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
- Thomas Butler, Sanchita Mourya, Weiqun Li, Brian Law, Tenley Archer, Taisei Kinoshita, Priyanka Somanath; Oral long-acting menin inhibitor normalises type 2 diabetes in two rat models. EASD 2022 Oral Presentation (#197). https://www.abstractsonline.com/pp8/#!/10613/presentation/934
- 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 Mellitus Rat Model. ADA Scientific Sessions 2022 (113-LB)
https://diabetesjournals.org/diabetes/article/71/Supplement_1/113-LB/146520/113-LB-Oral-Menin-Inhibitor-BMF-219-Displays-a
- Thomas Butler, Weiqun Li, Brian Law, Tenley Archer, Taisei Kinoshita, Priyanka Somanath; Oral Long-Acting Menin Inhibitor Normalizes Type 2 Diabetes Mellitus (T2DM) in Two Rat Models. ADA Scientific Sessions 2022 (P-851)
https://diabetesjournals.org/diabetes/article/71/Supplement_1/851-P/145721/851-P-Oral-Long-Acting-Menin-Inhibitor-Normalizes
- 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
- Brian Law, Daniel Lu, Priyanka Somanath, James T. Palmer, Taisei Kinoshita, Thomas Butler. Irreversible menin inhibitor, BMF-219, inhibits the growth of KRAS-mutated solid tumors. In AACR; April 8-13, 2022; New Orleans, LA https://www.abstractsonline.com/pp8/#!/10517/presentation/15102
- 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
Posters
AACR 2022 DLBCL MM
ASCO CLL
BMF-219 Exhibits Potent Cytotoxicity in KRAS-Mutated Solid Tumors
ADA Poster 2022 (Regular Abstract)
COVALENT-101 AACR TIP CT210
ADA Poster 2022 (Late Breaking)
Literature
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
- Strelow, J. M. (2016). A Perspective on the Kinetics of Covalent and Irreversible Inhibition. SLAS DISCOVERY: Advancing Life Sciences R&D, 22(1), 3–20. https://doi.org/10.1177/1087057116671509
- Kalgutkar, A. S., & Dalvie, D. K. (2012). Drug discovery for a new generation of covalent drugs. Expert Opinion on Drug Discovery, 7(7), 561–581. https://doi.org/10.1517/17460441.2012.688744
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), 1391–1402. https://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
Menin – Diabetes
- 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 biology, 218(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 research, 2010, 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