Grn163l
Identification
- Generic Name
- Grn163l
- DrugBank Accession Number
- DB05036
- Background
GRN163L is a novel anti-cancer drug. It has been characterized preclinically and shown to inhibit telomerase in human tumor cells of many cancer types (including lung, breast, prostate, liver, and early stage of human breast cancer), in both cell culture systems and animal models. Study of this drug shows the its potential utility in the treatment of patients with hematologic and solid tumor malignancies.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in leukemia (lymphoid) and solid tumors.
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- Pharmacodynamics
Not Available
- Mechanism of action
GRN163L has been characterized preclinically and shown to inhibit telomerase in human tumor cells of many cancer types. It targets the template region, or active site, of telomerase. GRN163L does not exhibit antisense activity (binding to messenger RNA), but rather directly bind to the RNA component of telomerase at the active site of the enzyme, thereby acting like a conventional pharmaceutical drug. Inhibiting telomerase activity should result in telomere shortening and therefore cause aging and death of cancer cells.
Target Actions Organism UTelomerase-binding protein EST1A Not Available Humans UN-terminal kinase-like protein Not Available Humans UProstaglandin E synthase 3 Not Available Humans UTelomerase reverse transcriptase Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Gryaznov SM, Jackson S, Dikmen G, Harley C, Herbert BS, Wright WE, Shay JW: Oligonucleotide conjugate GRN163L targeting human telomerase as potential anticancer and antimetastatic agent. Nucleosides Nucleotides Nucleic Acids. 2007;26(10-12):1577-9. [Article]
- Gomez-Millan J, Goldblatt EM, Gryaznov SM, Mendonca MS, Herbert BS: Specific telomere dysfunction induced by GRN163L increases radiation sensitivity in breast cancer cells. Int J Radiat Oncol Biol Phys. 2007 Mar 1;67(3):897-905. Epub 2006 Dec 15. [Article]
- Hochreiter AE, Xiao H, Goldblatt EM, Gryaznov SM, Miller KD, Badve S, Sledge GW, Herbert BS: Telomerase template antagonist GRN163L disrupts telomere maintenance, tumor growth, and metastasis of breast cancer. Clin Cancer Res. 2006 May 15;12(10):3184-92. [Article]
- Gellert GC, Dikmen ZG, Wright WE, Gryaznov S, Shay JW: Effects of a novel telomerase inhibitor, GRN163L, in human breast cancer. Breast Cancer Res Treat. 2006 Mar;96(1):73-81. Epub 2005 Dec 1. [Article]
- Dikmen ZG, Gellert GC, Jackson S, Gryaznov S, Tressler R, Dogan P, Wright WE, Shay JW: In vivo inhibition of lung cancer by GRN163L: a novel human telomerase inhibitor. Cancer Res. 2005 Sep 1;65(17):7866-73. [Article]
- External Links
- PubChem Substance
- 347909904
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Recruiting Treatment Myelofibrosis 1 2 Completed Treatment Locally Recurrent and Metastatic Breast Cancer 1 2 Completed Treatment Multiple Myeloma (MM) 1 2 Completed Treatment Myeloid Malignancies / Primary Myelofibrosis (PMF) / Secondary Myelofibrosis 1 2 Completed Treatment Non-Small Cell Lung Cancer (NSCLC) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Telomeric dna binding
- Specific Function
- Component of the telomerase ribonucleoprotein (RNP) complex that is essential for the replication of chromosome termini. May have a general role in telomere regulation. Promotes in vitro the abilit...
- Gene Name
- SMG6
- Uniprot ID
- Q86US8
- Uniprot Name
- Telomerase-binding protein EST1A
- Molecular Weight
- 160460.34 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Regulates COPI-mediated retrograde traffic. Has no detectable kinase activity in vitro.Isoform 6 acts as transcriptional activator. It binds to three different types of GC-rich DNA binding sites (b...
- Gene Name
- SCYL1
- Uniprot ID
- Q96KG9
- Uniprot Name
- N-terminal kinase-like protein
- Molecular Weight
- 89630.605 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Unfolded protein binding
- Specific Function
- Cytosolic prostaglandin synthase that catalyzes the oxidoreduction of prostaglandin endoperoxide H2 (PGH2) to prostaglandin E2 (PGE2) (PubMed:10922363). Molecular chaperone that localizes to genomi...
- Gene Name
- PTGES3
- Uniprot ID
- Q15185
- Uniprot Name
- Prostaglandin E synthase 3
- Molecular Weight
- 18697.195 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Trna binding
- Specific Function
- Telomerase is a ribonucleoprotein enzyme essential for the replication of chromosome termini in most eukaryotes. Active in progenitor and cancer cells. Inactive, or very low activity, in normal som...
- Gene Name
- TERT
- Uniprot ID
- O14746
- Uniprot Name
- Telomerase reverse transcriptase
- Molecular Weight
- 126995.435 Da
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52