LITERATURE
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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
Oral Presentations
Poster Presentations
COVALENT-102 TIP WCLC 2023
COVALENT-101 TIP SOHO 2023
ADA 2023: COVALENT-111 Preliminary Results in Type 2 Diabetes
AACR 2023 BMF-219 and BMF-500: Combination approaches using covalent menin and/or FLT3 inhibitors potentiate therapeutic use in AML
AACR 2023 BMF-219: Impacts key gene signatures and molecular pathways in CLL
COVALENT-102-TIP-AACR-RAS-2023
ASH 2022 BMF-500: An Orally Bioavailable Covalent Inhibitor of FLT3
IMS 2022 DLBCL MM
COVALENT-101 IMS TIP 2022
ADA Poster 2022 (Late Breaking)
ADA Poster 2022 (Regular Abstract)
ASCO CLL
COVALENT-101 AACR TIP CT210
BMF-219 Exhibits Potent Cytotoxicity in KRAS-Mutated Solid Tumors
AACR 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
- 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
- Martinez-Martin, S., Soucek, L. (2021). MYC inhibitors in multiple myeloma. Cancer Drug Resist, 4:842-65. https://www.ncbi.nlm.nih.gov/
pmc/articles/PMC8992455/
- 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 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