{"id":250674,"date":"2021-05-14T19:15:44","date_gmt":"2021-05-14T16:15:44","guid":{"rendered":"https:\/\/en.buradabiliyorum.com\/researchers-develop-first-in-class-inhibitors-against-key-leukemia-protein\/"},"modified":"2021-05-14T19:15:44","modified_gmt":"2021-05-14T16:15:44","slug":"researchers-develop-first-in-class-inhibitors-against-key-leukemia-protein","status":"publish","type":"post","link":"https:\/\/buradabiliyorum.com\/en\/researchers-develop-first-in-class-inhibitors-against-key-leukemia-protein\/","title":{"rendered":"#Researchers develop first-in-class inhibitors against key leukemia protein"},"content":{"rendered":"

“#Researchers develop first-in-class inhibitors against key leukemia protein<\/strong>”<\/p>\n

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\n An X-ray crystallography image showing an ASH1L inhibitor developed at U-M in complex with the protein. Credit: Grembecka\/Cierpicki Labs
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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.<\/p>\n

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\u2014preventing critical molecular interactions in the development and progression of leukemia.<\/p>\n

The team’s findings, which used fragment-based screening, followed by medicinal chemistry and a structure-based design, app<\/a>ear in Nature Communications<\/i>.<\/p>\n

In mouse models of mixed lineage leukemia, the lead compound, known as AS-99, successfully reduced leukemia progression.<\/p>\n

“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.<\/p>\n

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

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Scientists develop first drug-like compounds to inhibit elusive cancer-linked enzymes<\/a>\n <\/div>\n

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\n More information:<\/strong>
\n David S. Rogawski et al, Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity, Nature Communications<\/i> (2021). DOI: 10.1038\/s41467-021-23152-6<\/a><\/p><\/div>\n
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\n University of Michigan
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Citation<\/strong>:
\n Researchers develop first-in-class inhibitors against key leukemia protein (2021, May 14)
\n retrieved 15 May 2021
\n from https:\/\/medicalxpress.com\/news<\/a>\/2021-05-first-in-class-inhibitors-key-leukemia-protein.html<\/p>\n

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