Literature References

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).


  • 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.


  • 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.

Diabetes and Beta Cell Function

  • Rhodes CJ. Type 2 diabetes-a matter of beta-cell life and death? Science. 2005 Jan 21;307(5708):380-4. doi: 10.1126/science.1104345. PMID: 15662003.

  • Usman TO, Chhetri G, Yeh H, Dong HH. Beta-cell compensation and gestational diabetes. J Biol Chem. 2023 Oct 29;299(12):105405. doi: 10.1016/j.jbc.2023.105405. PMCID: PMC10694657.

  • Saisho Y. Postprandial C-Peptide to Glucose Ratio as a Marker of β Cell Function: Implication for the Management of Type 2 Diabetes. Int J Mol Sci. 2016 May 17;17(5):744. doi: 10.3390/ijms17050744. PMID: 27196896; PMCID: PMC4881566.

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Beta Cell Proliferation

  • Van Assche FA, Aerts L, De Prins F. A morphological study of the endocrine pancreas in human pregnancy. Br J Obstet Gynaecol. 1978 Nov;85(11):818-20. doi: 10.1111/j.1471-0528.1978.tb15835.x. PMID: 363135.

  • Linnemann AK, Baan M, Davis DB. Pancreatic β-cell proliferation in obesity. Adv Nutr. 2014 May 14;5(3):278-88. doi: 10.3945/an.113.005488. PMID: 24829474; PMCID: PMC4013180.

  • Cao, Y., Feng, Z., He, X., Zhang, X., Xing, B., Wu, Y., Hojnacki, T., Katona, B. W., Ma, J., Zhan, X., & Hua, X. (2022). Prolactin-regulated Pbk is involved in pregnancy-induced β-cell proliferation in mice. Journal of Endocrinology252(2), 107-123.

  • Shrivastava V, Lee M, Lee D, Pretorius M, Radford B, Makkar G, Huang C. Beta cell adaptation to pregnancy requires prolactin action on both beta and non-beta cells. Sci Rep. 2021 May 14;11(1):10372. doi: 10.1038/s41598-021-89745-9. PMID: 33990661; PMCID: PMC8121891.

  • Huang C. (2013). Wild-type offspring of heterozygous prolactin receptor-null female mice have maladaptive β-cell responses during pregnancy. The Journal of physiology591(5), 1325–1338.

  • Salazar-Petres, E. R., & Sferruzzi-Perri, A. N. (2022). Pregnancy-induced changes in β-cell function: what are the key players?. The Journal of physiology600(5), 1089–1117.

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Menin and Beta Cell Proliferation

  • 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.

  • Hughes, E., & Huang, C. (2011). Participation of Akt, menin, and p21 in pregnancy-induced beta-cell proliferation. Endocrinology152(3), 847–855.

  • Ma, J., Xing, B., Cao, Y., He, X., Bennett, K. E., Tong, C., An, C., Hojnacki, T., Feng, Z., Deng, S., Ling, S., Xie, G., Wu, Y., Ren, Y., Yu, M., Katona, B. W., Li, H., Naji, A., & Hua, X. (2021). Menin-regulated Pbk controls high fat diet-induced compensatory beta cell proliferation. EMBO molecular medicine13(5), e13524.

  • Zhang, H., Li, W., Wang, Q., Wang, X., Li, F., Zhang, C., Wu, L., Long, H., Liu, Y., Li, X., Luo, M., Li, G., & Ning, G. (2012). Glucose-mediated repression of menin promotes pancreatic β-cell proliferation. Endocrinology153(2), 602–611.
  • Yang, Y., Gurung, B., Wu, T., Wang, H., Stoffers, D. A., & Hua, X. (2010). Reversal of preexisting hyperglycemia in diabetic mice by acute deletion of the Men1 gene. Proceedings of the National Academy of Sciences of the United States of America107(47), 20358–20363.

  • Karnik, S. K., Hughes, C. M., Gu, X., Rozenblatt-Rosen, O., McLean, G. W., Xiong, Y., Meyerson, M., & Kim, S. K. (2005). Menin regulates pancreatic islet growth by promoting histone methylation and expression of genes encoding p27Kip1 and p18INK4c. Proceedings of the National Academy of Sciences of the United States of America102(41), 14659–14664.

  • Yang Y, Wang H, Hua X. Deletion of the Men1 gene prevents streptozotocin-induced hyperglycemia in mice. Exp Diabetes Res. 2010;2010:876701. doi: 10.1155/2010/876701. Epub 2011 Jan 17. PMID: 21318185; PMCID: PMC3034935.

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Menin in Oncology

  • 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.

  • 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.

  • 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.

  • Xia, Y., & Zhang, X. (2020). The Spectrum of MYC Alterations in Diffuse Large B-Cell Lymphoma. Acta haematologica, 143(6), 520–528.

  • 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.

  • 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.

  • 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.

  • Cierpicki, T., & Grembecka, J. (2014). Challenges and opportunities in targeting the menin–MLL interaction. Future Medicinal Chemistry, 6(4), 447–462.

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