New inhibitor against key leukemia protein: Approach opens a new avenue to study the biology of acute leukemia and for the development of new drugs

0

The protein made by the ASH1L gene plays a key role in the development of acute leukemia, along with other diseases. The ASH1L protein, however, has been challenging to target therapeutically.

Now a team of researchers led by Jolanta Grembecka, Ph.D., and Tomasz Cierpicki, Ph.D., from the University of Michigan has developed first-in-class small molecules to inhibit ASH1L’s SET domain — preventing critical molecular interactions in the development and progression of leukemia.

The team’s findings, which used fragment-based screening, followed by medicinal chemistry and a structure-based design, appear in Nature Communications.

Loading...

In mouse models of mixed lineage leukemia, the lead compound, known as AS-99, successfully reduced leukemia progression.

“This work points to a new, exiting avenue to develop new therapeutic agents against acute leukemia, as well as providing a new approach to further study the biological functions of ASH1L and its role in the development of the disease,” says Grembecka, associate professor of pathology at Michigan Medicine and co-director of the developmental therapeutics program at the U-M Rogel Cancer Center.

The study was a close collaboration between her lab and the lab of co-senior author Cierpicki, an associate professor of biophysics and pathology.

Loading...

Story Source:

Materials provided by Michigan Medicine – University of Michigan. Original written by Ian Demsky. Note: Content may be edited for style and length.

Stay connected with us on social media platform for instant update click here to join our  Twitter, & Facebook

Loading...

We are now on Telegram. Click here to join our channel (@TechiUpdate) and stay updated with the latest Technology headlines.

For all the latest Health News Click Here 

 For the latest news and updates, follow us on Google News

Loading...

Read original article here

Denial of responsibility! TechiLive.in is an automatic aggregator around the global media. All the content are available free on Internet. We have just arranged it in one platform for educational purpose only. In each content, the hyperlink to the primary source is specified. All trademarks belong to their rightful owners, all materials to their authors. If you are the owner of the content and do not want us to publish your materials on our website, please contact us by email – [email protected]. The content will be deleted within 24 hours.

Leave a comment