Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Synthetic Peptides That Antagonize the Angiotensin-Converting Enzyme-2 (ACE-2) Interaction with SARS-CoV-2 Receptor Binding Spike Protein
  by Afsaneh Sadremomtaz, Zayana M. Al-Dahmani, Angel J. Ruiz-Moreno, Alessandra Monti, Chao Wang, Taha Azad, John C. Bell, Nunzianna Doti, Marco A. Velasco-Velázquez, Debora de Jong, Jrgen de Jonge, Jolanda Smit, Alexander Dömling, Harry van Goor, and Matthew R. Groves
• [ASAP] Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2<italic toggle="yes">H</italic>-benzo[<italic toggle="yes">b</italic>][1,4]oxazin-6-yl Moiety
  by Shuhei Ikeda, Hideyuki Sugiyama, Hidekazu Tokuhara, Masataka Murakami, Minoru Nakamura, Yuya Oguro, Jumpei Aida, Nao Morishita, Satoshi Sogabe, Douglas R. Dougan, Sean C. Gay, Ling Qin, Naoto Arimura, Yasuko Takahashi, Masako Sasaki, Yusuke Kamada, Kazunobu Aoyama, Kouya Kimoto, and Makoto Kamata
• [ASAP] Design and Synthesis of Novel c-di-GMP G-Quadruplex Inducers as Bacterial Biofilm Inhibitors
  by Teng-Fei Xuan, Zi-Qiang Wang, Jun Liu, Hai-Tao Yu, Qian-Wen Lin, Wei-Min Chen, and Jing Lin
• [ASAP] Molecular Plasticity of Crystalline CK2α′ Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity
  by Dirk Lindenblatt, Violetta Applegate, Anna Nickelsen, Merlin Klußmann, Ines Neundorf, Claudia Götz, Joachim Jose, and Karsten Niefind
• [ASAP] Identification of Thieno[3,2-<italic toggle="yes">d</italic>]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3
  by Hanna Cho, Injae Shin, Hojong Yoon, Eunhye Jeon, Jiwon Lee, Younghoon Kim, SeongShick Ryu, Chiman Song, Nam Hoon Kwon, Youngji Moon, Sunghoon Kim, Nam Doo Kim, Hwan Geun Choi, and Taebo Sim
• [ASAP] Emerging Approaches to Overcome Acquired Drug Resistance Obstacles to Osimertinib in Non-Small-Cell Lung Cancer
  by Matin Shaikh, Yashodeep Shinde, Rahul Pawara, Malleshappa Noolvi, Sanjay Surana, Iqrar Ahmad, and Harun Patel
• [ASAP] Nitric Oxide Photo-Donor Hybrids of Ciprofloxacin and Norfloxacin: A Shift in Activity from Antimicrobial to Anticancer Agents
  by Antonino Nicolò Fallica, Carla Barbaraci, Emanuele Amata, Lorella Pasquinucci, Rita Turnaturi, Maria Dichiara, Sebastiano Intagliata, Marzia Bruna Gariboldi, Emanuela Marras, Viviana Teresa Orlandi, Claudia Ferroni, Cecilia Martini, Antonio Rescifina, Davide Gentile, Greta Varchi, and Agostino Marrazzo
• [ASAP] Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery
  by Guoqiang Dong, Yu Ding, Shipeng He, and Chunquan Sheng
• [ASAP] Terphenyl-Based Small-Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein–Protein Interaction
  by Damian Muszak, Ewa Surmiak, Jacek Plewka, Katarzyna Magiera-Mularz, Justyna Kocik-Krol, Bogdan Musielak, Dominik Sala, Radoslaw Kitel, Malgorzata Stec, Kazimierz Weglarczyk, Maciej Siedlar, Alexander Dömling, Lukasz Skalniak, and Tad A. Holak
• [ASAP] 3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents
  by Sho Konno, Kiyotaka Kobayashi, Miki Senda, Yuta Funai, Yuta Seki, Ikumi Tamai, Laura Schäkel, Kyousuke Sakata, Thanigaimalai Pillaiyar, Akihiro Taguchi, Atsuhiko Taniguchi, Michael Gütschow, Christa E. Müller, Koh Takeuchi, Mikako Hirohama, Atsushi Kawaguchi, Masaki Kojima, Toshiya Senda, Yoshiyuki Shirasaka, Wataru Kamitani, and Yoshio Hayashi

