Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Design and Discovery of Novel Cyclic Peptides as EDPs–EBP Interaction Inhibitors for the Treatment of Liver Fibrosis
  by Nazi Song, Haonan Li, Qinglin Tang, Suijia Luo, Zihan Shi, Qian Zhao, Runkai Li, Yili Chen, Xiaoqing Cai, and Xianxing Jiang
• [ASAP] Design and Synthesis of Functionally Active 5‑Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1
  by Rebecca A. Gallego, Louise Bernier, Hui Chen, Sujin Cho-Schultz, Loanne Chung, Michael Collins, Matthew Del Bel, Jeff Elleraas, Cinthia Costa Jones, Ciaran N. Cronin, Martin Edwards, Xu Fang, Timothy Fisher, Mingying He, Jacqui Hoffman, Ruiduan Huo, Mehran Jalaie, Eric Johnson, Ted W. Johnson, Robert S. Kania, Manfred Kraus, Jennifer Lafontaine, Phuong Le, Tongnan Liu, Michael Maestre, Jean Matthews, Michele McTigue, Nichol Miller, Qiming Mu, Xulong Qin, Shijian Ren, Paul Richardson, Allison Rohner, Neal Sach, Li Shao, Graham Smith, Ruirui Su, Bin Sun, Sergei Timofeevski, Phuong Tran, Shuiwang Wang, Wei Wang, Ru Zhou, Jinjiang Zhu, and Sajiv K. Nair
• [ASAP] Design, Synthesis, and Biological Evaluation of Novel Hybrids Containing Dihydrochalcone as Tyrosinase Inhibitors to Treat Skin Hyperpigmentation
  by Songtao Xue⧧, Zhiwei Li, Xiaotong Ze⧧, Xiuyuan Wu⧧, Chen He⧧, Wen Shuai⧧, Maria Marlow, Jian Chen, David Scurr, Zheying Zhu, Jinyi Xu⧧, and Shengtao Xu⧧
• [ASAP] Discovery of a PDZ Domain Inhibitor Targeting the Syndecan/Syntenin Protein–Protein Interaction: A Semi-Automated “Hit Identification-to-Optimization” Approach
  by Laurent Hoffer, Manon Garcia, Raphael Leblanc, Mikael Feracci, Stéphane Betzi, Khaoula Ben Yaala, Avais M. Daulat, Pascale Zimmermann, Philippe Roche, Karine Barral, and Xavier Morelli
• [ASAP] Application and Study of ROCK Inhibitors in Pulmonary Fibrosis: Recent Developments and Future Perspectives
  by Yuting Xie, Lin Yue, Yaojie Shi, Xingping Su, Cailing Gan, Hongyao Liu, Taixiong Xue, and Tinghong Ye
• [ASAP] Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response
  by Nan Sun, Kexin Yang, Wenzhong Yan, Mingyue Yao, Chengcheng Yu, Wenwen Duan, Xiaoke Gu, Dong Guo, Hualiang Jiang, Chengying Xie, and Jianjun Cheng
• [ASAP] Fluorine-18-Labeled Diaryl-azines as Improved β‑Amyloid Imaging Tracers: From Bench to First-in-Human Studies
  by Yuying Li, Kaixiang Zhou, Xiaojun Zhang, Hailong Zhao, Xiaoming Wang, Ruilin Dong, Yan Wang⊗, Baian Chen, Xiao-xin Yan⊗, Jiapei Dai, Yanying Sui, Jinming Zhang, and Mengchao Cui
• [ASAP] BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α_2B Antagonist
  by Daniel Meibom, Jutta Meyer, Clemens-Jeremias von Buehler, Karl D. Collins, Stefanie Maassen, Kersten Matthias Gericke, Jörg Hüser, Joachim Mittendorf, Nuria Ortega Hernandez, Jens Schamberger, Jan Stampfuss, Alexander Straub, Afra Torge, Norbert Witowski, and Frank Wunder
