medchem

Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains

http://feedproxy.google.com/~r/acs/jmcmar/~3/QT458clx_G0/acs.jmedchem.0c00075

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00075

Authors: Michael A. Clegg†‡?, Paul Bamborough†, Chun-wa Chung†, Peter D. Craggs†, Laurie Gordon†, Paola Grandi§, Melanie Leveridge†, Matthew Lindon†?, Gemma M. Liwicki†, Anne-Marie Michon§, Judit Molnar†#, Inmaculada Rioja†, Peter E. Soden†, Natalie H. Theodoulou†‡?, Thilo Werner§, Nicholas C. O. Tomkinson‡, Rab K. Prinjha†, and Philip G. Humphreys*†

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6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Nonalcoholic Steatohepatitis

http://feedproxy.google.com/~r/acs/jmcmar/~3/FWMvK6adOsM/acs.jmedchem.0c00542

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00542

Authors: Joseph M. Salamoun†#, Christopher J. Garcia†#, Stefan R. Hargett‡, Jacob H. Murray†, Sing-Young Chen§, Martina Beretta§, Stephanie J. Alexopoulos§, Divya P. Shah§, Ellen M. Olzomer§, Simon P. Tucker??, Kyle L. Hoehn*‡§, and Webster L. Santos*†

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Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF3 and Et Using Matrix Metalloproteinases As Structural Probes

http://feedproxy.google.com/~r/acs/jmcmar/~3/o-RmWaxu_XI/acs.jmedchem.0c00648

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00648

Authors: Nathalie Erdeljac†, Christian Thiehoff†, Ravindra P. Jumde‡, Constantin G. Daniliuc†, Sandra Ho¨ppner§, Andreas Faust§, Anna K. H. Hirsch*‡?, and Ryan Gilmour*†

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Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists


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  • R. Nakajima, H. Oono, S. Sugiyama, Y. Matsueda, T. Ida, S. Kakuda, J. Hirata, A. Baba, A. Makino, R. Matsuyama, R.D. White, R.. Wurz, Y. Shin, X. Min, A. Guzman-Perez, Z. Wang, A. Symons, S.K. Singh, S.R. Mothe, S. Belyakov, A. Chakrabarti, and S. Shuto, "Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists", ACS Medicinal Chemistry Letters, vol. 11, pp. 528-534, 2020. http://dx.doi.org/10.1021/acsmedchemlett.9b00649
  • An artificial intelligence approach to pro-actively inspire drug discovery with recommendations



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  • S.L. Rohall, L. Auch, J. Gable, J. Gora, J. Jansen, Y. Lu, E. Martin, M. Pancost-Heidebrecht, B. Shirley, N. Stiefl, and M. Lindvall, "An Artificial Intelligence Approach to Proactively Inspire Drug Discovery with Recommendations", Journal of Medicinal Chemistry, 2020. http://dx.doi.org/10.1021/acs.jmedchem.9b02130
  • Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

    Astra-Zeneca

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  • R.T. Howard, P. Hemsley, P. Petteruti, C.N. Saunders, J.A. Molina Bermejo, J.S. Scott, J.W. Johannes, and E.W. Tate, "Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors", ACS Chemical Biology, vol. 15, pp. 325-333, 2020. http://dx.doi.org/10.1021/acschembio.9b00963
  • Human Body-on-Chip platform enables in vitro prediction of drug behaviors in humans

    3 insightful articles on the possibility to miniaturize organism testing through miniaturized models:

    Overview at the Wyss Institute
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  • A. Herland, B.M. Maoz, D. Das, M.R. Somayaji, R. Prantil-Baun, R. Novak, M. Cronce, T. Huffstater, S.S.F. Jeanty, M. Ingram, A. Chalkiadaki, D. Benson Chou, S. Marquez, A. Delahanty, S. Jalili-Firoozinezhad, Y. Milton, A. Sontheimer-Phelps, B. Swenor, O. Levy, K.K. Parker, A. Przekwas, and D.E. Ingber, "Quantitative prediction of human pharmacokinetic responses to drugs via fluidically coupled vascularized organ chips", Nature Biomedical Engineering, vol. 4, pp. 421-436, 2020. http://dx.doi.org/10.1038/s41551-019-0498-9
  • R. Novak, M. Ingram, S. Marquez, D. Das, A. Delahanty, A. Herland, B.M. Maoz, S.S.F. Jeanty, M.R. Somayaji, M. Burt, E. Calamari, A. Chalkiadaki, A. Cho, Y. Choe, D.B. Chou, M. Cronce, S. Dauth, T. Divic, J. Fernandez-Alcon, T. Ferrante, J. Ferrier, E.A. FitzGerald, R. Fleming, S. Jalili-Firoozinezhad, T. Grevesse, J.A. Goss, T. Hamkins-Indik, O. Henry, C. Hinojosa, T. Huffstater, K. Jang, V. Kujala, L. Leng, R. Mannix, Y. Milton, J. Nawroth, B.A. Nestor, C.F. Ng, B. O’Connor, T. Park, H. Sanchez, J. Sliz, A. Sontheimer-Phelps, B. Swenor, G. Thompson, G.J. Touloumes, Z. Tranchemontagne, N. Wen, M. Yadid, A. Bahinski, G.A. Hamilton, D. Levner, O. Levy, A. Przekwas, R. Prantil-Baun, K.K. Parker, and D.E. Ingber, "Robotic fluidic coupling and interrogation of multiple vascularized organ chips", Nature Biomedical Engineering, vol. 4, pp. 407-420, 2020. http://dx.doi.org/10.1038/s41551-019-0497-x
  • Increasing Complexity: A Practical Synthetic Approach to Three‐Dimensional, Cyclic Sulfoximines and First Insights into Their in vitro Properties

    Bayer:

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  • E. Boulard, V. Zibulski, L. Oertel, P. Lienau, M. Schäfer, U. Ganzer, and U. Lücking, "Increasing Complexity: A Practical Synthetic Approach to Three‐Dimensional, Cyclic Sulfoximines and First Insights into Their in Vitro Properties", Chemistry – A European Journal, vol. 26, pp. 4378-4388, 2020. http://dx.doi.org/10.1002/chem.201905461