||Entecavir, a guanosine nucleoside analogue with activity against HBV reverse transcriptase, is efficiently phosphorylated to the active triphosphate form, which has an intracellular half-life of 15 hours. By competing with the natural substrate deoxyguanosine triphosphate, entecavir triphosphate functionally inhibits all three activities of the HBV reverse transcriptase: (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Entecavir triphosphate is a weak inhibitor of cellular DNA polymerases alpha, beta, and delta and mitochondrial DNA polymerase gamma with Ki values ranging from 18 to > 160 microM.
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DrugCentral Search Overview
Drug search example:
Generic drug names, drug synonyms, trade names terms can be used to search for drugs.
Example search for Lipitor can query using either “Atorvastatin” or “Lipitor”.A comprehensive list of drug development codes and salt or ester forms
are also stored in the database and can be used as search terms, for example search for "rosuvastatin" the following terms can be used: "rosuvastatin calcium" or "ZD4522".
Disease search example:
Supported disease terms are SNOMED-CT and OMOP vocabulary terms. Disease annotations for drugs approved before 2012 originate from OMOP vocabulary mappings. For drugs approved after 2012 disease annotations are extracted manually from approved drug labels and mapped to SNOMED-CT concepts.
Example search for “Chronic Hepatitis
returns the list of antiviral
indicated to treat “Chronic Hepatitis C” followed by drugs
contra-indicated in hepatitis C.
Target search example:
Supported target search terms are HUGO gene symbols, Uniprot accessions and target names, and Swissprot identifiers.
Example search for drugs targeting Mu-type opioid receptor can be run using either of the
terms: “OPRM1”, P35372, “OPRM
_HUMAN”, full or partial
Uniprot target name. Returned drugs are ranked using the following criteria: top ranked drugs have mechanism of action target Mu-type opioid receptor, next in the list are drugs with potencies measured against this receptor.
In collaboration with the IDG
Pharmacologic action search example:
Supported pharmacologic action terms are MeSH, FDA [EPC, MoA, PE], ChEBI action roles.
Example search for “HMG-CoA Reductase Inhibitor” FDA EPC term for statin drugs returns list of all statin drugs classified by FDA as HMG-CoA reductase inhibitors.
Ranked result list is annotated with 4 level ranking system ordered from highest to lowest:
A - query term matched drug name or synonyms, mechanism of action target, or drug indication.
B - query term matched disease term in drug contraindications or off-label uses, targets listed in drug bioactivity profiles (not MoA targets), or pharmacologic action descriptions.
C - query term matched short drug description text.
D - query term matched full text in FDA drug labels.