• [ASAP] Discovery of <bold>LL-K8-22</bold>: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex
  by Mingyu Wang, Rongkun Lin, Jiacheng Li, Yuying Suo, Jing Gao, Liping Liu, Liyuan Zhou, Yicheng Ni, Ziqun Yang, Jie Zheng, Jin Lin, Hu Zhou, Cheng Luo, and Hua Lin
• [ASAP] Discovery of a Promising Fluorine-18 Positron Emission Tomography Radiotracer for Imaging Sphingosine-1-Phosphate Receptor 1 in the Brain
  by Lin Qiu, Hao Jiang, Charles Zhou, Jinzhi Wang, Yanbo Yu, Haiyang Zhao, Tianyu Huang, Robert Gropler, Joel S. Perlmutter, Tammie L. S. Benzinger, and Zhude Tu

ACS Medicinal Chemistry Letters

• [ASAP] Targeting the “Undruggable” Driver Protein, KRAS^G12D, as Potential Therapy in Prostate Cancer
  by Robert B. Kargbo
• [ASAP] Discovery of Potent Deuterated Compounds as Potential KRAS^G12D Inhibitors in Cancer Therapy
  by Robert B. Kargbo
• [ASAP] A Shift in Thinking: Cellular Thermal Shift Assay-Enabled Drug Discovery
  by Isabel Martín Caballero and Stina Lundgren
• [ASAP] ChemBeads-Enabled Photoredox High-Throughput Experimentation Platform to Improve C(sp²)–C(sp³) Decarboxylative Couplings
  by Nathan J. Gesmundo, Noah P. Tu, Kathy A. Sarris, and Ying Wang
• [ASAP] Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery
  by Alexander Neumann, Lester Marrison, and Raphael Klein
• [ASAP] Orally Active Forms of DMT, 5‑MeO-DMT, and Long-Acting MDMA for the Treatment of Neuropsychiatric Disorders
  by Robert B. Kargbo
• [ASAP] Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry
  by Agata Gitlin-Domagalska, Dawid Dębowski, Aleksandra Maciejewska, Sergey Samsonov, Martyna Maszota-Zieleniak, Natalia Ptaszyńska, Anna Łęgowska, and Krzysztof Rolka
• [ASAP] The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders
  by Simon Poulter, Nigel Austin, Rachel Armstrong, Matt Barnes, Sarah Joanne Bucknell, Alicia Higueruelo, Joydeep Banerjee, Andy Mead, Richard Mould, Cliona MacSweeney, M. Alistair O’Brien, Lisa Alice Stott, and Stephen P. Watson
• [ASAP] Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2
  by Zachary W. Davis-Gilbert, Andreas Krämer, James E. Dunford, Stefanie Howell, Filiz Senbabaoglu, Carrow I. Wells, Frances M. Bashore, Tammy M. Havener, Jeffery L. Smith, Mohammad A. Hossain, Udo Oppermann, David H. Drewry, and Alison D. Axtman
• [ASAP] Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use
  by Satoru Ito, Sachie Otsuki, Hirokazu Ohsawa, Atsushi Hirano, Hideki Kazuno, Satoshi Yamashita, Kosuke Egami, Yoshihiro Shibata, Ikuo Yamamiya, Fumiaki Yamashita, Yasuo Kodama, Kaoru Funabashi, Hiromi Kazuno, Toshiharu Komori, Satoshi Suzuki, Hiroshi Sootome, Hiroshi Hirai, and Takeshi Sagara

Journal of Natural Products

• [ASAP] Antiangiogenic Pterocarpan and Flavonoid Constituents of <italic toggle="yes">Erythrina lysistemon</italic>
  by Sarah M. Nassief, Masouda E. Amer, Eman Shawky, Kamakshi Sishtla, Eduard Mas-Claret, Anbukkarasi Muniyandi, Timothy W. Corson, Dulcie A. Mulholland, and Sawsan El-Masry
