LITERATURE

Abstracts

  • Priyanka Somanath, Sanchita Mourya, Weiqun Li, Tenley C. Archer, Brian Law, Daniel Lu, Tripta Rughwani, Lekha Kumar, Taisei Kinoshita, Mini Balakrishnan, Thomas Butler; Oral menin inhibitor, BMF-219, displays a significant and durable reduction in HbA1c in a type 2 diabetes rat model. EASD 2022 Short Oral Discussion (#590).
    https://www.abstractsonline.com/pp8/#!/10613/presentation/1318
  • Farhad Ravandi, Ashwin Kishtagari, Hetty E Carraway, Gary J. Schiller, Steve Morris, Alexandru Cacovean, Bhagyashree (Kelshikar) Yadav, Thomas Butler, Jeffrey E. Lancet; COVALENT-101: A phase 1 study of BMF-219, a novel oral irreversible menin inhibitor, in patients with relapsed/refractory (R/R) acute leukemia (AL), diffuse large B-cell lymphoma (DLBCL), and multiple myeloma (MM). J Clin Oncol 40, 2022 (suppl 16; abstr TPS7064)
    https://ascopubs.org/doi/abs/10.1200/JCO.2022.40.16_suppl.TPS7064
  • Priyanka Somanath, Daniel Lu, Brian Law, Tenley Archer, Tripta Rughwani, Lekha Kumar, Taisei Kinoshita, Mini Balakrishnan, Thomas Butler; Preclinical activity of irreversible Menin inhibitor, BMF-219, in chronic lymphocytic leukemia. J Clin Oncol 40, 2022 (suppl 16; abstr 7541)
    https://ascopubs.org/doi/abs/10.1200/JCO.2022.40.16_suppl.7541
  • Farhad Ravandi-Kashani, Ashwin Kishtagari, Hetty Carraway, Emily Curran, Gary Schiller, Alex Cacovean, Bhagyashree Yadav, Thomas Butler, Jeffrey Lancet.  A phase 1 study of BMF-219, a novel oral irreversible menin inhibitor, as single-agent in patients with relapsed/refractory (R/R) acute leukemia (AL), diffuse large B-cell lymphoma (DLBCL), and multiple myeloma (MM)  In AACR; April 8-13, 2022; New Orleans, LA https://www.abstractsonline.com/pp8/#!/10517/presentation/20306
  • Priyanka Somanath, Daniel Lu, Brian Law, James T. Palmer, Taisei Kinoshita, Mini Balakrishnan, Thomas Butler. Anti-tumor activity of irreversible menin inhibitor, BMF-219, in High-Grade B-Cell Lymphoma and Multiple Myeloma preclinical models. In AACR; April 8-13, 2022; New Orleans, LA https://www.abstractsonline.com/pp8/#!/10517/presentation/15520
  • Priyanka Somanath, Daniel Lu, Brian Law, Tenley C. Archer, Alexandru Cacovean, James T. Palmer, Taisei Kinoshita, Thomas Butler; Novel Irreversible Menin Inhibitor, BMF-219, Shows Potent Single Agent Activity in Clinically Relevant DLBCL Cells. Blood 2021; 138 (Supplement 1): 4318. https://doi.org/10.1182/blood-2021-148045
 

Oral Presentations

Poster Presentations

AACR 2022 DLBCL MM
BMF-219 Exhibits Potent Cytotoxicity in KRAS-Mutated Solid Tumors
COVALENT-101 AACR TIP CT210
ASCO CLL
ADA Poster 2022 (Regular Abstract)
ADA Poster 2022 (Late Breaking)
COVALENT-101 IMS TIP 2022
IMS 2022 DLBCL MM

Publications

Covalent Inhibition

  • Cheng, S.-S., Yang, G.-J., Wang, W., Leung, C.-H., & Ma, D.-L. (2020). The design and development of covalent protein-protein interaction inhibitors for cancer treatment. Journal of Hematology & Oncology, 13(1)https://doi.org/10.1186/s13045-020-00850-0

