Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Potent Ruthenium–Ferrocene Bimetallic Antitumor Antiangiogenic Agent That Circumvents Platinum Resistance: From Synthesis and Mechanistic Studies to <italic toggle="yes">In Vivo</italic> Evaluation in Zebrafish
  by Manikandan M, Shubhankar Gadre, Sushanta Chhatar, Gourav Chakraborty, Naushad Ahmed, Chinmoy Patra, and Malay Patra
• [ASAP] Development of SOS1 Inhibitor-Based Degraders to Target <italic toggle="yes">KRAS</italic>-Mutant Colorectal Cancer
  by Yujia Bian, Diego Alem, Francisca Beato, Tara L. Hogenson, Xinrui Yang, Kun Jiang, Jianfeng Cai, Wen Wee Ma, Martin Fernandez-Zapico, Aik Choon Tan, Nicholas J. Lawrence, Jason B. Fleming, Yu Yuan, and Hao Xie
• [ASAP] The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation
  by Jana Flegel, Saad Shaaban&, Zhi Jun Jia, Britta Schulte, Yilong Lian, Adrian Krzyzanowski, Malte Metz, Tabea Schneidewind, Fabian Wesseler, Anke Flegel, Alisa Reich, Alexandra Brause, Gang Xue, Minghao Zhang, Lara Dötsch, Isabelle D. Stender, Jan-Erik Hoffmann, Rebecca Scheel, Petra Janning, Fraydoon Rastinejad, Dennis Schade, Carsten Strohmann, Andrey P. Antonchick◊, Sonja Sievers, Pedro Moura-Alves, Slava Ziegler, and Herbert Waldmann
• [ASAP] A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives
  by Si Ha, Guoshun Luo, and Hua Xiang
• [ASAP] Heterobivalent Inhibitors of Acetyl-CoA Carboxylase: Drug Target Residence Time and Time-Dependent Antibacterial Activity
  by Matthew T. Cifone, YongLe He, Rajeswari Basu, Nan Wang, Shabnam Davoodi, Lauren A. Spagnuolo, Yuanyuan Si, Taraneh Daryaee⧫, Craig E. Stivala, Stephen G. Walker, and Peter J. Tonge
• [ASAP] Discovery of Orally Bioavailable <italic toggle="yes">N</italic>‑Benzylpiperidinol Derivatives as Potent and Selective USP7 Inhibitors with In Vivo Antitumor Immunity Activity against Colon Cancer
  by Xing Li, Shanlin Yang, Honghan Zhang, Xipeng Liu, Yuchen Gao, Yuqi Chen, Liu Liu, Dalin Wang, Zijiang Liang, Shengjie Liu, Liang Dai, Qinglong Xu, Haoliang Yuan, Caiping Chen, Hongbin Sun, and Xiaoan Wen
• [ASAP] Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
  by Emily J. Hanan, Marie-Gabrielle Braun, Robert A. Heald, Calum MacLeod, Connie Chan, Saundra Clausen, Kyle A. Edgar, Charles Eigenbrot, Richard Elliott, Nicholas Endres, Lori S. Friedman, Emily Gogol, Xiao-Hui Gu, Rebecca Hong Thibodeau, Philip S. Jackson, James R. Kiefer, Jamie D. Knight, Michelle Nannini, Raman Narukulla, Amanda Pace⧫, Jodie Pang, Hans E. Purkey, Laurent Salphati, Deepak Sampath, Stephen Schmidt, Steve Sideris, Kyung Song, Swathi Sujatha-Bhaskar, Mark Ultsch, Heidi Wallweber, Jianfeng Xin, SiewKuen Yeap, Amy Young, Yu Zhong, and Steven T. Staben
• [ASAP] Transcriptional Inhibition of MicroRNA miR-122 by Small Molecules Reduces Hepatitis C Virus Replication in Liver Cells
  by Cole Emanuelson, Nicholas Ankenbruck, Rohan Kumbhare, Meryl Thomas, Colleen Connelly, Yasmine Baktash, Glenn Randall, and Alexander Deiters
• [ASAP] Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer
