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Page 1
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. Among authors: pietrak b. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Zhang Z, Ghosh A, Connolly PJ, King P, Wilde T, Wang J, Dong Y, Li X, Liao D, Chen H, Tian G, Suarez J, Bonnette WG, Pande V, Diloreto KA, Shi Y, Patel S, Pietrak B, Szewczuk L, Sensenhauser C, Dallas S, Edwards JP, Bachman KE, Evans DC. Zhang Z, et al. Among authors: pietrak b. J Med Chem. 2021 Aug 12;64(15):11570-11596. doi: 10.1021/acs.jmedchem.1c00890. Epub 2021 Jul 19. J Med Chem. 2021. PMID: 34279934
Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors.
Sinnamon RH, McDevitt P, Pietrak BL, Leydon VR, Xue Y, Lehr R, Qi H, Burns M, Elkins P, Ward P, Vincentini G, Fisher D, Grimes M, Brandt M, Auger KR, Ho T, Johanson K, Jones CS, Schwartz B, Sweitzer TD, Kirkpatrick RB. Sinnamon RH, et al. Among authors: pietrak bl. Protein Expr Purif. 2010 Oct;73(2):167-76. doi: 10.1016/j.pep.2010.05.002. Epub 2010 May 10. Protein Expr Purif. 2010. PMID: 20457255
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin AG, Faitg TH, Richter M, Groy A, Seefeld MA, Darcy MG, Peng X, Federowicz K, Yang J, Zhang SY, Minthorn E, Jaworski JP, Schaber M, Martens S, McNulty DE, Sinnamon RH, Zhang H, Kirkpatrick RB, Nevins N, Cui G, Pietrak B, Diaz E, Jones A, Brandt M, Schwartz B, Heerding DA, Kumar R. Gilmartin AG, et al. Among authors: pietrak b. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
Crystallographic structure of a small molecule SIRT1 activator-enzyme complex.
Dai H, Case AW, Riera TV, Considine T, Lee JE, Hamuro Y, Zhao H, Jiang Y, Sweitzer SM, Pietrak B, Schwartz B, Blum CA, Disch JS, Caldwell R, Szczepankiewicz B, Oalmann C, Yee Ng P, White BH, Casaubon R, Narayan R, Koppetsch K, Bourbonais F, Wu B, Wang J, Qian D, Jiang F, Mao C, Wang M, Hu E, Wu JC, Perni RB, Vlasuk GP, Ellis JL. Dai H, et al. Among authors: pietrak b. Nat Commun. 2015 Jul 2;6:7645. doi: 10.1038/ncomms8645. Nat Commun. 2015. PMID: 26134520 Free PMC article.
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: pietrak bl. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: pietrak bl. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
41 results