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Menin – Oncology / Review

  • Issa, G. C., Ravandi, F., DiNardo, C. D., Jabbour, E., Kantarjian, H. M., & Andreeff, M. (2021). Therapeutic implications of menin inhibition in acute leukemias. Leukemia, 35(9), 2482–2495. https://doi.org/10.1038/s41375-021-01309-y
  • Ozyerli‐Goknar, E., Nizamuddin, S., & Timmers, H. T. M. (2021). A Box of Chemistry to Inhibit the MEN1 Tumor Suppressor Gene Promoting Leukemia. ChemMedChem, 16(9), 1391–1402https://doi.org/10.1002/cmdc.202000972
  • Xia, Y., & Zhang, X. (2020). The Spectrum of MYC Alterations in Diffuse Large B-Cell Lymphoma. Acta haematologica, 143(6), 520–528. https://doi.org/10.1159/000505892
  • Jovanović, K. K., Roche-Lestienne, C., Ghobrial, I. M., Facon, T., Quesnel, B., & Manier, S. (2018). Targeting MYC in multiple myeloma. Leukemia, 32(6), 1295–1306. https://doi.org/10.1038/s41375-018-0036-x
  • Wu, G., Yuan, M., Shen, S., Ma, X., Fang, J., Zhu, L., Sun, L., Liu, Z., He, X., Huang, D., Li, T., Li, C., Wu, J., Hu, X., Li, Z., Song, L., Qu, K., Zhang, H., & Gao, P. (2017). Menin enhances c-Myc-mediated transcription to promote cancer progression. Nature communications, 8, 15278. https://doi.org/10.1038/ncomms15278
  • Kuhn, M. W. M., Song, E., Feng, Z., Sinha, A., Chen, C.-W., Deshpande, A. J., … Armstrong, S. A. (2016). Targeting Chromatin Regulators Inhibits Leukemogenic Gene Expression in NPM1 Mutant Leukemia. Cancer Discovery, 6(10), 1166–1181. https://doi.org/10.1158/2159-8290.CD-16-0237
  • Cierpicki, T., & Grembecka, J. (2014). Challenges and opportunities in targeting the menin–MLL interaction. Future Medicinal Chemistry, 6(4), 447–462. https://doi.org/10.4155/fmc.13.214
  • Matkar, S., Thiel, A., & Hua, X. (2013). Menin: a scaffold protein that controls gene expression and cell signaling. Trends in Biochemical Sciences, 38(8), 394–402. https://doi.org/10.1016/j.tibs.2013.05.005

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Menin – Diabetes

  • Dzama, M. M., Steiner, M., Rausch, J., Sasca, D., Schonfeld, J., Kunz, K., Taubert, M. C., McGeehan, G. M., Chen, C. W., Mupo A., Hahnel P., Theobald, M., Kindler, T., Koche, R. P., Vassiliou, G. S., Armstrong, S. A., Kuhn, M. W. (2020). Synergistic targeting of FLT3 mutations in AML via combined menin-MLL and FLT3 inhibition. Blood, 136(21): 2442–2456. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8215191/
  • Ma, J., Xing, B., Cao, Y., He, X., Bennett, K. E., Tong, C., An, C., … Hua, X. (2021). Menin-regulated Pbk controls high fat diet-induced compensatory beta cell proliferation. EMBO molecular medicine, 13(5), e13524. https://doi.org/10.15252/emmm.202013524
  • Xing, B., Ma, J., Jiang, Z., Feng, Z., Ling, S., Szigety, K., Su, W., Zhang, L., Jia, R., Sun, Y., Zhang, L., Kong, X., Ma, X., & Hua, X. (2019). GLP-1 signaling suppresses menin’s transcriptional block by phosphorylation in β cells. The Journal of cell biology218(3), 855–870. https://doi.org/10.1083/jcb.201805049
  • Yang, Y., Wang, H., & Hua, X. (2010). Deletion of the Men1 gene prevents streptozotocin-induced hyperglycemia in mice. Experimental diabetes research2010, 876701. https://doi.org/10.1155/2010/876701
  • Karnik, S. K., Chen, H., McLean, G. W., Heit, J. J., Gu, X., Zhang, A. Y., Fontaine, M., Yen, M. H., & Kim, S. K. (2007). Menin controls growth of pancreatic beta-cells in pregnant mice and promotes gestational diabetes mellitus. Science (New York, N.Y.), 318(5851), 806–809. https://doi.org/10.1126/science.1146812

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