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Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-18 Hong Jia, Wei Deng, Baoyu Hao, Min Cai, Dong Guo, Yu Cai, Xiaoming Dai, Zhipeng Wu, Weigang He, Jian Wang, Guanglin Wang, Sumei Xia, Na Li, Weiguo Su, Guangxiu Dai
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Discovery of Novel Binders to Sterol Regulatory Element-Binding Protein-1 by High-Throughput Screening ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-17 Takashi Maruyama, Yu Takahashi, Kahori Hiro, Kohji Murase, Hirotatsu Kojima, Takayoshi Okabe, Yoshio Yamauchi, Ryuichiro Sato
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Synthesis of Monofluorinated 7-Hydroxycoumarin-3-Carboxamides as Cell-Permeable Fluorescent Molecular Probes ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-15 Digamber Rane, Anver Basha Shaik, Szu Lee, Xiaojun Hu, Blake R. Peterson
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Structural Evaluations of a Selective Human STINGA230 Agonist and Its Use in Macrophage Immunotherapies ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-12 Zhichao Tang, Junxing Zhao, Ying Li, Shallu Tomer, Manikandan Selvaraju, Nicholas Tien, Diyun Sun, David K. Johnson, Anjie Zhen, Pingwei Li, Jingxin Wang
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Novel Myeloperoxidase Inhibitors for Treating Multiple Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-11 Ram W. Sabnis
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In This Issue, Volume 15, Issue 4 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-11 Andrew P. Riley
This article has not yet been cited by other publications.
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Efficient Radiolabeling of Proteins and Antibodies via Maleamate–Cysteine Bioconjugation ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-10 Sajid Mushtaq, Kyo Chul Lee, Ji Ae Park, Jung Young Kim
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Novel CD73 Inhibitors for Treating Cancer ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-09 Ram W. Sabnis
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Discovery of Disubstituted Carboranes as Inhibitors of Heat Shock Protein 90–Heat Shock Factor 1 Interaction ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-08 Yujie Shao, Kazuki Miura, Yasunobu Asawa, Taiki Morita, Guangzhe Li, Hiroyuki Nakamura
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Structural Investigations of Phthalazinone Derivatives as Allosteric Inhibitors of Human DNA Methyltransferase 3A ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-08 Ivan Hernandez, Ethan Ward, Thomas R. R. Pettus, Norbert O. Reich
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Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-05 Nils Pemberton, Nina Compagne, Argyrides Argyrou, Emma Evertsson, Anders Gunnarsson, Jason G. Kettle, Jonathan P. Orme, Richard A. Ward
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Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-05 Roland W. Bürli, Kevin J. Doyle, Louise Dickson, Anna Rowland, Kim Matthews, Andrew J. Stott, Martin Teall, Bernardino Ossola, Samuel G. Russell, Jenna R. M. Harvey, Yiming Wu, Lakshminarayana Narayana, Nicola L. Brice, Mark Carlton, Lee A. Dawson
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Fitting of kinact and KI Values from Endpoint Pre-incubation IC50 Data ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-04 Lavleen K. Mader, Jeffrey W. Keillor
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Intracellular Pharmacokinetics of Activated Drugs in a Prodrug–Enzyme–Ultrasound System: Evaluations on ZD2767P+CPG2+US ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-04 Tinghe Yu, Xinya Li, Tianran Yu, Mengjie Chen, Yong Sun, Rui Ran
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A Potent Solution for Tumor Growth and Angiogenesis Suppression via an ELR+CXCL-CXCR1/2 Pathway Inhibitor ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-03 Oleksandr Grytsai, Maeva Dufies, Julie Le Du, Olivia Rastoin, Leticia Christina Pires Gonçalves, Lou Mateo, Sandra Lacas-Gervais, Yihai Cao, Luc Demange, Gilles Pagès, Rachid Benhida, Cyril Ronco
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Synthesis and Monoamine Oxidase Inhibitory Activity of Halogenated Flavones ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-03 Jorge I. Castillo-Arellano, Zachary Stryker, Michael D. Wyatt, Francisco León
