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Characterization of Hepatotropic Small Molecule Inhibitors of Hypoxia Inducible Factor Prolyl Hydroxylase in the Prevention of Oxygen-Induced Retinopathy J. Med. Chem. (IF 6.8) Pub Date : 2025-06-04
Christie Campla, George Hoppe, Minzhong Yu, Juliana Woda, Neal S. Peachey, Vara Prasad Josyula, Shaun R. Stauffer, Jonathan E. SearsRetinopathy of prematurity (ROP) blinds severely premature infants and is caused by oxygen supplementation. Hypoxia-inducible factor (HIF) stabilization during hyperoxia can prevent oxygen-induced retinopathy (OIR), the experimental correlate of ROP. Stabilization of hepatic HIF-1 alone can prevent OIR while contemporaneously protecting other organ systems, such as the lung and brain, from oxygen toxicity
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Target Engagement Assays in Early Drug Discovery J. Med. Chem. (IF 6.8) Pub Date : 2025-06-04
Sahra St John-Campbell, Gurdip Bhalay -
Design, Synthesis, and Evaluation of Pyrazolopyridine Derivatives as Novel Calreticulin (CALR) Ligands That Inhibit Triple-Negative Breast Cancer (TNBC) via Inducing Calcium Overloading J. Med. Chem. (IF 6.8) Pub Date : 2025-06-04
Jiaguo Lu, Anqi Yin, Shenpeng Tan, Ruihong Zhuge, Yi Liu, Peng Zhang, Li Liu, Xuan Xuan, Huirong Li, Wenyan Wang, Xiaolin Zhang, Qikun Yin, Hongbo WangTriple-negative breast cancer (TNBC) is the most aggressive subtype of breast cancer, posing significant therapeutic challenges due to the lack of effective targets. Elevating intracellular calcium levels is a promising strategy in cancer therapy, and highly expressed calreticulin (CALR) in tumors has emerged as a potential target for inducing calcium overload. However, few studies on CALR ligands
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Uncovering the Unusual Inhibition Mechanism of a Trypanosome Alternative Oxidase Inhibitor Displaying Broad-Spectrum Activity against African Animal Trypanosomes J. Med. Chem. (IF 6.8) Pub Date : 2025-06-04
Godwin U. Ebiloma, Emmanuel O. Balogun, Natsumi Arai, Momoka Otani, Cecilia Baldassarri, Amani Alhejely, Eduardo Cueto-Díaz, Harry P. De Koning, Christophe Dardonville, Tomoo Shiba -
Cyclic Peptide Therapeutic Agents Discovery: Computational and Artificial Intelligence-Driven Strategies J. Med. Chem. (IF 6.8) Pub Date : 2025-06-04
Kang Lin, Chengyun Zhang, Renren Bai, Hongliang Duan -
Heparan Sulfate-Based Neoproteoglycan for Targeted Lysosomal Degradation of Amyloid-β J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Sharath S. Vishweshwara, Saurabh Anand, Preeti Ravindra Bhoge, Virendrasinh Mahida, Ankita Chandra, Srinivas Vinod Saladi, Raghavendra Kikkeri -
Design, Synthesis, and Biological Activity Evaluation of Deuterated Diphenyl Azole Alcohol-Based CYP51 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Yixiang Sun, Zirui Luo, Kejian Li, Hongjian Wang, Zixuan Gao, Jiachen Zhang, Rongrong Liu, Rui Liu, Xudong Wu, Nian Liu, Haoyu Zhang, Xin Su, Wenbo Yin, Dongmei Zhao, Maosheng Cheng -
Discovery of a Novel and Potent MET Transcription Inhibitor Targeting Promoter G-Quadruplex for the Treatment of NSCLC J. Med. Chem. (IF 6.8) Pub Date : 2025-06-02
Wenjian Min, Chunling Chen, Zhongrui Shi, Huanaoyu Yang, Yanyin Wang, Junfeng He, Qiman Zhang, Yunchu Zhao, Yi Hou, Jiayu Ding, Yasheng Zhu, Chengliang Sun, Kai Yuan, Peng Yang, Xiao Wang -
Opioid Enantiomers: Exploring the Complex Interplay of Stereochemistry, Pharmacodynamics, and Therapeutic Potential J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Jingwei Gao, Dingjun Jiang, Hongshuang Wang, Xiaohui Wang -
