Life_Sciences

Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A2B Adenosine Receptor Antagonists

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Ana Mallo-Abreu†‡, Rube´n Prieto-Di´az†‡, Willem Jespers§, Jhonny Azuaje†‡, Maria Majellaro†‡, Carmen Velando†, Xerardo Garci´a-Mera‡, Olga Caaman~o‡, Jose´ Brea*?, Mari´a I. Loza?, Hugo Gutie´rrez-de-Tera´n*§, and Eddy Sotelo*†‡
feedproxy.google.com/~r/acs/jmcmar/~3/1qU8NP1dGq8/acs.jmedchem.0c00564

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Mining Public Domain Data to Develop Selective DYRK1A Inhibitors

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Scott H. Henderson*†?, Fiona Sorrell#, James Bennett§, Marcus T. Hanley‡, Sean Robinson?, Iva Hopkins Navratilova??, Jonathan M. Elkins#?, and Simon E. Ward*‡
feedproxy.google.com/~r/acs/amclct/~3/EJtGSi6hNCU/acsmedchemlett.0c00279

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Biocatalytic in Vitro and in Vivo FMN Prenylation and (De)carboxylase Activation

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Khorcheska A. Batyrova†‡?, Anna N. Khusnutdinova†‡?, Po-Hsiang Wang†§?, Rosa Di Leo†, Robert Flick†, Elizabeth A. Edwards†, Alexei Savchenko†?, and Alexander F. Yakunin*†#
feedproxy.google.com/~r/acs/acbcct/~3/C99DyWuRD2w/acschembio.0c00136

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Identifying the Target of an Antiparasitic Compound in Toxoplasma Using Thermal Proteome Profiling

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Alice L. Herneisen†‡, Saima M. Sidik‡, Benedikt M. Markus‡§, David H. Drewry??, William J. Zuercher?, and Sebastian Lourido*†‡
feedproxy.google.com/~r/acs/acbcct/~3/WJrXkN42d-c/acschembio.0c00369

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Discovery of Novel Antibiotics as Covalent Inhibitors of Fatty Acid Synthesis

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Jia Wang†, Xiaoping Ye†, Xiaohan Yang†, Youyan Cai†, Shengjun Wang†, Jieyu Tang†, Meena Sachdeva§?, Yu Qian†, Wenhao Hu†, Jennifer A. Leeds§?, and Yanqiu Yuan*†‡
feedproxy.google.com/~r/acs/acbcct/~3/QPv0V_l8I5g/acschembio.9b00982

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Discovery of Dihydropyrrolo[1,2-a]pyrazin-3(4H)-one-Based Second-Generation GluN2C- and GluN2D-Selective Positive Allosteric Modulators (PAMs) of the N-Methyl-d-Aspartate (NMDA) Receptor

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Matthew P. Epplin†, Ayush Mohan†, Lynnea D. Harris†, Zongjian Zhu‡, Katie L. Strong†, John Bacsa†, Phuong Le‡, David S. Menaldino†, Stephen F. Traynelis*‡, and Dennis C. Liotta*†
feedproxy.google.com/~r/acs/jmcmar/~3/14GwdcB2vm0/acs.jmedchem.9b01733

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Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Le Wang†, George A. Doherty†, Andrew S. Judd*†, Zhi-Fu Tao†, T. Matthew Hansen†, Robin R. Frey†, Xiaohong Song†, Milan Bruncko†, Aaron R. Kunzer†, Xilu Wang†, Michael D. Wendt†, John A. Flygare§#, Nathaniel D. Catron†, Russell A. Judge†, Chang H. Park†, Shashank Shekhar†, Darren C. Phillips†, Paul Nimmer†, Morey L. Smith†, Stephen K. Tahir†, Yu Xiao†, John Xue†, Haichao Zhang†, Phuong N. Le†, Michael J. Mitten†, Erwin R. Boghaert†, Wenqing Gao†, Peter Kovar†, Edna F. Choo§, Dolores Diaz§?, Wayne J. Fairbrother§, Steven W. Elmore†, Deepak Sampath§?, Joel D. Leverson†, and Andrew James Souers†
feedproxy.google.com/~r/acs/amclct/~3/c0aozCJa-Fw/acsmedchemlett.9b00568

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From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Kyler W. Pugh†§, Zheng Zhang†§, Jian Wang‡, Xiuzhi Xu‡, Vitumbiko Munthali†, Ang Zuo†, and Brian S. J. Blagg*†
feedproxy.google.com/~r/acs/amclct/~3/DvHL7HIJA3M/acsmedchemlett.0c00100

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Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein–Protein Inhibitors: Two Test Cases Illustrated by IL1ß-IL1R and p38a–TAB1 Complexes

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Charlie Nichols†‡, Joseph Ng‡, Annika Keshu‡, Geoff Kelly§, Maria R. Conte‡, Michael S. Marber†, Franca Fraternali‡, and Gian F. De Nicola*†‡
feedproxy.google.com/~r/acs/jmcmar/~3/tZv_V9eYnzg/acs.jmedchem.0c00403

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Structure–Permeability Relationship of Semipeptidic Macrocycles—Understanding and Optimizing Passive Permeability and Efflux Ratio

