30 C
Kolkata
Monday, May 17, 2021

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

Facebook
Twitter
Pinterest
WhatsApp


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.

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.

Story Source:

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



Source link

Facebook
Twitter
Pinterest
WhatsApp
NEWS EDITOR
News Editor - Breaking News Exchange is mainly to inform the public about events that are around them and may affect them. Often news is for entertainment purposes too; to provide a distraction of information about other places people are unable to get to or have little influence over. News can make people feel connected too.

Related Articles

LEAVE A REPLY

Please enter your comment!
Please enter your name here

Stay Connected

578FansLike
623FollowersFollow
144SubscribersSubscribe
- Advertisement -

Latest Articles