mithramycin

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Ligands
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	-0.39
No. Lipinski's rules broken	3

Molecular properties generated using the CDK

No information available.

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.

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].

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].