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A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation.
Bodine PV, Stauffer B, Ponce-de-Leon H, Bhat RA, Mangine A, Seestaller-Wehr LM, Moran RA, Billiard J, Fukayama S, Komm BS, Pitts K, Krishnamurthy G, Gopalsamy A, Shi M, Kern JC, Commons TJ, Woodworth RP, Wilson MA, Welmaker GS, Trybulski EJ, Moore WJ. Bodine PV, et al. Among authors: kern jc. Bone. 2009 Jun;44(6):1063-8. doi: 10.1016/j.bone.2009.02.013. Epub 2009 Feb 27. Bone. 2009. PMID: 19254787
Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides.
Moore WJ, Kern JC, Bhat R, Commons TJ, Fukayama S, Goljer I, Krishnamurthy G, Magolda RL, Nogle L, Pitts K, Stauffer B, Trybulski EJ, Welmaker GS, Wilson M, Bodine PV. Moore WJ, et al. Among authors: kern jc. J Med Chem. 2009 Jan 8;52(1):105-16. doi: 10.1021/jm801144h. J Med Chem. 2009. PMID: 19072540
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z. Zhang P, et al. Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. doi: 10.1016/j.bmc.2007.07.011. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17681796
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.
Gilbert AM, Bursavich MG, Lombardi S, Adedoyin A, Dwyer JM, Hughes Z, Kern JC, Khawaja X, Rosenzweig-Lipson S, Moore WJ, Neal SJ, Olsen M, Rizzo SJ, Springer D. Gilbert AM, et al. Among authors: kern jc. Bioorg Med Chem Lett. 2011 Jan 1;21(1):195-9. doi: 10.1016/j.bmcl.2010.11.038. Epub 2010 Nov 12. Bioorg Med Chem Lett. 2011. PMID: 21126874
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE. Fensome A, et al. Among authors: kern jc. J Med Chem. 2008 Mar 27;51(6):1861-73. doi: 10.1021/jm701080t. Epub 2008 Mar 5. J Med Chem. 2008. PMID: 18318463
39 results