ACS Medicinal Chemistry Letters

• [ASAP] Use of Crystallography and Molecular Modeling for the Inhibition of the Botulinum Neurotoxin A Protease
  by Lewis D. Turner, Alexander L. Nielsen, Lucy Lin, Antonio J. Campedelli, Nicholas R. Silvaggi△, Jason S. Chen, Amanda E. Wakefield, Karen N. Allen, and Kim D. Janda
• [ASAP] Discovery of Small Molecule Entry Inhibitors Targeting the Fusion Peptide of SARS-CoV-2 Spike Protein
  by Xin Hu, Catherine Z. Chen, Miao Xu, Zongyi Hu, Hui Guo, Zina Itkin, Paul Shinn, Parker Ivin, Madeleine Leek, T. Jake Liang, Min Shen, Wei Zheng, and Matthew D. Hall
• [ASAP] Ugi Reaction Synthesis of Oxindole–Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors
  by Pedro Brandão, Óscar López, Luisa Leitzbach, Holger Stark, José G. Fernández-Bolaños, Anthony J. Burke, and Marta Pineiro
• [ASAP] Exploring Ligand-Directed <italic toggle="yes">N</italic>-Acyl-<italic toggle="yes">N</italic>-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development
  by Mingxing Teng, Jie Jiang, Scott B. Ficarro, Hyuk-Soo Seo, Jae Hyun Bae, Katherine A. Donovan, Eric S. Fischer, Tinghu Zhang, Sirano Dhe-Paganon, Jarrod A. Marto, and Nathanael S. Gray
• [ASAP] Novel Carbazoles for Treating Inflammatory and Autoimmune Diseases
  by Ram W. Sabnis
• [ASAP] Novel Substituted Heterocyclic and Heteroaryl Compounds for Treating Huntington’s Disease
  by Ram W. Sabnis
• [ASAP] A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists
  by Elisia Villemure, Jack A. Terrett, Robin Larouche-Gauthier, Martin Déry, Huifen Chen, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Steven Magnuson, and Matthew Volgraf
• [ASAP] Novel Compounds for Treating Malaria
  by Ram W. Sabnis
• [ASAP] Discovery of the First Non-cGMP Mimetic Small Molecule Activators of cGMP-Dependent Protein Kinase 1 α (PKG1α)
  by Jennifer Hanisak, Aileen Soriano, Gregory C. Adam, Andrea Basso, David Bauman, David Bell, Emily Frank, Gregory O’Donnell, Paul Tawa, Andreas Verras, Yang Yu, Lei Zhang▼, and W. Michael Seganish
• [ASAP] Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology
  by Min Lu, Hongjun Zhang, Derun Li, Matthew Childers, Qinglin Pu, Rachel L. Palte, Symon Gathiaka, Thomas W. Lyons, Anandan Palani, Peter W. Fan, Peter Spacciapoli, J. Richard Miller, Hyelim Cho, Mangeng Cheng, Kalyan Chakravarthy, Jennifer O’Neil, Padmanabhan Eangoor, Adam Beard, Hai-Young Kim, Josep Saurí, Hakan Gunaydin, David L. Sloman, Phieng Siliphaivanh, Jared Cumming, and Christian Fischer

Journal of Natural Products

• [ASAP] Visible-Light-Promoted Biomimetic Reductive Functionalization of Quaternary Benzophenanthridine Alkaloids
  by Lin Wang, Xinhao Wang, Wei Wang, Wei Liu, Yisong Liu, Hongqi Xie, Oliver Reiser, Jianguo Zeng, and Pi Cheng
• [ASAP] Saccharochelins A–H, Cytotoxic Amphiphilic Siderophores from the Rare Marine Actinomycete <italic toggle="yes">Saccharothrix</italic> sp. D09
  by Qiyao Shen, Guangzhi Dai, Vinothkannan Ravichandran, Yang Liu, Lin Zhong, Haiyan Sui, Xiangmei Ren, Nianzhi Jiao, Youming Zhang, Haibo Zhou, and Xiaoying Bian
• [ASAP] Synthesis and Biological Evaluation of Falcarinol-Type Analogues as Potential Calcium Channel Blockers
  by Yang Li, Wan-Li Tan, Kai Guo, Xiao-Wei Gao, Jun Wei, Dong Yi, Chun Zhang, and Qin Wang
• [ASAP] Phormidepistatin from the Cyanobacterium UIC 10484: Assessing the Phylogenetic Distribution of the Statine Pharmacophore
  by Peter Sullivan, Aleksej Krunic, Lydia J. Davis, Hwan Seung Kim, Joanna E. Burdette, and Jimmy Orjala
• [ASAP] Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling
  by Edin Muratspahić, Nataša Tomašević, Shahrooz Nasrollahi-Shirazi, Jasmin Gattringer, Fabiola Susanna Emser, Michael Freissmuth, and Christian W. Gruber
• [ASAP] Δ⁹-<italic toggle="yes">cis</italic>-Tetrahydrocannabinol: Natural Occurrence, Chirality, and Pharmacology
  by Michael A. Schafroth, Giulia Mazzoccanti, Ines Reynoso-Moreno, Reto Erni, Federica Pollastro∧, Diego Caprioglio∧, Bruno Botta, Gianna Allegrone∧, Giulio Grassio, Andrea Chicca, Francesco Gasparrini, Jürg Gertsch, Erick M. Carreira, and Giovanni Appendino∧
• [ASAP] Cyclic, Hydrophobic Hexapeptide Fusahexin Is the Product of a Nonribosomal Peptide Synthetase in <italic toggle="yes">Fusarium graminearum</italic>
  by Klaus R. Westphal, Simone Bachleitner, Manja M. Severinsen, Mathias L. Brundt, Frederik T. Hansen, Trine Srensen, Rasmus D. Wollenberg, Erik Lyse, Lena Studt, Jens L. Srensen, Teis E. Sondergaard, and Reinhard Wimmer
• [ASAP] Fusaricide is a Novel Iron Chelator that Induces Apoptosis through Activating Caspase-3
  by Yaling Hui, Ting Tang, Jing Wang, Huanhuan Zhao, Hong-Ying Yang, Junmin Xi, Baoxin Zhang, Jianguo Fang, Kun Gao, and Yueting Wu
• [ASAP] Advancements in Natural Products Research from Central and South America: A Virtual Issue
  by Roberto G. S. Berlinck(Associate Editor, Journal of Natural Products) and Philip J. Proteau(Editor-in-Chief, Journal of Natural Products)
• [ASAP] Precursor Supply Increases the Accumulation of 4-Hydroxy-6-(4-hydroxyphenyl)-α-pyrone after NRPS–PKS Gene Expression
  by Wen Li, Jie Fan, Ge Liao, Wen-Bing Yin, and Shu-Ming Li