• [ASAP] Nicolaioidesin C: An Antiausterity Agent Shows Promising Antitumor Activity in a Pancreatic Cancer Xenograft Mouse Model
  by Nguyen Duy Phan, Ashraf M. Omar, Ikue Takahashi, Hayato Baba, Tomoyuki Okumura, Johji Imura, Takuya Okada, Naoki Toyooka, Tsutomu Fujii, and Suresh Awale
• [ASAP] Pauciflorins A–E, Unexpected Chromone–Monoterpene-Derived Meroterpenoids from <italic toggle="yes">Centrapalus pauciflorus</italic>
  by Gordana Krstić, Muhammad Bello Saidu, Petra Bombicz, Sourav De, Hazhmat Ali, István Zupkó, Róbert Berkecz, Umar Shehu Gallah▽, Dóra Rédei, and Judit Hohmann
• [ASAP] Dendrillic Acids A and B: Nitrogenous, Rearranged Spongian Nor-Diterpenes from a <italic toggle="yes">Dendrilla</italic> sp. Marine Sponge
  by Samuele Sala, Patrick J. C. James, Gareth L. Nealon, Jane Fromont, Oliver Gomez, Daniel Vuong, Ernest Lacey, and Gavin R. Flematti
• [ASAP] Discovery and Biosynthesis of Imidazolium Antibiotics from the Probiotic <italic toggle="yes">Bacillus licheniformis</italic>
  by Song Lim Ham, Tae Hyun Lee, Kyung Jun Kim, Jung Ha Kim, Su Jung Hwang, Sun Ho Lee, Jae Sik Yu, Ki Hyun Kim, Hyo-Jong Lee, Wonsik Lee, and Chung Sub Kim
• [ASAP] Sadopeptins A and B, Sulfoxide- and Piperidone-Containing Cyclic Heptapeptides with Proteasome Inhibitory Activity from a <italic toggle="yes">Streptomyces</italic> sp.
  by Jiyoon Park, Jiseong Kim, Sunghoon Hwang, Daehyun Oh, Young Eun Du, Sang-Jip Nam, Hyeung-geun Park, Min Jae Lee, and Dong-Chan Oh
• [ASAP] Aromatic Polyketides from the Mangrove-Derived <italic toggle="yes">Streptomyces</italic> sp. SCSIO 40069
  by Lili Sun, Hanning Zhu, Liping Zhang, Yiguang Zhu, Disna Ratnasekera, Changsheng Zhang, and Qingbo Zhang
• [ASAP] Exploring the Limits of Cyanobactin Macrocyclase PatGmac: Cyclization of PawS-Derived Peptide Sunflower Trypsin Inhibitor‑1 and Cyclotide Kalata B1
  by Taj Muhammad, Wael E Houssen, Louise Thomas, Cristina-Nicoleta Alexandru-Crivac▽, Sunithi Gunasekera, Marcel Jaspars, and Ulf Göransson
• [ASAP] High-Resolution Liquid Chromatography–Mass Spectrometry-Based Metabolomics for the Classification of <italic toggle="yes">Chuquiraga</italic> (Barnadesioideae, Asteraceae): New Phenylpropanoid Derivatives as Chemical Markers for <italic toggle="yes">Chuquiraga spinosa</italic>
  by Gari V. Ccana-Ccapatinta, Guillermo F. Padilla-Gonzalez, Paola L. Ferreira, Marcelo Monge, Joao Semir, Milton Groppo, and Fernando B. Da Costa
• [ASAP] Metabolite and Molecular Characterization of <italic toggle="yes">Mitragyna speciosa</italic> Identifies Developmental and Genotypic Effects on Monoterpene Indole and Oxindole Alkaloid Composition
  by Larissa C. Laforest, Michelle A. Kuntz, Siva Rama Raju Kanumuri, Sushobhan Mukhopadhyay, Abhisheak Sharma, Sarah E. O’Connor, Christopher R. McCurdy, and Satya Swathi Nadakuduti