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Antoine Le Roux†, E´milie Blaise†, Pierre-Luc Boudreault†, Christian Comeau†, Annie Doucet†, Marilena Giarrusso†, Marie-Pierre Collin‡, Thomas Neubauer‡, Florian Ko¨lling‡, Andreas H. Go¨ller‡, Lea Seep‡, Dieudonne´ T. Tshitenge‡, Matthias Wittwer‡, Maximilian Kullmann‡, Alexander Hillisch‡, Joachim Mittendorf‡, and Eric Marsault*†
feedproxy.google.com/~r/acs/jmcmar/~3/d6fSGIb2fLI/acs.jmedchem.0c00013

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Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Yinuo Wu†, Yi-Jing Tian†, Mei-Ling Le†, Si-Rui Zhang, Chen Zhang, Meng-Xing Huang, Mei-Yan Jiang, Bei Zhang, and Hai-Bin Luo*
feedproxy.google.com/~r/acs/jmcmar/~3/qK0-jTXihy8/acs.jmedchem.0c00711

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Aromatic Cytokinin Arabinosides Promote PAMP-like Responses and Positively Regulate Leaf Longevity

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Magdale´na Bryksova´†?, Siarhei Dabravolski‡?, Zuzana Kuc?erova´§?, Filip Zavadil Koka´s?‡?, Martina S?pundova´§, Lucie Pli´halova´†?, Toma´s? Taka´c?#, Jir?i´ Gru´z?, Martin Hudec?ek?, Veronika Hlous?kova´?, Radoslav Koprna†, Ondr?ej Nova´k?, Miroslav Strnad?, Ondr?ej Pli´hal*‡?, and Karel Dolez?al†?
feedproxy.google.com/~r/acs/acbcct/~3/SW_FCguQgVo/acschembio.0c00306

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Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Masakazu Atobe*†, Takayuki Serizawa†, Natsumi Yamakawa†#, Kenichiro Takaba†, Yukiko Nagano‡, Toshiaki Yamaura§, Eiichi Tanaka§, Atsutoshi Tazumi??, Shino Bito??, Masashi Ishiguro?, and Masashi Kawanishi†
feedproxy.google.com/~r/acs/jmcmar/~3/fJkqju23Wew/acs.jmedchem.0c00449

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Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Masakazu Atobe*†, Takayuki Serizawa†, Natsumi Yamakawa†#, Kenichiro Takaba†, Yukiko Nagano‡, Toshiaki Yamaura§, Eiichi Tanaka§, Atsutoshi Tazumi??, Shino Bito??, Masashi Ishiguro?, and Masashi Kawanishi†
feedproxy.google.com/~r/acs/jmcmar/~3/fJkqju23Wew/acs.jmedchem.0c00449

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Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Ulrich Lu¨cking*, Lars Wortmann*, Antje M. Wengner, Julien Lefranc, Philip Lienau, Hans Briem, Gerhard Siemeister, Ulf Bo¨mer, Karsten Denner, Martina Scha¨fer, Marcus Koppitz, Knut Eis, Florian Bartels, Benjamin Bader, Wilhelm Bone, Dieter Moosmayer, Simon J. Holton, Uwe Eberspa¨cher, Joanna Grudzinska-Goebel, Christoph Schatz, Gesa Deeg, Dominik Mumberg, and Franz von Nussbaum
feedproxy.google.com/~r/acs/jmcmar/~3/B9M1J_YSg7k/acs.jmedchem.0c00369

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COVID-19: Drug Targets and Potential Treatments

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Carmen Gil*†, Tiziana Ginex†, Ine´s Maestro†, Vanesa Nozal†, Luci´a Barrado-Gil†, Miguel A´ngel Cuesta-Geijo†, Jesu´s Urquiza‡, David Rami´rez§, Covadonga Alonso‡, Nuria E. Campillo†, and Ana Martinez*†
feedproxy.google.com/~r/acs/jmcmar/~3/9VBcRkWJ2Os/acs.jmedchem.0c00606

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Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Liu Hu†?, Xing Cai§?, Suzhen Dong§?, Yongjia Zhen†, Jidi Hu†, Shenjun Wang†, Jingwen Jiang†, Jiawu Huang†, Yuqiao Han§, Yu Qian*†‡, Yanqiu Yuan*†, and Wenhao Hu†‡
feedproxy.google.com/~r/acs/jmcmar/~3/gVn0SYaVCLs/acs.jmedchem.0c00079

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Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Liu Hu†?, Xing Cai§?, Suzhen Dong§?, Yongjia Zhen†, Jidi Hu†, Shenjun Wang†, Jingwen Jiang†, Jiawu Huang†, Yuqiao Han§, Yu Qian*†‡, Yanqiu Yuan*†, and Wenhao Hu†‡
feedproxy.google.com/~r/acs/jmcmar/~3/gVn0SYaVCLs/acs.jmedchem.0c00079

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Gadolinium-Based Neuroprognostic Magnetic Resonance Imaging Agents Suppress COX-2 for Prevention of Reperfusion Injury after Stroke

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Hee-Kyung Kim†‡, Jung-Jin Lee§, Garam Choi§?, Bokyung Sung?, Yeoun-Hee Kim§, Ah Rum Baek?, Soyeon Kim?, Huijin Song‡, Minsup Kim?, Art E. Cho?, Gang Ho Lee#, Sungjun Moon¶, Min-Kyoung Kang?, Jae Jun Lee?, and Yongmin Chang*???
feedproxy.google.com/~r/acs/jmcmar/~3/PEZr3AEFEmg/acs.jmedchem.0c00285

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