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Discovery of Novel Bicyclic Pyrazoles as Potent PIP5K1C Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-03 Koji Ochiai, Shigeki Seto, Masanobu Yajima, Ryosuke Namie, Noriaki Hashimoto, Motomichi Fujita, Akinobu Yokoyama, Takahiro Suezawa, Hitomi Matsui, Satoshi Tomizawa, Yuji Ishibashi, Yuta Tanaka, Miho Yajima, Michiaki Nagasawa, Naoki Ando
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Novel Isoxazolidines as RIPK1 Inhibitors for Treating Alzheimer’s Disease, Multiple Sclerosis, and Amyotrophic Lateral Sclerosis ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-04-02 Ram W. Sabnis
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Imidazole Bioisostere Activators of Endopeptidase Neurolysin with Enhanced Potency and Metabolic Stability ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-29 Md. Shafikur Rahman, Shiva Hadi Esfahani, Yong Zhang, Aarfa Queen, Manar Aljarrah, Haya Kandil, Andrew Baez, Thomas J. Abbruscato, Vardan T. Karamyan, Paul C. Trippier
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Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-28 Matthew Allison, Rebecca L. Davie, Adrian J. Mogg, Sally L. Hampton, Jonas Emsley, Michael J. Stocks
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Macrocyclic Oxindole Peptide Epoxyketones─A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-27 Marion G. Götz, Kacey Godwin, Rachel Price, Robert Dorn, Gabriel Merrill-Steskal, William Klemmer, Hunter Hansen, Gautam Produturi, Megan Rocha, Mathias Palmer, Lea Molacek, Zack Strater, Michael Groll
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How Shilajit-Based Nanocarriers Alter Classical Doxorubicin Delivery to Breast Cancer Cells (MCF-7 and ZR-75-1) ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-27 Zahra Asadi, Saba Jalilian, Elham Arkan, Faranak Aghaz
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Novel ACC Inhibitors for Treating Acne ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-27 Ram W. Sabnis
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The Science and Art of Structure-Based Virtual Screening ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-25 Hongtao Zhao
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Discovery of Hepatitis B Virus Surface Antigen Suppressor GS-8873 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-22 Darryl Kato, Regina Wai-Yan Choy, Eda Canales, Ryan A. Dick, April D. Lake, Nathan D. Shapiro, Elbert Chin, Jiayao Li, Jennifer R. Zhang, Qiaoyin Wu, Roland D. Saito, Sammy Metobo, Evangelos Aktoudianakis, Scott D. Schroeder, Zheng-Yu Yang, Dylan M. Glatt, Scott Balsitis, Lindsay Gamelin, Mei Yu, Guofeng Cheng, William E. Delaney, IV, John O. Link
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In Retrospect: Root-Cause Analysis of Structure–Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833) ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-21 Stephen W. Wright, Kathleen A. Farley, Seungil Han, John D. Knafels, Katherine L. Lee
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59 Years of MIKIW─A Historical Perspective Brought Up-to-Date and an Invitation to Collaborate ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-21 Douglas Armstrong
Published as part of ACS Medicinal Chemistry Letters virtual special issue “Celebrating the 60th Anniversary of the MIKIW Meeting-in-Miniature”. My first MIKI Meeting was in 1964. I just barely missed the very first MIKI Meeting in 1963, which was held several months before I started graduate school studying medicinal chemistry in the College of Pharmacy at the University of Iowa under the mentorship
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Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-19 Sun Hee Kim, Sangdon Han, Jian Zhao, Shimiao Wang, Ana Karin Kusnetzow, Greg Reinhart, Melissa A. Fowler, Stacy Markison, Michael Johns, Rosa Luo, R. Scott Struthers, Yunfei Zhu, Stephen F. Betz
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Balanced Permeability Index: A Multiparameter Index for Improved In Vitro Permeability ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-19 Dahlia R. Weiss, Javier L. Baylon, Ethan D. Evans, Anthony Paiva, Gerry Everlof, Jingfang Cutrone, Fabio Broccatelli
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hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-17 Dickson Mambwe, Dina Coertzen, Meta Leshabane, Mwila Mulubwa, Mathew Njoroge, Liezl Gibhard, Gareth Girling, Kathryn J. Wicht, Marcus C. S. Lee, Sergio Wittlin, Diogo Rodrigo Magalhães Moreira, Lyn-Marie Birkholtz, Kelly Chibale