Dual Conjugation of Long- and Medium-Chain Fatty Acids to BimBH3 Peptide Yields Ultra Long-Acting Inhibitors of Intracellular PTPN1/2 J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Chuanliang Zhang, Guozhen Dong, Xiao Wu, Jin Chen, Yanqing Wang, Liyan Gong, Xianmin Yang, Yiying Shi, Zongwen Gu, Xiang Gao, Yaning Zheng, Han Wu, Ke Zheng, Xiaochun Liu, Yuchao Gu -
Discovery of KIN-8741, a Highly Selective Type IIb c-Met Kinase Inhibitor with Broad Mutation Coverage and Quality Drug-Like Properties for the Treatment of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Xiaohu S. Ouyang, Kathryn B. Grandinetti, Morgan Boren, Subhas Chakravorty, Shubham Chopade, Ping Jiang, Toufike Kanouni, Tatiana Koudriakova, Om Makwana, Shawn K. Pack, Michelle Perez, Rowena Suriben, Noel Timple, Sanjeev Thohan, Sean Uryu, Scott Womble, Ding Yuan, Robert S. Kania, Jason M. Cox -
Unraveling the Efficacy of AR Antagonists Bearing N-(4-(Benzyloxy)phenyl)piperidine-1-sulfonamide Scaffold in Prostate Cancer Therapy by Targeting LBP Mutations J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Xin Chai, Xinyue Wang, Lvtao Cai, Haiyi Chen, Siyu Wang, Jianing Liao, Huating Wang, Yuxin Zhou, Lei Xu, Luhu Shan, Xiaohong Xu, Yuhui Yang, Junzhao He, Yaqin Fu, Tingjun Hou, Rong Sheng, Dan Li -
Discovery of a Proteolysis-Targeting Chimera Degrader of JAK2 as a Potential Therapeutic Agent for JAK2-Mediated Myeloproliferative Neoplasms J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Caolin Wang, Ziqi Chen, Siyu Wang, Jie Wang, Panpan Yu, Chulu Huang, Yunpeng Wu, Zhenjiang Zhao, Wenyi Mei, Honglin Li, Lili Zhu -
Induction of Cuproptosis with a Highly Cytotoxic Tripodal Cu(II) Complex for Anticancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2025-06-03
Ricarda Zimmermann, Nicolás Montesdeoca, Johannes Karges -
Corrections to “VHH Nanobody Versatility against Pentameric Ligand-Gated Ion Channels” J. Med. Chem. (IF 6.8) Pub Date : 2025-06-02
Dorota Nemecz, Weronika Nowak, Ákos NemeczPage 8502 Section 2: Typographical errors not caught during copy edits should be corrected as such: a comma after “peripheral,” in the second sentence of the first paragraph. An o is missing from “Drosophila melanogaster” in the second to last sentence. Page 8507 Section 4.1: Last paragraph a comma should be removed after NbR101 in the sentence “These interactions consist of NbR101 making a salt bridge
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Optimization of 1-Methyl-3-(pyridin-3-yl)-1H-indol Derivatives as ROR1 Inhibitors with Improved Activity and Selectivity J. Med. Chem. (IF 6.8) Pub Date : 2025-06-02
Qingquan Zheng, Xingyang Qiu, Dongdong Luo, Hulin Ma, Yue Ming, Wenchen Pu, Min Ai, Jianhua He, Yong Peng -
Lead Optimization of a Butyrylcholinesterase Inhibitor for the Treatment of Alzheimer’s Disease J. Med. Chem. (IF 6.8) Pub Date : 2025-06-02
Urban Košak, Nika Strašek Benedik, Damijan Knez, Simon Žakelj, Jurij Trontelj, Anja Pišlar, Selena Horvat, Aljoša Bolje, Neža Žnidaršič, Neža Grgurevič, Tanja Švara, Jakob Kljun, Anna Skrzypczak-Wiercioch, Bingbing Lv, Yucheng Xiong, Qinjie Wang, Rui Bian, Jikuan Shao, José Dias, Florian Nachon, Xavier Brazzolotto, Jure Stojan, Haopeng Sun, Kinga Sałat, Stanislav Gobec -
Recognition of the CREB-Binding Protein/Mixed Lineage Leukemia Interface by Sulfonyl-γ-AApeptides: Beyond Mimicry of Mixed Lineage Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2025-06-02
Bo Huang, Minghui Wang, Emily Gregory-Lott, Bingbing X. Li, Yu Yu Win, Ning Shen, Jianyu Chen, Sihao Li, Chuanhai Cao, Xiangshu Xiao, Gary W. Daughdrill, Jianfeng Cai -
Metalla-Aromatic Oligomers: Efficient Photocatalytic Activation for Phototherapy J. Med. Chem. (IF 6.8) Pub Date : 2025-06-01
