oxidative stress, or some second messengers. This review briefly compiles our current knowledge about the molecular mechanisms of regulations, and functions of the TRP channels in the β-cells, the α-cells, and some insulinoma cell lines.

show abstract

“…When the pancreatic beta cells in physiological state, the activity of KATP is balanced. The elevation of this KATP activity leads to stop insulin secretion, while reducing it leads to stimulate insulin secretion (98) in addition, intracellular calcium concentration (Ca2+) can also affect insulin secretion (99,100,101). In case of non-stimulated B-cells, Ca2+ sustained in low level controlled by Ca2+ ATPase on endoplasmic reticulum and plasma membrane.…”

Section: Anti-diabetic Effectmentioning

confidence: 99%

Sulfonamide derivatives: Synthesis and applications

Baraa G. Alani,

Khulood S Salim,

Alaa Saleh Mahdi

et al. 2024

Int. J. Front. Chem. Pharm. Res.

View full text Add to dashboard Cite

Sulfonamides belong to an important class of compounds which showed wide ranges of biological activities like antibacterial, antiviral, diuretic, hypo-glycemic, anticancer, anti-inflammatory and recently anti-covid-19. Over the last few decades, various pharmacological activities of sulfonamide conjugates were published. Moreover, many lead compounds with sulfonamide functionality are also in clinical trial for the treatment of various medical conditions. For these reasons, development of an efficient process for the synthesis of sulfonamides has always been in the focus for research in organic field synthesis. The most typical method for the synthesis involves reaction between primary or secondary amines and sulfonyl chloride in presence of organic or inorganic bases. Although this method is effective, but the nucleophilicity of amines may vary depending on the groups attached to it. In general, primary amines are highly reactive, whereas secondary amines show very low to almost nil reactivity. In this study, we have reviewed past and recent biological effects of some sulfonamide derivatives and some advances efficient synthetic procedures for some types of sulfonamides.

show abstract

Sulfonyl(thio)urea derivative induction of insulin secretion is mediated by potassium, calcium, and sodium channel signal transduction

Cited by 11 publications

References 52 publications

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

Molecular Regulations and Functions of the Transient Receptor Potential Channels of the Islets of Langerhans and Insulinoma Cells

Sulfonamide derivatives: Synthesis and applications

Contact Info

Product

Resources

About