mithramycin

Ligand id: 8394

Name: mithramycin

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 21
Hydrogen bond donors 11
Rotatable bonds 15
Topological polar surface area 358.2
Molecular weight 1084.47
XLogP -1.61
No. Lipinski's rules broken 3

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Before withdrawl from the market, this compound was used in the treatment of testicular cancer [1], Paget’s disease of bone, hypercalcemia and hypercalciuria.
Mechanism Of Action and Pharmacodynamic Effects
Mithramycin binds to DNA and prevents association of transcriptional activators at GC-rich binding sites [2]. Mithramycin inhibits histone methyltransferase (HMT) enzyme activity in lung cancer cells [3], and is effective against SETDB1 HMT protein overexpression which drives tumorigenesis in non-small and small lung cancer cell lines and primary tumours [4]. The drug is also effective in inhibiting aberrant HMT-induced histone H3 (K9) trimethylation in Huntington's disease (HD) and may therefore present a novel neuroprotective mechanism for treating HD [5].