Science Feeds

Journal of Medicinal Chemistry

• [ASAP] Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells
  by Giuseppe Faudone, Iris Bischoff-Kont, Lea Rachor, Sabine Willems, Rezart Zhubi, Astrid Kaiser, Apirat Chaikuad, Stefan Knapp, Robert Fürst, Jan Heering, and Daniel Merk
• [ASAP] Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[<italic toggle="yes">c</italic>][1,2,5]oxadiazole Derivatives as Potent PD-L1 Inhibitors with <italic toggle="yes">In Vivo</italic> Antitumor Activity
  by Liu Liu, Zhiying Yao, Shijun Wang, Tao Xie, Guoqing Wu, Honghan Zhang, Pu Zhang, Yaojun Wu, Haoliang Yuan, and Hongbin Sun
• [ASAP] Potent and Subtype-Selective Dopamine D₂ Receptor Biased Partial Agonists Discovered via an Ugi-Based Approach
  by Ana Mallo-Abreu, Irene Reyes-Resina, Jhonny Azuaje, Rafael Franco, Aitor García-Rey, Maria Majellaro, Darío Miranda-Pastoriza, Xerardo García-Mera, Willem Jespers, Hugo Gutiérrez-de-Terán, Gemma Navarro, and Eddy Sotelo
• [ASAP] Abolishing Dopamine D_2long/D₃ Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H₂ Receptor Agonists
  by Katharina Tropmann, Merlin Bresinsky, Lisa Forster, Denise Mönnich, Armin Buschauer, Hans-Joachim Wittmann, Harald Hübner, Peter Gmeiner, Steffen Pockes, and Andrea Strasser
• [ASAP] Mechanism-Based Insights into Removing the Mutagenicity of Aromatic Amines by Small Structural Alterations
  by Igor Shamovsky, Lena Ripa, Frank Narjes, Britta Bonn, Stefan Schiesser, Ina Terstiege, and Christian Tyrchan
• [ASAP] Novel Bisubstrate Inhibitors for Protein N-Terminal Acetyltransferase D
  by Youchao Deng, Sunbin Deng, Yi-Hsun Ho, Sarah M. Gardner, Zhi Huang, Ronen Marmorstein, and Rong Huang
• [ASAP] Total Synthesis and Antimalarial Activity of 2-(<italic toggle="yes">p</italic>-Hydroxybenzyl)-prodigiosins, Isoheptylprodigiosin, and Geometric Isomers of Tambjamine MYP1 Isolated from Marine Bacteria
  by Papireddy Kancharla, Yuexin Li, Monish Yeluguri, Rozalia A. Dodean, Kevin A. Reynolds, and Jane X. Kelly
• [ASAP] Application of Alanine Scanning to Determination of Amino Acids Essential for Peptide Adsorption at the Solid/Solution Interface and Binding to the Receptor: Surface-Enhanced Raman/Infrared Spectroscopy versus Bioactivity Assays
  by Edyta Proniewicz, Grzegorz Burnat, Helena Domin, Izabela Mauch, Marta Makowska, and Adam Prahl
• [ASAP] Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer
  by Kevin D. Freeman-Cook, Robert L. Hoffman, Douglas C. Behenna, Britton Boras, Jordan Carelli, Wade Diehl, Rose Ann Ferre, You-Ai He, Andrea Hui, Buwen Huang, Nanni Huser, Rhys Jones, Susan E. Kephart, John Lapek, Michele McTigue, Nichol Miller, Brion W. Murray, Asako Nagata, Lisa Nguyen, Sherry Niessen, Sacha Ninkovic, Inish O’Doherty, Martha A. Ornelas, James Solowiej, Scott C. Sutton, Khanh Tran, Elaine Tseng, Ravi Visswanathan, Meirong Xu, Luke Zehnder, Qin Zhang, Cathy Zhang, and Stephen Dann
• [ASAP] X-ray Structure-Guided Discovery of a Potent, Orally Bioavailable, Dual Human Indoleamine/Tryptophan 2,3-Dioxygenase (hIDO/hTDO) Inhibitor That Shows Activity in a Mouse Model of Parkinson’s Disease
  by Xiang-Li Ning, Yu-Zhi Li, Cui Huo, Ji Deng, Cheng Gao, Kai-Rong Zhu, Miao Wang, Yu-Xiang Wu, Jun-Lin Yu, Ya-Li Ren, Zong-Yuan Luo, Gen Li, Yang Chen, Si-Yao Wang, Cheng Peng, Ling-Ling Yang, Zhou-Yu Wang, Yong Wu, Shan Qian, and Guo-Bo Li

