You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameOSI-461
Accession NumberDB05415
TypeSmall Molecule
GroupsInvestigational
DescriptionOSI-461 is a second-generation molecule belonging to a new class of drugs termed selective apoptotic anti-neoplastic drugs (SAANDs).
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationInvestigated for use/treatment in crohn's disease, inflammatory bowel disease, kidney cancer, leukemia (lymphoid), and prostate cancer.
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of actionOSI-461 is cGMP phosphodiesterase (cGMP-PDEs) inhibitors which is designed to lead to sustained activation of the intracellular signaling protein, Protein Kinase G (PKG), and subsequent stimulation of apoptosis through the c-Jun kinase pathway. Broad spectrum inhibition of cGMP-PDEs have been shown to lead to elevation in cGMP levels and the sustained activation of PKG. This in turn directly phosphorylates MEKK1 leading to activation of the N-terminal c-Jun kinase (JNK-1) pathway, a known pro-apoptotic signaling pathway.
TargetKindPharmacological actionActionsOrganismUniProt ID
cGMP-specific 3',5'-cyclic phosphodiesteraseProteinunknownNot AvailableHumanO76074 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Shimizu M, Suzui M, Deguchi A, Lim JT, Xiao D, Hayes JH, Papadopoulos KP, Weinstein IB: Synergistic effects of acyclic retinoid and OSI-461 on growth inhibition and gene expression in human hepatoma cells. Clin Cancer Res. 2004 Oct 1;10(19):6710-21. [PubMed:15475462 ]
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Metal ion binding
Specific Function:
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, PubMed:15489334). Specifically regulates nitric-oxide-generated cGMP (PubMed:15489334).
Gene Name:
PDE5A
Uniprot ID:
O76074
Molecular Weight:
99984.14 Da
Comments
comments powered by Disqus
Drug created on November 18, 2007 11:24 / Updated on August 17, 2016 12:24