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Published on: September 18, 2013
Recent Progress of Small Molecule Menin-MLL Interaction Inhibitors as Therapeutic Agents for Acute Leukemia
Hao Lei1, San-Qi Zhang1, Shu Fan1
1Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, Shaanxi 710061, PR China.
Abstract:
Mixed lineage leukemia (MLL) gene rearrangements are associated with acute leukemia. The protein menin is regarded as a critical oncogenic cofactor of the resulting MLL fusion proteins in acute leukemia. A direct interaction between menin and the MLL amino terminal sequences is necessary for MLL fusion protein-mediated leukemogenesis. Thus, inhibition of the interaction between menin and MLL has emerged as a novel therapeutic strategy. Recent improvements in structural biology and chemical reactivity have promoted the design and development of selective and potent menin-MLL interaction inhibitors. In this Perspective, different classes of menin-MLL interaction inhibitors are comprehensively summarized. Further research potential, challenges, and opportunities in the field are also discussed.
Insights
Targeting the menin-Mixed Lineage Leukemia (MLL) protein interaction offers a new therapeutic strategy for acute leukemia. Inhibitors blocking this interaction are being developed to combat MLL gene rearrangements.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Mixed lineage leukemia (MLL) gene rearrangements are a key driver of acute leukemia.
- The protein menin acts as an oncogenic cofactor for MLL fusion proteins, essential for leukemogenesis.
- Inhibition of the menin-MLL interaction is a promising therapeutic strategy.
Purpose of the Study:
- To comprehensively summarize current classes of menin-MLL interaction inhibitors.
- To discuss the research potential, challenges, and opportunities in developing these inhibitors.
Main Methods:
- Review of recent advancements in structural biology and chemical reactivity.
- Analysis of different classes of selective and potent menin-MLL interaction inhibitors.
Main Results:
- Development of selective and potent inhibitors targeting the menin-MLL interaction.
- Identification of various inhibitor classes based on structural and chemical properties.
Conclusions:
- Menin-MLL interaction inhibitors represent a novel therapeutic avenue for MLL-associated acute leukemias.
- Further research is needed to overcome challenges and capitalize on opportunities in this field.
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