Peer-Reviewed Scientific Background
RELEVANT PUBLICATIONS
- Ross BD, Jang Y, Welton A, Bonham CA, Palagama DSW, Heist K, Boppisetti J, Imaduwage KP, Robison T, King LR, Zhang EZ, Amirfazli C, Luker KE, Lee WY, Luker GD, Chenevert TL, Van Dort ME. A lymphatic-absorbed multi-targeted kinase inhibitor for myelofibrosis therapy. Nature Communication 2022 Aug 17;13(1):4730. doi: 10.1038/s41467-022-32486-8. (https://www.nature.com/articles/s41467-022-32486-8).
- Van Dort ME, Jang Y, Bonham CA, Heist K, Palagama DSW, McDonald L, Zhang EZ, Chenevert TL, Luker GD, Ross BD. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996. doi: 10.1016/j.ejmech.2021.113996. PMID: 34802837; PMCID: PMC8792322.
- Smith A, Pawar M, Van Dort ME, Galbán S, Welton AR, Thurber GM, Ross BD, Besirli CG. Ocular Toxicity Profile of ST-162 and ST-168 as Novel Bifunctional MEK/PI3K Inhibitors. J Ocul Pharmacol Ther. 2018 Jul/Aug;34(6):477-485. doi: 10.1089/jop.2017.0126. Epub 2018 Apr 30. PMID: 29708810; PMCID: PMC6088257.
- Van Dort ME, Galbán S, Nino CA, Hong H, Apfelbaum AA, Luker GD, Thurber GM, Atangcho L, Besirli CG, Ross BD. Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168). ACS Med Chem Lett. 2017 Jul 24;8(8):808-813. doi: 10.1021/acsmedchemlett.7b00111. PMID: 28835793; PMCID: PMC5554897.
- Galbán S, Apfelbaum AA, Espinoza C, Heist K, Haley H, Bedi K, Ljungman M, Galbán CJ, Luker GD, Dort MV, Ross BD. A Bifunctional MAPK/PI3K Antagonist for Inhibition of Tumor Growth and Metastasis. Mol Cancer Ther. 2017 Nov;16(11):2340-2350. doi: 10.1158/1535-7163.MCT-17-0207. Epub 2017 Aug 3. PMID: 28775144; PMCID: PMC5669819.
- Van Dort ME, Galbán S, Wang H, Sebolt-Leopold J, Whitehead C, Hong H, Rehemtulla A, Ross BD. Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor. Bioorg Med Chem. 2015 Apr 1;23(7):1386-94. doi: 10.1016/j.bmc.2015.02.053. Epub 2015 Mar 6. PMID: 25766633; PMCID: PMC4370322.
- Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. PMID: 18952427.
- Ohren JF, Chen H, Pavlovsky A, Whitehead C, Zhang E, Kuffa P, Yan C, McConnell P, Spessard C, Banotai C, Mueller WT, Delaney A, Omer C, Sebolt-Leopold J, Dudley DT, Leung IK, Flamme C, Warmus J, Kaufman M, Barrett S, Tecle H, Hasemann CA. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. doi: 10.1038/nsmb859. Epub 2004 Nov 14. Erratum in: Nat Struct Mol Biol. 2005 Mar;12(3):278. PMID: 15543157.
