Ketenes are mostly used as the remarkable and common starting materials for structurally diverse five-membered and fused five-membered compounds, such as lactones, furans, benzofurans, dioxolane derivatives, pyrroles, succinimide, indoles, oxindoles, isoindoles, thiophenes, oxazoles, benzoxazole...

The association of bioactive nucleus with other pharmacological agents is hoped to improve the efficacy of the treatment by combining the effects of different pharmacological mechanisms of action. Keeping this in view, a series of 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-one derivatives have been ...

Analysis of the results of studies of docking 1 and 7a with c-Met kinase led to the identification of benzo[d]oxazol-2(3H)-one-quinolone derivatives as potential inhibitors of this enzyme. A molecular hybrid strategy, using a 4-ethoxy-7-substituted-quinoline core and a benzo[d]oxazol-2(3H)-one s...

Inspired by the common structural characteristics of numerous known antitumor compounds targeting DNA or topoisomerase I, 3-(benzazol-2-yl)-quinoxaline-based scaffold was designed via the combination of two important privileged structure units —quinoxaline and benzazole. Thirty novel 3-(benzazo...

Amylin is an important gut-brain axis hormone. Since amylin and amyloid-β peptide (Aβ) share similar β sheet secondary structure despite not having the same primary sequences, we hypothesized that the accumulation of Aβ in the brains of subjects with Alzheimer's disease (AD) might compe...

Amylin (AMY) is a member of calcitonin family of peptides. In this study, the effects of intrathecal (i.t) injection of AMY on the inflammatory pain and on the cAMP accumulation in the rat spinal cells were investigated. By using AMY receptor antagonists, we also studied the pharmacology of AMY ...

Amylin analogs are important adjunctive drugs in the treatment of diabetes mellitus. However, a dual therapy with insulin involves inconvenient multiple injections. Here we describe a novel n-terminal PEGylated human amylin analog – BZ043 – and its potential to improve the control of glycemia ...

SummaryObjectivesPain and disability are the main clinical manifestations of osteoarthritis, for which only symptomatic therapies are available. Hence, there is a need for therapies that can simultaneously alter disease progression and provide pain relief. KBP is a dual amylin- and calcitonin-re...

Azadirachta excelsa increases the secretion of plasma insulin with subsequent reduction of fasting blood glucose. However, its protective effect towards brain amylin and insulin levels as well as the memory and learning functions remain elusive. Thus, this study aimed to ascertain the effect of ...

The ubiquitin-proteasomal-system (UPS) and the autophagy-lysosomal-system (ALS) are both highly susceptible for disturbances leading to the accumulation of cellular damage. A decline of protein degradation during aging results in the formation of oxidatively damaged and aggregated proteins final...

BackgroundAmylin is a pancreatic β-cell hormone that produces effects in several different organ systems. One of its best-characterized effects is the reduction in eating and body weight seen in preclinical and clinical studies. Amylin activates specific receptors, a portion of which it shares ...

Amylin is a pancreatic β-cell hormone co-secreted with insulin, plays a role in normal glucose homeostasis, and forms amyloid in the pancreatic islets of individuals with type-2 diabetes. Aggregated amylin is also found in blood and extra-pancreatic tissues, including myocardium. Myocardial amy...

Islet Amyloid Polypeptide (IAPP), also known as amylin, is a 37-amino-acid peptide hormone that is secreted by pancreatic islet β-cells. Amylin is complementary to insulin in regulating and maintaining blood glucose levels in the human body. The misfolding and aggregation of amylin is primarily...

Full-length native rat amylin 1–37 has previously been widely shown to be unable to form fibrils and to lack the toxicity of the human amylin form leading to its use as a non-amyloidogenic control peptide. A recent study has suggested that rat amylin 1–37 forms amyloidogenic β-sheet structure...

ABSTRACT:Plants are consumed by bacteria, fungi and animals and utilization of plant proteins requires their hydrolysis, a process which is catalyzed by proteases. Plants defend themselves against other organisms by elaborating physical and chemical defenses, the latter including protein and non...

We investigated the response of Helicoverpa armigera larvae towards ingestion of Cicer arietinum Kunitz proteinase inhibitor (CaKPI), which caused antagonistic effects on developing H. armigera larvae. CaKPI-degrading proteinases were not detectable in either control or sensitized larvae. There ...

SummaryProtease inhibitors in buckwheat seeds are separated into two main groups — anionic and cationic inhibitors, according to their behaviour on ion-exchange chromatography. Three anionic inhibitors (BWI-la, BWI-2a and BWI-4a) and two cationic (BWI-2c and BWI-4c) were purified to homogeneity...

The Murraya Koenigii trypsin inhibitor was found to be the major protein component of the seed extract. The quantity of protein was determined to be approximately 20% of total protein extracted by simple buffer extraction. During different stages of seed development after flowering, the protein ...

Winged bean albumin-1 (WBA) is the main seed albumin of Psophocarpus tetragonolobus, a legume that has excellent potential as a protein-rich food source for humid tropical climates. WBA crystallises in a tetragonal space group and the structure was solved by X-ray crystallography with a combinat...

Three protease inhibitors, namely a chymotrypsin inhibitor (WbCI), a trypsin inhibitor (WbTI) and a chymotrypsin trypsin inhibitor (WbCTI) were purified to homogeneity from the imbibed winged bean (Psophocarpus tetragonolobus (L.) Dc) seeds by affinity chromatography on trypsin and chymotrypsin ...