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Page 1
Discovery and Optimization of a Porcupine Inhibitor.
Duraiswamy AJ, Lee MA, Madan B, Ang SH, Tan ES, Cheong WW, Ke Z, Pendharkar V, Ding LJ, Chew YS, Manoharan V, Sangthongpitag K, Alam J, Poulsen A, Ho SY, Virshup DM, Keller TH. Duraiswamy AJ, et al. Among authors: keller th. J Med Chem. 2015 Aug 13;58(15):5889-99. doi: 10.1021/acs.jmedchem.5b00507. Epub 2015 Jul 16. J Med Chem. 2015. PMID: 26110200
Wnt addiction of genetically defined cancers reversed by PORCN inhibition.
Madan B, Ke Z, Harmston N, Ho SY, Frois AO, Alam J, Jeyaraj DA, Pendharkar V, Ghosh K, Virshup IH, Manoharan V, Ong EH, Sangthongpitag K, Hill J, Petretto E, Keller TH, Lee MA, Matter A, Virshup DM. Madan B, et al. Among authors: keller th. Oncogene. 2016 Apr 28;35(17):2197-207. doi: 10.1038/onc.2015.280. Epub 2015 Aug 10. Oncogene. 2016. PMID: 26257057 Free PMC article.
Fragment-based ligand design of novel potent inhibitors of tankyrases.
Larsson EA, Jansson A, Ng FM, Then SW, Panicker R, Liu B, Sangthongpitag K, Pendharkar V, Tai SJ, Hill J, Dan C, Ho SY, Cheong WW, Poulsen A, Blanchard S, Lin GR, Alam J, Keller TH, Nordlund P. Larsson EA, et al. Among authors: keller th. J Med Chem. 2013 Jun 13;56(11):4497-508. doi: 10.1021/jm400211f. Epub 2013 Jun 4. J Med Chem. 2013. PMID: 23672613
Pharmacophore Model for Wnt/Porcupine Inhibitors and Its Use in Drug Design.
Poulsen A, Ho SY, Wang W, Alam J, Jeyaraj DA, Ang SH, Tan ES, Lin GR, Cheong VW, Ke Z, Lee MA, Keller TH. Poulsen A, et al. Among authors: keller th. J Chem Inf Model. 2015 Jul 27;55(7):1435-48. doi: 10.1021/acs.jcim.5b00159. Epub 2015 Jun 15. J Chem Inf Model. 2015. PMID: 26024410
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.
Cherian J, Nacro K, Poh ZY, Guo S, Jeyaraj DA, Wong YX, Ho M, Yang HY, Joy JK, Kwek ZP, Liu B, Wee JL, Ong EH, Choong ML, Poulsen A, Lee MA, Pendharkar V, Ding LJ, Manoharan V, Chew YS, Sangthongpitag K, Lim S, Ong ST, Hill J, Keller TH. Cherian J, et al. Among authors: keller th. J Med Chem. 2016 Apr 14;59(7):3063-78. doi: 10.1021/acs.jmedchem.5b01712. Epub 2016 Apr 5. J Med Chem. 2016. PMID: 27011159
Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.
Ho SY, Alam J, Jeyaraj DA, Wang W, Lin GR, Ang SH, Tan ESW, Lee MA, Ke Z, Madan B, Virshup DM, Ding LJ, Manoharan V, Chew YS, Low CB, Pendharkar V, Sangthongpitag K, Hill J, Keller TH, Poulsen A. Ho SY, et al. Among authors: keller th. J Med Chem. 2017 Aug 10;60(15):6678-6692. doi: 10.1021/acs.jmedchem.7b00662. Epub 2017 Jul 20. J Med Chem. 2017. PMID: 28671458
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.
Kwiatkowski J, Liu B, Tee DHY, Chen G, Ahmad NHB, Wong YX, Poh ZY, Ang SH, Tan ESW, Ong EH, Nurul Dinie, Poulsen A, Pendharkar V, Sangthongpitag K, Lee MA, Sepramaniam S, Ho SY, Cherian J, Hill J, Keller TH, Hung AW. Kwiatkowski J, et al. Among authors: keller th. J Med Chem. 2018 May 24;61(10):4386-4396. doi: 10.1021/acs.jmedchem.8b00060. Epub 2018 May 4. J Med Chem. 2018. PMID: 29688013
Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
Ho SY, Wang W, Ng FM, Wong YX, Poh ZY, Tan SWE, Ang SH, Liew SS, Joyner Wong YS, Tan Y, Poulsen A, Pendharkar V, Sangthongpitag K, Manchester J, Basarab G, Hill J, Keller TH, Cherian J. Ho SY, et al. Among authors: keller th. Eur J Med Chem. 2018 Sep 5;157:610-621. doi: 10.1016/j.ejmech.2018.08.025. Epub 2018 Aug 11. Eur J Med Chem. 2018. PMID: 30125722
Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3.
Huang C, Liew SS, Lin GR, Poulsen A, Ang MJY, Chia BCS, Chew SY, Kwek ZP, Wee JLK, Ong EH, Retna P, Baburajendran N, Li R, Yu W, Koh-Stenta X, Ngo A, Manesh S, Fulwood J, Ke Z, Chung HH, Sepramaniam S, Chew XH, Dinie N, Lee MA, Chew YS, Low CB, Pendharkar V, Manoharan V, Vuddagiri S, Sangthongpitag K, Joy J, Matter A, Hill J, Keller TH, Foo K. Huang C, et al. Among authors: keller th. ACS Med Chem Lett. 2019 May 23;10(6):978-984. doi: 10.1021/acsmedchemlett.9b00170. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223458 Free PMC article.
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