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Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.
King HM, Rana S, Kubica SP, Mallareddy JR, Kizhake S, Ezell EL, Zahid M, Naldrett MJ, Alvarez S, Law HC, Woods NT, Natarajan A. King HM, et al. Bioorg Med Chem Lett. 2021 Jul 1;43:128061. doi: 10.1016/j.bmcl.2021.128061. Epub 2021 Apr 23. Bioorg Med Chem Lett. 2021. PMID: 33895280 Free PMC article.
Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy.
Sagar S, Singh S, Mallareddy JR, Sonawane YA, Napoleon JV, Rana S, Contreras JI, Rajesh C, Ezell EL, Kizhake S, Garrison JC, Radhakrishnan P, Natarajan A. Sagar S, et al. Eur J Med Chem. 2021 Oct 15;222:113579. doi: 10.1016/j.ejmech.2021.113579. Epub 2021 May 30. Eur J Med Chem. 2021. PMID: 34098465 Free PMC article.
Small-molecule IKKβ activation modulator (IKAM) targets MAP3K1 and inhibits pancreatic tumor growth.
Napoleon JV, Sagar S, Kubica SP, Boghean L, Kour S, King HM, Sonawane YA, Crawford AJ, Gautam N, Kizhake S, Bialk PA, Kmiec E, Mallareddy JR, Patil PP, Rana S, Singh S, Prahlad J, Grandgenett PM, Borgstahl GEO, Ghosal G, Alnouti Y, Hollingsworth MA, Radhakrishnan P, Natarajan A. Napoleon JV, et al. Proc Natl Acad Sci U S A. 2022 May 3;119(18):e2115071119. doi: 10.1073/pnas.2115071119. Epub 2022 Apr 27. Proc Natl Acad Sci U S A. 2022. PMID: 35476515 Free PMC article.
DHODH inhibition enhances the efficacy of immune checkpoint blockade by increasing cancer cell antigen presentation.
Mullen NJ, Shukla SK, Thakur R, Kollala SS, Wang D, Chaika N, Santana JF, Miklavcic WR, LaBreck DA, Mallareddy JR, Price DH, Natarajan A, Mehla K, Sykes DB, Hollingsworth MA, Singh PK. Mullen NJ, et al. bioRxiv [Preprint]. 2024 Jan 13:2023.04.03.535399. doi: 10.1101/2023.04.03.535399. bioRxiv. 2024. Update in: Elife. 2024 Jul 08;12:RP87292. doi: 10.7554/eLife.87292 PMID: 37066260 Free PMC article. Updated. Preprint.