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PERK Inhibition by HC-5404 Sensitizes Renal Cell Carcinoma Tumor Models to Antiangiogenic Tyrosine Kinase Inhibitors.
Stokes ME, Calvo V, Fujisawa S, Dudgeon C, Huang S, Ballal N, Shen L, Gasparek J, Betzenhauser M, Taylor SJ, Staschke KA, Rigby AC, Mulvihill MJ, Bose N, Lightcap ES, Surguladze D. Stokes ME, et al. Among authors: gasparek j. Clin Cancer Res. 2023 Dec 1;29(23):4870-4882. doi: 10.1158/1078-0432.CCR-23-1182. Clin Cancer Res. 2023. PMID: 37733811 Free PMC article.
Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
Calvo V, Surguladze D, Li AH, Surman MD, Malibhatla S, Bandaru M, Jonnalagadda SK, Adarasandi R, Velmala M, Singireddi DRP, Velpuri M, Nareddy BR, Sastry V, Mandati C, Guguloth R, Siddiqui S, Patil BS, Chad E, Wolfley J, Gasparek J, Feldman K, Betzenhauser M, Wiens B, Koszelak-Rosenblum M, Zhu G, Du H, Rigby AC, Mulvihill MJ. Calvo V, et al. Among authors: gasparek j. Bioorg Med Chem Lett. 2021 Jul 1;43:128058. doi: 10.1016/j.bmcl.2021.128058. Epub 2021 Apr 23. Bioorg Med Chem Lett. 2021. PMID: 33895276 Free article.