Mention of hERG is found in literature. However, pkCSM software mention inhibition of hERG I and hERG II. Could some one help me know what is hERG II. Whether a compound non-inhibitor of hERG I but inhibiotr of hERG II be accepted as a drug candidate.
Three hERG genes have been identified to date, hERG1, hERG2 and hERG3. Also, hERG1 has two isoforms, hERG1a and hERG1b.
The vast majority of non neuronal tissues and cancers tend to express hERG1A. However, leukemias preferentially express the other isoform, i.e. hERG1B.
Gasparoli and colleagues (Gasparoli L et al 2015, Mol Pharmacol. 87:183-196.) developed a pyrimido-indole derivative which shows more selective inhibition of hERG1B.
There is a lot of literature available regarding these isoforms.
Thank you, Dr. Ahuja. I learnt about hERG3. Could you please help me by citing one or two reviews on hERG so that I can learn more about these.
It is cited that drug candidate should not block hERG as it effects function of heart. Could you please, throw light on it.
I am attaching relevant literature.
It is correct that hERG blockage is related to cardiovascular disorders, but there are many hERG blocker drugs which are in the market or are under development. The thing to be considered is the safety factor available considering the in vitro inhibition/animal exposure/human exposure level of drug.
There is a new line where hERG blockers are being considered effective for cancer treatment.
- Badges
- Science topic
- Similar topics
- Chemistry
- Pharmacology
- Pharmaceuticals
- Drugs