Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.20 (alpha-glucosidase)
 4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The isolation and study of Anopheles gambiae genes that are differentially expressed in development, notably in tissues associated with the maturation and transmission of the malaria parasite, is important for the elucidation of basic molecular mechanisms underlying vector-parasite interactions. We have used the differential display technique to screen for mRNAs specifically expressed in adult males, females, and midgut tissues of blood-fed and unfed females. We also screened for mRNAs specifically induced upon bacterial infection of larval stage mosquitoes. We have characterized 19 distinct cDNAs, most of which show developmentally regulated expression specificity during the mosquito life cycle. The most interesting are six new sequences that are midgut-specific in the adult, three of which are also modulated by blood-feeding. The gut-specific sequences encode a maltase, a V-ATPase subunit, a GTP binding protein, two different lectins, and a nontrypsin serine protease. The latter sequence is also induced in larvae subjected to bacterial challenge. With the exception of a mitochondrial DNA fragment, the other 18 sequences constitute expressed genomic sequence tags, 4 of which have been mapped cytogenetically.
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PMID:Identification and characterization of differentially expressed cDNAs of the vector mosquito, Anopheles gambiae. 891 45

Alogliptin (codenamed SYR-322) is a recently approved anti-diabetic drug in Japan, which has been under clinical development phase III in USA and Europe. Alogliptin has been developed by Takeda under the brand name "Nesina". Alogliptin is a highly selective ( > 10,000-time selectivity, potent, reversible and durable serine protease dipeptidyl peptidase IV enzyme is compared to DPP-8 and DPP-9) inhibitor, which has been developed as an alternative second-line to metformin in place of a sulphonylurea. Alogliptin has been observed to increase and prolong the action of incretin hormone by inhibiting the DPP-IV enzyme activity. Alogliptin has been observed to well absorb and show low plasma protein binding, which displays slow-binding properties to DPP-IV enzyme. The X-ray crystallography studies have been revealed that Alogliptin binds to DPP-IV active site by non-covalently and provides sustained reduction of plasma DPP-IV activity as well as lowering of blood glucose, in drug-naive patients with T2DM and inadequate glycemic control, once daily oral dosing regimen with varying levels of doses ranging from 25-800 mg. Alogliptin is approved as monotherapy and in combination with alpha-glucosidase & thiazolidinediones. The 26 week clinical study of Alogliptin revealed that Alogliptin doesn't increase the weight and well tolerated. In the present review, we have tried to cover biology of DPP-IV, molecular chemistry, chemical characterization, crystal polymorphic information, interaction studies, commercial synthesis, current patent status, adverse effects and clinical status of Alogliptin giving emphasis on the medicinal chemistry aspect.
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PMID:Novel serine protease dipeptidyl peptidase IV inhibitor: alogliptin. 2251 82

Culicoides biting midges (Diptera: Ceratopogonidae) are hematophagous insects with over 1400 species distributed throughout the world. Many of these species are of particular agricultural importance as primary vectors of bluetongue and Schmallenberg viruses, yet little is known about Culicoides genomics and proteomics. Detailed studies of members from other blood-feeding Dipteran families, including those of mosquito (Culicidae) and black fly (Simuliidae), have shown that protein components within the insect's saliva facilitate the blood feeding process. To determine the protein components in Culicoides sonorensis midges, secreted saliva was collected for peptide sequencing by tandem mass spectrometry. Forty-five secreted proteins were identified, including members of the D7 odorant binding protein family, Kunitz-like serine protease inhibitors, maltase, trypsin, and six novel proteins unique to C. sonorensis. Identifying the complex myriad of proteins in saliva from blood-feeding Dipteran species is critical for understanding their role in blood feeding, arbovirus transmission, and possibly the resulting disease pathogenesis.
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PMID:The salivary secretome of the biting midge, Culicoides sonorensis. 2494 43