ASAP Science Feeds

Journal of Medicinal Chemistry

• The Phenotypic Hit-to-Probe Challenge
  by Sven Herschel, Thomas Ullrich, Enrico Schmidt, Jean Quancard, and Dennis Schade
• Ligand-Dependent Affinity but State-Dominated Efficacy in Structure-Based GPCR Pharmacology Prediction
  by Jianxiang Huang, Xin Qiao, Chunhao Zhu, Xiaobing Lan, and Shaoyong Lu
• Rethinking log P : Lipophilicity =̷ Hydrophobicity
  by Michael D. Shultz and Eric J. Martin
• Discovery of Anti-apoptotic BAX Inhibitors
  by Marta Diceglie, Jörg Contzen, Andreas Oder, Arundhasa Chandrabalan, Max Ruwolt, Justin Kale, Anton F. Ketzel, Scott Houliston, Edgar Specker, Silke Radetzki, Keven Mallow, Lina Hellwig, Annette Aigner, Martin Neuenschwander, Justin Philip Pogmore, Tao Xin, Rima Al-Awar, David E. Uehling, Han Sun, Fan Liu, Jens Peter von Kries, David W. Andrews, Philipp Mergenthaler, and Marc Nazaré
• Discovery of Indazole-Based Dual-Pharmacophore Inhibitors of Dengue and Zika Proteases as Promising Antivirals
  by Shubham K. Singh, Vijayarani Potluri, Surabhi Naza, Raveendra Madhukar Bhat, Poonam Patil, Hemavarshine M. S, Bhavita Kattula, Sarvalakshmi Pusarapu, Kalichamy Alagarasu, Rangappa S. Keri, Deepti Parashar, Anthony Addlagatta, and Pragati K. Prasad
• Discovery of Tricyclic Oxazinoquinolinone-Based BCL6 PROTAC Degraders with Potent Activity Against Diffuse Large B-Cell Lymphoma
  by Xuetao Chen, Rujun Xu, Xiaoran Wang, Huidan Wu, Nan Wang, Xin Huang, Wenjing Kang, Qidong You, Xiaoke Guo, and Zhengyu Jiang
• Discovery of GTA182, a Novel CNS-Active Tricyclic Amide MTA-Cooperative PRMT5 Inhibitor for MTAP -Deleted Cancers
  by Bing Yao, Weifeng Mao, Minghua Wang, Junqing Zhang, Shanshan Xie, Kai Cheng, Xinbo Hu, Wei Liu, Xiangping Zhang, Zhengqing Zhu, James D. Joseph, Mingxi Li, Xiaohui Gu, and Fred Aswad
• Structure-Guided Discovery of Orally Bioavailable Allosteric SLC6A19 Inhibitors that Promote Urinary Amino Acid Excretion In Vivo
  by Tao Wang, Matthew S. Dowling, Dahui Zhou, David Jonathan Wasilko, Meihua Tu, Denis Feliers, Barbara Bernardo, Joseph Tillotson, Wenzhe Ma, Janice Brown, Zachary Johnson, Joshua A. Lees, Andrew Fensome, Andre Shavnya, Jennifer Clemens, Steven Coffey, Caroline A. Blakemore, Melissa Avery, Jamison B. Tuttle, Phillip Hudson, Magdalena Korczynska, John Murray, Jade Williams, Jun Xiao, Jason Dutra, Dianne Hernandez, Kevin D. Hesp, Vincent Mascitti, Srinath Jagarlapudi, Rose Keenan, Jessica Ward, Robert Barnes, Emily Jordan, Natalie Ochocki, Daniel Callahan, Kimberly Steen, Amit S. Kalgutkar, Kari R. Fonseca, Raman Sharma, Nicholas Ferguson, Amanda King-Ahmad, Andrew J. Bessire, Amy Moody, Tristan S. Maurer, Ingrid A. Stock, Ruth Sommese, Tracy Phillips, Paula M. Loria, Huixian Wu, David Hepworth, Matthew F. Sammons, Lei Zhang, and Yuan Zhang
• Discovery and Optimization of Anticancer Dibenzothiazepinones That Target the Ribosome Biogenesis Factor NVL
  by Ye Tao, Holly H. Guo, Victor E. Cruz, Divya Reddy, Ashley Leach, Noelle S. Williams, Arin B. Aurora, Vishal Khivansara, Yan Han, Jan P. Erzberger, Deepak Nijhawan, and Jef K. De Brabander
• Medicinal Chemistry Strategies for Targeting RNA-Binding Proteins: Design, Optimization, and Therapeutic Potential
  by Bangbang Li, Hao Shen, Zeliang Xu, Yixi Wang, Jiayu Ding, Zhongrui Shi, Chengliang Sun, Peng Yang, and Xiao Wang

Journal of Medicinal Chemistry – Current Issue

• Issue Publication Information
• Issue Editorial Masthead
• Structure-Affinity and Selectivity of Aryl-Sulfamates as Inhibitors of Carbonic Anhydrase IX
• An Innovative Auto-Antagonistic Multi-Target Strategy: MOR/DOR/NPFFR 2 Agonists Achieve Separation of Analgesia from Side Effects
• Mapping the N/OFQ(1−13)-NH 2 Address Domain to Identify G Protein-Biased NOP Receptor Agonists

Journal of Medicinal Chemistry Letters

• A Nontoxin Aminopyrimidine Probe for Near State-Independent Na V 1.7 Inhibition
• Novel Compounds as Glucagon-Like Peptide-1 Receptor Agonists for Treating Type 2 Diabetes Mellitus and Obesity
• Discovery of Small Peptides as Dual Inhibitors of IL-4 and IL-13 Signaling
• Design, Synthesis, and Comparative Selection Analysis of a Chemically Diverse Peptide-Like DNA-Encoded Library

Journal of Natural Products

• Eudesmane Sesquiterpenoids from Dregea Volubilis Suppress Kidney Stones via Akt Signalling to Inhibit Oxalate Biosynthesis in Drosophila
• Computationally-Guided Structure Revision of the Chartellamides
• Phenolic Metabolites as Therapeutics for Chronic Diseases: One Researcher’s PAINS Is Another’s Translatable Polypharmacology
• Identification and Spatial Distribution of Long-Chain Alkyl Sulfates from the Solitary Ascidian Ascidiella aspersa
• Chrysanthevelides A−D, the Rearranged 5/5/5 Tricyclic Spiro-Guaianolides and 1, 3-Dioxolane-Containing Nor-Guaianolide Dimers from Chrysanthemum vestitum Target PKM2 to Mediate the Anti-Inflammatory Effect