  by Guoquan Wan, Zhanzhan Feng, Qiangsheng Zhang, Xiao Li, Kai Ran, Huan Feng, Tianwen Luo, Shuyan Zhou, Chang Su, Wei Wei, Ningyu Wang, Chao Gao, Lifeng Zhao, and Luoting Yu
• [ASAP] Optimization of 1,2,4-Triazole-3-thiones toward Broad-Spectrum Metallo-β-lactamase Inhibitors Showing Potent Synergistic Activity on VIM- and NDM-1-Producing Clinical Isolates
  by Alice Legru, Federica Verdirosa, Yen Vo-Hoang, Giusy Tassone, Filippo Vascon, Caitlyn A. Thomas, Filomena Sannio, Giuseppina Corsica, Manuela Benvenuti, Georges Feller, Rémi Coulon, Francesca Marcoccia, Savannah Rowane Devente, Ezeddine Bouajila, Catherine Piveteau, Florence Leroux, Rebecca Deprez-Poulain, Benoît Deprez, Patricia Licznar-Fajardo, Michael W. Crowder, Laura Cendron, Cecilia Pozzi, Stefano Mangani, Jean-Denis Docquier, Jean-François Hernandez, and Laurent Gavara

ACS Medicinal Chemistry Letters

• [ASAP] Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure–Activity Relationship
  by Laura Figuerola-Asencio, Paula Morales, Pingwei Zhao, Dow P. Hurst, Sommayah S. Sayed, Katsuya L. Colón, María Gómez-Cañas, Javier Fernández-Ruiz, Mitchell P. Croatt, Patricia H. Reggio, Mary E. Abood, and Nadine Jagerovic
• [ASAP] ATP Mimetic Attack on the Nucleotide-Binding Domain to Overcome ABC Transporter Mediated Chemoresistance
  by Tatyana A. Grigoreva, Aleksandra V. Sagaidak, Svetlana V. Vorona, Daria S. Novikova, and Vyacheslav G. Tribulovich
• [ASAP] Identification of a Target Site for Covalent Inhibition of Protein Phosphohistidine Phosphatase 1
  by Hyeong Jun Kim, Hoyoung Jung, Soyeon Kim, Jeong Kon Seo, and Jung-Min Kee
• [ASAP] From Oxetane to Thietane: Extending the Antiviral Spectrum of 2′-Spirocyclic Uridines by Substituting Oxygen with Sulfur
  by Sandrine Grosse, Abdellah Tahri, Pierre Raboisson, Yannis Houpis, Bart Stoops, Edgar Jacoby, Jean-Marc Neefs, Marnix Van Loock, Olivia Goethals, Peggy Geluykens, Jean-François Bonfanti, and Tim H. M. Jonckers
• [ASAP] Pyrazolidine Carboxamide Analogs as Selective Agonists of the Cannabinoid 2 Receptor
  by Gerard Rosse
• [ASAP] Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)
  by David E. Heppner, Florian Wittlinger, Tyler S. Beyett, Tatiana Shaurova, Daniel A. Urul, Brian Buckley, Calvin D. Pham, Ilse K. Schaeffner, Bo Yang, Blessing C. Ogboo, Earl W. May, Erik M. Schaefer, Michael J. Eck, Stefan A. Laufer, and Pamela A. Hershberger
• [ASAP] Potent PROTACs Targeting EGFR Mutants in Drug Discovery
  by Robert B. Kargbo
• [ASAP] Discovery of Potent PROTACs for the Potential Treatment of Leukemia
  by Robert B. Kargbo
• [ASAP] Emerging Proteolysis Targeting Antibodies (PROTABs) for Application in Cancer Therapy
  by Robert B. Kargbo
• [ASAP] Potential Therapeutic Transdermal Psychoactive Drug Delivery Technology
  by Robert B. Kargbo

Journal of Natural Products

• [ASAP] Polycyclic Polyprenylated Acylphloroglucinols Bearing a Lavandulyl-Derived Substituent from <italic toggle="yes">Garcinia xanthochymus</italic> Fruits
  by Zhi-Hong Xu, Robert B. Grossman, Yu-Feng Qiu, Yang Luo, Tian Lan, and Xing-Wei Yang
