Role of KLHL6 inactivation in mature B-cell malignancies

NIH RePORTER · NIH · R01 · $368,288 · view on reporter.nih.gov ↗

Abstract

Project Summary Mature B-cell neoplasms are the fifth most common neoplasm in both males and females. They arise from B- cells that have entered germinal centers and display great heterogeneity at the clinical and genetic levels. The clinical success of proteasome inhibitors, bortezomib, and E3 ubiquitin ligase inhibitors, lenalinomide for the treatment of multiple myeloma and B-cell lymphomas has made the Ubiquitin pathway a bona fide target for cancer therapeutics. Thus, defining how novel E3 ligases function at a molecular level and investigating their role in B-cell malignancies remains a major research imperative in order to develop more specific therapeutic avenues. KLHL6 is a gene of unknown function that is mutated in mature B-cell malignancies such as chronic lymphocytic leukemia, diffuse large B-cell lymphoma, follicular lymphoma, and multiple myeloma. We have demonstrated that KLHL6 is an E3 ubiquitin ligase and cancer-associated mutations inactivate its catalytic activity. The goals of this research proposal are to define the molecular and cellular functions of KLHL6 with regards substrate degradation and analyze the effects of KLHL6-loss in vivo. Our central hypothesis is that KLHL6 is novel tumor suppressor that may contribute to the pathogenesis of DLBCL and MM by regulating cell proliferation, differentiation and survival.

Key facts

NIH application ID
9982852
Project number
5R01CA207513-05
Recipient
UNIVERSITY OF PENNSYLVANIA
Principal Investigator
Luca Busino
Activity code
R01
Funding institute
NIH
Fiscal year
2020
Award amount
$368,288
Award type
5
Project period
2016-08-01 → 2022-07-31