ACS Medicinal Chemistry Letters

• [ASAP] Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate
  by Olga Bobiļeva, Raitis Bobrovs, Iveta Kaņepe, Liene Patetko, Gints Kalniņš, Mihails Šišovs, Anna L. Bula, Solveiga Gri̅nberga, Ma̅rtiņš Borodušķis, Anna Ramata-Stunda, Nils Rostoks, Aigars Jirgensons, Kaspars Ta̅rs, and Kristaps Jaudzems
• [ASAP] Novel <italic toggle="yes">N</italic>-Heteroaryl Quinazolin-2-amine Derivatives as LRRK2 Inhibitors for Treating Parkinson’s Disease
  by Ram W. Sabnis
• [ASAP] Novel Pyridazines as Autotaxin Inhibitors for Treating Inflammatory Airway or Fibrotic Diseases
  by Ram W. Sabnis
• [ASAP] Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs
  by Giuseppe Ermondi, Diego Garcia Jimenez, Matteo Rossi Sebastiano, and Giulia Caron
• [ASAP] Artificial Intelligence Deconstructs Drug Targeting <italic toggle="yes">In Vivo</italic> by Leveraging a Transformer Platform
  by Ariel Fernández
• [ASAP] Discovery and Optimization of a Series of Benzofuran Selective ERAP1 Inhibitors: Biochemical and <italic toggle="yes">In Silico</italic> Studies
  by Safia Deddouche-Grass, Cyrielle Andouche, Felix Bärenz, Célia Halter, Arnaud Hohwald, Louison Lebrun, Nathalie Membré, Renaud Morales, Nicolas Muzet, Matthieu Poirot, Morgane Reynaud, Véronique Roujean, Fabienne Weber, André Zimmermann, Rama Heng, and Nicolas Basse
• [ASAP] Novel Substituted 3,4-Dihydroquinazoline Derivatives for Treating Hepatitis B Virus Infection
  by Ram W. Sabnis
• [ASAP] DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry
  by Bing Xia, G. Joseph Franklin, Xiaojie Lu, Katie L. Bedard, LaShadric C. Grady, Jennifer D. Summerfield, Eric X. Shi, Bryan W. King, Kenneth E. Lind, Cynthia Chiu, Eleanor Watts, Vera Bodmer, Xiaopeng Bai, and Lisa A. Marcaurelle
• [ASAP] Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell
  by Kyohei Hayashi, Shota Uehara, Shiho Yamamoto, Douglas R. Cary, Junichi Nishikawa, Taichi Ueda, Hiroki Ozasa, Kousuke Mihara, Norito Yoshimura, Taeko Kawai, Takashi Ono, Saki Yamamoto, Masataka Fumoto, and Hidenori Mikamiyama
• [ASAP] Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria
  by Jinyue Ding, Rajesh Gumpena, Marc-Olivier Boily, Alexandre Caron, Oliver Chong, Jennifer H. Cox, Valerie Dumais, Samuel Gaudreault, Aaron H. Graff, Andrew King, John Knight, Renata Oballa, Jayakumar Surendradoss, Tim Tang, Joyce Wu, W. Todd Lowther, and David A. Powell