• [ASAP] Antitumor Activity of Piceamycin by Upregulation of N‑Myc Downstream-Regulated Gene 1 in Human Colorectal Cancer Cells
  by Kay Zin Kyaw, Woong Sub Byun, Yern-Hyerk Shin, Thanh-Hau Huynh, Ji Yun Lee, Eun Seo Bae, Hyen Joo Park, Dong-Chan Oh, and Sang Kook Lee
• [ASAP] Discovery of Efrotomycin Congeners and Heterologous Expression-Based Insights into the Self-Resistance Mechanism
  by Chunyan Fang, Qingbo Zhang&, Wenjun Zhang&, Changsheng Zhang&, and Yiguang Zhu&
• [ASAP] Synthesis and Bioactivity of Thiocarboxylic A and Derivatives
  by Franziska Gillsch, Fredrick Mbui, Ursula Bilitewski, and Rainer Schobert
• [ASAP] Meroantarctines A–C, Meroterpenoids with Rearranged Skeletons from the Alga-Derived Fungus <italic toggle="yes">Penicillium antarcticum</italic> KMM 4685 with Potent p‑Glycoprotein Inhibitory Activity
  by Elena V. Leshchenko, Alexandr S. Antonov, Sergey A. Dyshlovoy, Dmitrii V. Berdyshev, Jessica Hauschild, Olesya I. Zhuravleva, Gleb V. Borkunov, Alexander S. Menshov, Natalya N. Kirichuk, Roman S. Popov, Andrey V. Gerasimenko, Anatoly A. Udovenko, Markus Graefen, Carsten Bokemeyer, Gunhild von Amsberg, and Anton N. Yurchenko
• [ASAP] Concise Biosynthesis of Tropone-Containing Spiromaterpenes by a Sesquiterpene Cyclase and a Multifunctional P450 from a Deep-Sea-Derived <italic toggle="yes">Spiromastix</italic> sp. Fungus
  by Jie Liu, Xiang Guo, Xingchen Guo, Boyuan Zhong, Tao Wang, Dong Liu, Hongwei Jin, Jinwei Ren, Zihe Liu, Jiangtao Gao□, Shu-Ming Li, Aili Fan, and Wenhan Lin
• [ASAP] Selective Inhibition of PTP1B by New Anthraquinone Glycosides from <named-content content-type="genus-species" xlink:type="simple">Knoxia valerianoides</named-content>
  by Zheng Zhang, Zhi-Peng Shang, Yan Jiang, Zhao-Xia Qu, Ren-Yong Yang, Jing Zhang, Ye-Xi Lin, and Feng Zhao
• [ASAP] Evaluating the <italic toggle="yes">in Vitro</italic> Efficacy of Quassinoids from <italic toggle="yes">Eurycoma longifolia</italic> and <italic toggle="yes">Eurycoma harmandiana</italic> against Common Cold Human Coronavirus OC43 and SARS-CoV‑2 Using In-Cell Enzyme-Linked Immunosorbent Assay
  by Rattanathorn Choonong, Sasiporn Ruangdachsuwan, Theeraporn Churod, Somnuek Palabodeewat, Surat Punyahathaikul, Sanjira Juntarapornchai, Kunjimas Ketsuwan, Jukrapun Komaikul, Promsin Masrinoul, Tharita Kitisripanya, Thaweesak Juengwatanatrakul, Gorawit Yusakul, Tripetch Kanchanapoom, and Waraporn Putalun
• [ASAP] Diaporisoindole B Reduces Lipid Accumulation in THP‑1 Macrophage Cells via MAPKs and PPARγ–LXRα Pathways and Promotes the Reverse Cholesterol Transport by Upregulating SR-B1 and LDLR in HepG2 Cells
  by Hongju Liu, Huiyi Xie, Changqun Li, Lingling Wang, Qiling Chen, Xin Ouyang, and Chong Yan
• [ASAP] <italic toggle="yes">Seco</italic> B‑Type Oligomers from <italic toggle="yes">Pinus massoniana</italic> Expand the Procyanidin Chemical Space and Exhibit Dental Bioactivity
  by Bin Zhou, Yvette Alania, Mariana Reis, Shu-Xi Jing, James B. McAlpine, Ana K. Bedran-Russo, Shao-Nong Chen, Daneel Ferreira, and Guido F. Pauli