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Design, Synthesis, and Evaluation of 8-(o-Tolyl)quinazoline Derivatives as Small-Molecule PD-1/PD-L1 Antagonists ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-15 Xingye Wu, He Li, Han Liu, Xueyan Ding, Xinting Chen, Chenxi Yin, Yali Gao, Junjie Ma
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Chemical Space Profiling of SARS-CoV-2 PLpro Using DNA-Encoded Focused Libraries ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-14 Xudong Wang, Ying Zhu, Qingyi Zhao, Weiwei Lu, Yechun Xu, Hangchen Hu, Xiaojie Lu
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Discovery of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides as Human Carbonic Anhydrase Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-13 Davide Moi, Serena Vittorio, Andrea Angeli, Claudiu T. Supuran, Valentina Onnis
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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-12 Mayako Michino, Tanweer A. Khan, Michael W. Miller, Yoshiyuki Fukase, Jeremie Vendome, Carolina Adura, J. Fraser Glickman, Yiman Liu, Liling Wan, C. David Allis, Andrew W. Stamford, Peter T. Meinke, Louis M. Renzetti, Stacia Kargman, Nigel J. Liverton, David J. Huggins
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Exploring Scaffold Hopping for Novel 2-(Quinolin-4-yloxy)acetamides with Enhanced Antimycobacterial Activity ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-11 Ana Flávia Borsoi, Alessandro Silva Ramos, Nathalia Sperotto, Bruno Lopes Abbadi, Fernanda Souza Macchi Hopf, Adilio da Silva Dadda, Raoní Scheibler Rambo, Mauro Neves Muniz, Josiane Delgado Paz, Estevão Silveira Grams, Fernanda Fries da Silva, Kenia Pissinate, Luiza Galina, Laura Calle González, Lovaine Silva Duarte, Marcia Alberton Perelló, Alexia de Matos Czeczot, Cristiano Valim Bizarro, Luiz Augusto
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Novel Phosphorylpurinone Compounds for Treating Cancer ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Ram W. Sabnis
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Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Ram W. Sabnis
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Empowering Voices: Inspiring Women in Medicinal Chemistry ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Maria-Jesus Blanco, Joanne J. Bronson, Erin F. DiMauro, Carolyn Dzierba, MariJean Eggen, Amanda L. Garner, Gunda Georg, Jeanine Giarolla, Nicole C. Goodwin, Melissa C. Grenier-Davies, Carrie Haskell-Luevano, Ulrike Holzgrabe, Rong Huang, H. Rachel Lagiakos, Katerina Leftheris, Yvonne Martin, Maria João Matos, Tricia L. May-Dracka, Christa E. Müller, Amy H. Newman, Emma Parmee, Jennifer C. Petter, Nuria
As we celebrate International Women’s Day 2024 with the theme “Inspire Inclusion”, the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and
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Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-07 Stefan McCarver, Luke Hanna, Andrew Samant, Aaron A. Thompson, Mark Seierstad, Arjun Saha, Dongpei Wu, Brian Lord, Steven W. Sutton, Vishal Shah, Cynthia M. Milligan, Michelle Wennerholm, Jonathan Shelton, Terry P. Lebold, Brock T. Shireman
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Identification of Dual Inhibitors Targeting Main Protease (Mpro) and Cathepsin L as Potential Anti-SARS-CoV-2 Agents ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-01 Santo Previti, Roberta Ettari, Elsa Calcaterra, Michele Roggia, Benito Natale, Annabelle C. Weldert, Christin Müller-Ruttloff, Florian Salisch, Anna Irto, Rosalia Maria Cigala, John Ziebuhr, Tanja Schirmeister, Sandro Cosconati, Maria Zappalà
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Novel-Type GABAB PAMs: Structure–Activity Relationship in Light of the Protein Structure ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-01 Balázs Krámos, Zsuzsa Hadady, Attila Makó, Gábor Szántó, Nóra Felföldi, Ildikó Magdó, Amrita Ágnes Bobok, Imre Bata, Viktor Román, András Visegrády, György M. Keserű, István Greiner, János Éles
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Combination of Allosteric and Orthosteric EGFR Inhibitors for Treating Non-Small-Cell Lung Cancer ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 Ram W. Sabnis
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Tips for Getting Your Manuscript Accepted into ACS Medicinal Chemistry Letters ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 John G. Woodland, Kelly Chibale
Scientific publications are the culmination of the scientific enterprise, providing the foundation for new hypotheses and technologies. A good paper, written for and by researchers, clearly and convincingly presents the findings of a carefully conducted study to the larger scientific community. Scientific publications also yield indirect rewards; for example, they may advance a researcher’s career