Journal of Natural Products

• [ASAP] Correction to Antibacterial and NF-κB Inhibitory Lumazine Peptides, Aspochalasin, γ-Butyrolactone Derivatives, and Cyclic Peptides from a Hawaiian <italic toggle="yes">Aspergillus flavipes</italic>
  by Cong Wang, Xiaohua Wu, Helong Bai, KH Ahammad Uz Zaman, Shaobin Hou, Jennifer Saito, Supakit Wongwiwatthananukit, Hyung Sik Kim, and Shugeng Cao
• [ASAP] Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of <italic toggle="yes">Kaempferia elegans</italic>
  by Pornsuda Chawengrum, Jutatip Boonsombat, Chulabhorn Mahidol, Chatchakorn Eurtivong, Prasat Kittakoop, Sanit Thongnest, and Somsak Ruchirawat
• [ASAP] ¹H HR-MAS NMR-Based Metabolomic Fingerprinting to Distinguish Morphological Similarities and Metabolic Profiles of <italic toggle="yes">Maytenus ilicifolia</italic>, a Brazilian Medicinal Plant
  by Sher Ali, Katlin S. Rech, Gul Badshah, Frederico L. F. Soares, and Andersson Barison
• [ASAP] Taccalonolide C-6 Analogues, Including Paclitaxel Hybrids, Demonstrate Improved Microtubule Polymerizing Activities
  by April L. Risinger, Shayne D. Hastings, and Lin Du
• [ASAP] Eriodictyol-Amplified 67-kDa Laminin Receptor Signaling Potentiates the Antiallergic Effect of <italic toggle="yes">O</italic>-Methylated Catechin
  by Yoshinori Fujimura, Konatsu Fujino, Takanori Yoshimoto, Ayaka Nezu, Yuki Marugame, Jaehoon Bae, Motofumi Kumazoe, and Hirofumi Tachibana
• [ASAP] Inhibition of BACE1 and Amyloid-β Aggregation by Meroterpenoids from the Mushroom <italic toggle="yes">Albatrellus yasudae</italic>
  by Youki Masuda, Koji Fujihara, Satoshi Hayashi, Hiroaki Sasaki, Yoshihiro Kino, Hitoshi Kamauchi, Masahiro Noji, Jun-ichi Satoh, Toshikatsu Takanami, Kaoru Kinoshita, and Kiyotaka Koyama
• [ASAP] Antibacterial and Cytotoxic Phenyltetracenoid Polyketides from <italic toggle="yes">Streptomyces morookaense</italic>
  by Xiaoxia Li, Ping Wu, Hanxiang Li, Jinghua Xue, Hanhong Xu, and Xiaoyi Wei
• [ASAP] Homophymamide A, Heterodetic Cyclic Tetrapeptide from a <italic toggle="yes">Homophymia</italic> sp. Marine Sponge: A Cautionary Note on Configurational Assignment of Peptides That Contain a Ureido Linkage
  by Daichi Kanki, Shohei Nakamukai, Yusuke Ogura, Hirosato Takikawa, Yuji Ise, Yasuhiro Morii, Nobuhiro Yamawaki, Tomohiro Takatani, Osamu Arakawa, Shigeru Okada, and Shigeki Matsunaga
• [ASAP] Generation and Biological Evaluation of Degraded Derivatives of the Three <italic toggle="yes">E</italic>/<italic toggle="yes">Z</italic>-Isomers of Yaku’amide B
  by Koichi Kamiya, Hiroaki Itoh, and Masayuki Inoue
• [ASAP] Mechanistic Insights into the Leishmanicidal and Bactericidal Activities of Batroxicidin, a Cathelicidin-Related Peptide from a South American Viper (<italic toggle="yes">Bothrops atrox</italic>)
  by Anderson Dematei, João B. Nunes, Daniel C. Moreira, Jéssica A. Jesus, Márcia D. Laurenti, Ana C. A. Mengarda, Maria Silva Vieira□■, Constança Pais do Amaral△, Marco M. Domingues△, Josué de Moraes, Luiz F. D. Passero, Guilherme Brand, Lucinda J. Bessa, Reinhard Wimmer▽, Selma A. S. Kuckelhaus, Ana M. Tomás□■▼, Nuno C. Santos△, Alexandra Plácido, Peter Eaton⬡, and José Roberto S. A. Leite