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Items: 15


Recent advances in the development of Mcl-1 inhibitors for cancer therapy.

Hird AW, Tron AE.

Pharmacol Ther. 2019 Jun;198:59-67. doi: 10.1016/j.pharmthera.2019.02.007. Epub 2019 Feb 18.


Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.

Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW.

Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w.


Concurrent Inhibition of Pim and FLT3 Kinases Enhances Apoptosis of FLT3-ITD Acute Myeloid Leukemia Cells through Increased Mcl-1 Proteasomal Degradation.

Kapoor S, Natarajan K, Baldwin PR, Doshi KA, Lapidus RG, Mathias TJ, Scarpa M, Trotta R, Davila E, Kraus M, Huszar D, Tron AE, Perrotti D, Baer MR.

Clin Cancer Res. 2018 Jan 1;24(1):234-247. doi: 10.1158/1078-0432.CCR-17-1629. Epub 2017 Oct 26.


Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress.

Doshi KA, Trotta R, Natarajan K, Rassool FV, Tron AE, Huszar D, Perrotti D, Baer MR.

Oncotarget. 2016 Jul 26;7(30):48280-48295. doi: 10.18632/oncotarget.10209.


Next-generation sequencing identifies a novel ELAVL1-TYK2 fusion gene in MOLM-16, an AML cell line highly sensitive to the PIM kinase inhibitor AZD1208.

Tron AE, Keeton EK, Ye M, Casas-Selves M, Chen H, Dillman KS, Gale RE, Stengel C, Zinda M, Linch DC, Lai Z, Khwaja A, Huszar D.

Leuk Lymphoma. 2016 Dec;57(12):2927-2929. Epub 2016 May 17. No abstract available.


SCF β-TRCP targets MTSS1 for ubiquitination-mediated destruction to regulate cancer cell proliferation and migration.

Zhong J, Shaik S, Wan L, Tron AE, Wang Z, Sun L, Inuzuka H, Wei W.

Oncotarget. 2013 Dec;4(12):2339-53.


Structure of a glomulin-RBX1-CUL1 complex: inhibition of a RING E3 ligase through masking of its E2-binding surface.

Duda DM, Olszewski JL, Tron AE, Hammel M, Lambert LJ, Waddell MB, Mittag T, DeCaprio JA, Schulman BA.

Mol Cell. 2012 Aug 10;47(3):371-82. doi: 10.1016/j.molcel.2012.05.044. Epub 2012 Jun 28.


Negative regulation of the stability and tumor suppressor function of Fbw7 by the Pin1 prolyl isomerase.

Min SH, Lau AW, Lee TH, Inuzuka H, Wei S, Huang P, Shaik S, Lee DY, Finn G, Balastik M, Chen CH, Luo M, Tron AE, Decaprio JA, Zhou XZ, Wei W, Lu KP.

Mol Cell. 2012 Jun 29;46(6):771-83. doi: 10.1016/j.molcel.2012.04.012. Epub 2012 May 17.


The glomuvenous malformation protein Glomulin binds Rbx1 and regulates cullin RING ligase-mediated turnover of Fbw7.

Tron AE, Arai T, Duda DM, Kuwabara H, Olszewski JL, Fujiwara Y, Bahamon BN, Signoretti S, Schulman BA, DeCaprio JA.

Mol Cell. 2012 Apr 13;46(1):67-78. doi: 10.1016/j.molcel.2012.02.005. Epub 2012 Mar 8.


Rictor forms a complex with Cullin-1 to promote SGK1 ubiquitination and destruction.

Gao D, Wan L, Inuzuka H, Berg AH, Tseng A, Zhai B, Shaik S, Bennett E, Tron AE, Gasser JA, Lau A, Gygi SP, Harper JW, DeCaprio JA, Toker A, Wei W.

Mol Cell. 2010 Sep 10;39(5):797-808. doi: 10.1016/j.molcel.2010.08.016.


Redox regulation of plant homeodomain transcription factors.

Tron AE, Bertoncini CW, Chan RL, Gonzalez DH.

J Biol Chem. 2002 Sep 20;277(38):34800-7. Epub 2002 Jul 1.


Combinatorial interactions of two amino acids with a single base pair define target site specificity in plant dimeric homeodomain proteins.

Tron AE, Bertoncini CW, Palena CM, Chan RL, Gonzalez DH.

Nucleic Acids Res. 2001 Dec 1;29(23):4866-72.


Positively charged residues at the N-terminal arm of the homeodomain are required for efficient DNA binding by homeodomain-leucine zipper proteins.

Palena CM, Tron AE, Bertoncini CW, Gonzalez DH, Chan RL.

J Mol Biol. 2001 Apr 20;308(1):39-47.


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