==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb


Details of Th1212 which contains 1 entries.


Entry 1
(1) Primary information
ID1821
ThPP IDTh1212
Therapeutic Peptide/Protein NameInsulin Pork
SequenceA chain GIVEQCCTSICSLYQLENYCN B chain FVNQHLCGSHLV view full sequnce in fasta
Functional ClassificationIa
Molecular Weight5795.6
Chemical FormulaC257H387N65O76S6
Isoelectric Point5.39
Hydrophobicity0.218
Melting Point (℃)NA
Half LifeNA
DescriptionInsulin isolated from pig pancreas. Composed of alpha and beta chains, processed from pro-insulin. Forms a hexameric structure.
Indication/DiseaseFor the treatment of type I and II diabetes mellitus.
PharmacodynamicsInsulin is used in the treatment of type I and type II diabetes. The primary activity of insulin is the regulation of glucose metabolism. In muscle and other tissues (except the brain), insulin causes rapid transport of glucose and amino acids intracellularly. It also promotes anabolism, and inhibits protein catabolism. In the liver, insulin promotes the uptake and storage of glucose in the form of glycogen, inhibits gluconeogenesis, and promotes the conversion of excess glucose into fat.
Mechanism of ActionInsulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism.
Toxicity
MetabolismInsulin is predominantly cleared by metabolic degradation via a receptor-mediated process.
AbsorptionNA
Volume of DistributionNA
ClearanceNA
CategoriesHypoglycemic Agents, Antidiabetic Agents
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetInsulin receptor, Insulin-like growth factor 1 receptor, Insulin-degrading enzyme, HLA class II histocompatibility antigen, DQ alpha 2 chain, HLA class II histocompatibility antigen, DQ beta 1 chain, Retinoblastoma-associated protein, Cathepsin D, Carboxypeptidase E, Neuroendocrine convertase 2, Neuroendocrine convertase 1, Protein NOV homolog, Low-density lipoprotein receptor-related protein 2, Insulin-like growth factor-binding protein 7, Synaptotagmin-like protein 4, Cytochrome P450 1A2
Information of corresponding available drug in the market
Brand NameIletin II
CompanyLilly
Brand DiscriptionNPH Iletin II (purified insulin, Lilly) is a crystalline suspension of insulin with protamine and zinc providing an intermediate-acting insulin with a slower onset of action and a longer duration of activity (slightly more than 24 hours) than that of regular insulin.
Prescribed forNA
Chemical NameNA
Formulation100 units/mL (U-100)
Physcial Appearancesterile suspension
Route of AdministrationSubcutaneous
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Linkhttps://www.drugs.com/drp/iletin-ii-nph-pork-100-units.html
PubMed ID25941658, 24673155, 24118819, 23448197, 28250698, 28295934, 28282219, 28275957, 28234565
3-D StructureTh1212 (View) or (Download)