Data from Pan-PIM Kinase Inhibition Provides a Novel Therapy for Treating Hematologic Cancers

Autor: Matthew T. Burger, Jocelyn Holash, Richard Zang, J. Alex Aycinena, Cornelia Bellamacina, Mika Lindvall, Gisele Nishiguchi, Jiong Lan, Wooseok Han, Christopher Wilson, Joerg Trappe, Peter Drueckes, Estelle Pfister, Audrey Kauffmann, Christine Fritsch, Tiffany Tsang, Jamie Narberes, Robert Warne, Paul Feucht, Michael Doyle, Jianjun Yu, Julie Chan, Stephen Basham, Xiao-Hong Niu, Jing Lu, Yumin Dai, Tatiana Zavorotinskaya, Marjorie Ison, Christie Fanton, Joseph Castillo, Min Chen, Yingyun Wang, John L. Langowski, Pablo D. Garcia

Purpose: PIM kinases have been shown to act as oncogenes in mice, with each family member being able to drive progression of hematologic cancers. Consistent with this, we found that PIMs are highly expressed in human hematologic cancers and show that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21b7a0911566c282b44322df88773977
https://doi.org/10.1158/1078-0432.c.6522398

Synthesis and Structure–Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases

Autor: Pablo Garcia, Gisele Nishiguchi, Wooseok Han, Mika Lindvall, Cornelia Bellamacina, Yumin Dai, Matthew Burger, John L. Langowski, Richard Zang, Zheng Chen, Gordana Atallah, Song Lin, Paul Feucht, Jiong Lan, Yu Ding, Alice Rico, Tatiana Zavorotinskaya

Publikováno v: Journal of Medicinal Chemistry. 63:14885-14904

Overexpression of PIM 1, 2, and 3 kinases is frequently observed in many malignancies. Previously, we discovered a potent and selective pan-PIM kinase inhibitor, compound 2, currently in phase I clinical trials. In this work, we were interested in re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59a2e2a773b3d977656af5f3b13f2c0a
https://doi.org/10.1021/acs.jmedchem.0c01279

Towards the sustainable discovery and development of new antibiotics

Autor: Ian H. Gilbert, Kenneth Pfarr, Timo Jaeger, Mika Lindvall, Anders Karlén, Philippe Glaser, Jennifer Herrmann, Marco Pieroni, Bertrand Aigle, Evi Stegmann, Heather Graz, Andrea Schiefer, Jean-Luc Pernodet, Thomas Hesterkamp, Rui Moreira, Heike Brötz-Oesterhelt, Andrew W. Truman, Andreas Keller, Ludovic Halby, Alexander Titz, José R. Tormo, Michael Graz, Kira J. Weissman, Olga Genilloud, Marc Stadler, Claus-Michael Lehr, Paola B. Arimondo, Mark Brönstrup, Savithri Ramurthy, Eriko Takano, Frédéric Peyrane, Mathias Winterhalter, Marnix H. Medema, Maarten van Dongen, Anna K. H. Hirsch, Achim Hoerauf, Helge B. Bode, Laurent Fraisse, Laura J. V. Piddock, Martin Empting, Brigitta Loretz, Yanyan Li, Heinz E. Moser, Tilmann Weber, Marcus Miethke, Silke Alt, Stefano Sabatini, Wolfgang Wohlleben, Peter Hammann, Stefano Donadio, Andriy Luzhetskyy, Myriam Seemann, Rolf Müller, Hrvoje Petković

Publikováno v: Nature Reviews. Chemistry
Nature Reviews Chemistry
Nature Reviews Chemistry, Nature Publishing Group, 2021, 5 (10), pp.726-749. ⟨10.1038/s41570-021-00313-1⟩
Nature Reviews Chemistry, 5, 726-749
Nature Reviews Chemistry, 2021, 5 (10), pp.726-749. ⟨10.1038/s41570-021-00313-1⟩
Nature Reviews Chemistry 5 (2021)

An ever-increasing demand for novel antimicrobials to treat life-threatening infections caused by the global spread of multidrug-resistant bacterial pathogens stands in stark contrast to the current level of investment in their development, particula

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de6afeefa93064508d90818e2ce9e55e
https://pubmed.ncbi.nlm.nih.gov/34426795

AI-based recommendations for drug discovery

Autor: Jonathan Gable, Peter Skewes-Cox, Margaret Pancost-Heidebrecht, Yipin Lu, William Shirley, Lydia Auch, Jacob Gora, Nikolaus Stiefl, Eric Martin, Mika Lindvall, Johanna Jansen, STEVEN ROHALL

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::640bb135d57b655fcbd25a723242f96c
https://doi.org/10.1021/scimeetings.0c07015

Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae – Identification of LYS228

Autor: Cindy Li, Xu Zang, Vijay Sethuraman, Xiaoyu Shen, Johanne Blais, Heinz E. Moser, Kyuto Tashiro, Ellie Growcott, Ramadevi Prathapam, Anthony Casarez, Aregahegn Yifru, Charles Vitt, David McKenney, Tsuyoshi Uehara, Patrick J Rudewicz, Fengxia Li, Hongqiu Guo, Adriana K. Jones, Louis E. Metzger, Wanben Gong, Jacob Shaul, Alun Bermingham, Taryn Cariaga, Richard Colvin, Xiaodong Lin, Dita M. Rasper, Mika Lindvall, Dazhi Tang, Vladimir Capka, Steven Whitebread, Sara Lopez, Meiliana Tjandra, Qingming Zhu, Nancy Turner, Robert Lowell Simmons, Charles R. Dean, Alex Fekete, Folkert Reck

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 28:748-755

Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of MBLs confers resistance in Gram-negative bacteria to all classes of β-lactam antibiotics, with the except

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82fc48314e0379bba2ac0622f8f85e46
https://doi.org/10.1016/j.bmcl.2018.01.006