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Novel Heterocyclic PAD4 Inhibitors for Treating Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 Ram W. Sabnis
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Forging a Future Free from Neglected Tropical Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-26 Flavio da Silva Emery, Kelly Chibale
World Neglected Tropical Diseases Day (“World NTD Day”), established by the World Health Organization and observed every January 30th, raises awareness and mobilizes action against neglected tropical diseases (NTDs), affecting over 1.6 billion people worldwide. (1,2) In recent years, we have witnessed advances in the development of tools to control, prevent, and eliminate at least one NTD in many countries
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Forgotten Natural Products: Semisynthetic Development of Blasticidin S As an Antibiotic Lead ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-23 Cole Gannett, Kateland Tiller, Anthony J. Briganti, Anne M. Brown, James Weger-Lucarelli, Andrew N. Lowell
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Design, Synthesis, and Antifungal Activity of 3-Substituted-2(5H)-Oxaboroles ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-22 Rose Campbell, Nicklas W. Buchbinder, Connor Szwetkowski, Yumeng Zhu, Karla Piedl, Mindy Truong, John B. Matson, Webster L. Santos, Emily Mevers
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64Cu-Labeled Boron-Containing Cyclic RGD Peptides for BNCT and PET Imaging ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-21 Soyeon Kim, Sajid Mushtaq, Kyo Chul Lee, Ji Ae Park, Jung Young Kim
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Probing the Use of Triphenyl Phosphonium Cation for Mitochondrial Nucleoside Delivery ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-15 Mathis Guiraud, Lamiaa M. A. Ali, Emma Gabrieli-Magot, Laure Lichon, Morgane Daurat, David Egron, Magali Gary-Bobo, Suzanne Peyrottes
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ZX703: A Small-Molecule Degrader of GPX4 Inducing Ferroptosis in Human Cancer Cells ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-15 Mengdie Hu, Xiaomei Li, Lin Wang, Yanping Zhang, Yujie Sun, Hui Hua, Huina Liu, Ting Cai, Dongsheng Zhu, Qiuping Xiang
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Pyrrolidinone Derivatives as NIK Inhibitors for Treating Inflammatory and Autoimmune Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-14 Ram W. Sabnis
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Suppressive Effects of Neuromedin U Receptor 2-Selective Peptide Agonists on Appetite and Prolactin Secretion in Mice ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-14 Asuka Nomoto, Yui Suzuki, Katsuya Morito, Kazuki Nagasawa, Kentaro Takayama
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Innovations in Pharmacology: Enhancing Bioavailability and Efficacy through Novel Compositions ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Pioneering Methods in Brain Optimization and Mental Health Treatment ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Novel Heterocyclic Compounds for Treating Huntington’s Disease ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Ram W. Sabnis, Anika R. Sabnis
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Novel AT2R Antagonists for Treating Chronic Pain ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Ram W. Sabnis
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AI in Pharma: Transforming Drug Discovery and Strategic Management with MYC-Modulating Compounds and BET Protein Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Advancements in Predictive Medicine: NLRP3 Inflammasome Inhibitors and AI-Driven Predictive Health Analytics ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-12 Robert B. Kargbo
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Selective Recognition of c-KIT 1 G-Quadruplex by Structural Tuning of Heteroaromatic Scaffolds and Side Chains ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-12 Khushnood Fatma, Prasanth Thumpati, Deepanjan Panda, Ravichandiran Velayutham, Jyotirmayee Dash
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Synthesis and Biophysical Characterization of Fingolimod Derivatives as Cardiac Troponin Antagonists ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-07 Laszlo Kondacs, Priyanka Parijat, Alexander J. A. Cobb, Thomas Kampourakis