Shiyan Chen, Guotao Yuan, Liu Wang, Jungryun Kim, Haobing Wang, Jiyoung Yoo, Fengshu Cao, Xintong Lin, Huaiyi Huang, Jong Seung Kim, Haiping Xia, Pingyu Zhang -
Optimization of Tambjamines Active against Multiple Stages of Malaria Parasites J. Med. Chem. (IF 6.8) Pub Date : 2025-06-01
Amrendra Kumar, Yuexin Li, Xiaowei Zhang, Xiannu Jin, William E. Dennis, Ravi Chetree, Cameron Blount, Diana Caridha, Michael S. Madejczyk, Patricia J. Lee, Kristina Pannone, Jesse DeLuca, Chau Vuong, Susan Leed, Hieu T. Dinh, Kennedy Mdaki, Rohit Mahato, Priyam Sen, Trisha Mondal, Karabi Phukan, Ankur Saha, Anongruk Chim-Ong, Liwang Cui, Rajachandrasekhar Valmon, Sivanna Chithanna, Rozalia A. Dodean -
Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis J. Med. Chem. (IF 6.8) Pub Date : 2025-05-31
Siyi Zhang, Zhen Li, Bo Li, Zhiyi Li, Huiqian Peng, Lixian Shen, Lejing Zhu, Tong Mo, Jialiang Peng, Linsheng Zhuo, Zhen Wang, Weifan Jiang -
Lysine-Targeted Covalent Strategy Leading to the Discovery of Novel Potent PROTAC-Based PI3Kδ Degraders J. Med. Chem. (IF 6.8) Pub Date : 2025-05-31
Bo Yuan, Jiaxin Liu, Yujie Wu, Mengyao Chen, Ying Lai, Hong-Yi Zhao, Zhe Yang, San-Qi Zhang, Minhang Xin -
Discovery of Novel Potent Molecule for Treating Cisplatin-Induced Acute Kidney Injury Driven by Phenotypic Screening J. Med. Chem. (IF 6.8) Pub Date : 2025-05-31
Yan Lou, Feilong Zhou, Daxing Shi, Yu Zhang, Jin Dong, Xiaobao Shen, Xing Chen, Xinhua Liu -
Harder than Metal: Challenging Antimicrobial Resistance with Metallo-β-lactamase Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-05-30
Antonietta De Falco, Antonella Ilenia Alfano, Luigi Cutarella, Mattia Mori, Margherita Brindisi -
Developing Potent and Selective Anticancer Therapy through Chemical Approaches and the Combination of Cationic Amphipathic Oncolytic Peptides J. Med. Chem. (IF 6.8) Pub Date : 2025-05-30
Hai Bui Thi Phuong, Bao Loc Nguyen, Linyu Huang, Thi Oanh Oanh Nguyen, Ngoc Duy Le, Beomsu Kim, Basavaraj Rudragouda Patil, Thang Nguyen Quoc, Jeonghwan Kim, Huy Xuan Luong, and Jong Oh Kim -
Rational Design of Novel Quinazolinone–Pyrrolodihydropyrrolone Analogs as PIM/HDAC Dual-Target Inhibitors for the Treatment of Acute Myelocytic Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2025-05-30
Yabing Xin, Can Xiao, Nan Wang, Huidan Wu, Wenjing Kang, Xuetao Chen, Chihong Liu, Qidong You, Zhengyu Jiang, Xiaoke Guo -
Design of an Oral STING Agonist through Intramolecular Hydrogen Bond Ring Mimicking to Achieve Complete Tumor Regression J. Med. Chem. (IF 6.8) Pub Date : 2025-05-29
Hong-Yi Zhao, Jinsong Tao, Luchen Zhang, Qiuxia Li, Miao He, Bo Wen, Zhongwei Liu, Hannah Myatt, Duxin Sun -
Structural Optimization of Next-Generation TRK Inhibitors against Acquired Drug Resistance Mutations for the Treatment of Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2025-05-29
Zichao Xu, Yueling Liu, Peng Wang, Xia Peng, Jiawei Cheng, Yinchun Ji, Xutong Li, Dongze Lin, Jing Zhao, Songbin Chen, Zhiyang Xu, Mingyue Zheng, Meiyu Geng, Hong Liu, Jing Ai, Chunpu Li -
Discovery of CYP1A1 Inhibitors for Host-Directed Therapy against Sepsis J. Med. Chem. (IF 6.8) Pub Date : 2025-05-29
Fangjie Wang, Sheng-Li Niu, Wei Li, Hong-Yuan Liu, Xue Gong, Xiaoyuan Ma, Bo Zhao, Dongmei He, Jinyu Xia, Liang Gong, Yiqin Cui, Rui Gao, Huaping Liang, Jing Gu, Qin Ouyang -
Correction to “A NIR-II Photoacoustic/NIR-IIa Fluorescent Probe for Targeted Imaging of Glioma under NIR-II Excitation” J. Med. Chem. (IF 6.8) Pub Date : 2025-05-29
Shuxin Lyu, Siyu Lu, Conghao Gui, Chunyan Guo, Juanjuan Han, Yuling Xiao, Ruiping Zhang, Xuechuan HongWe apologize for the error in the acknowledgments section. The funding number for the National Key R&D Program of China was incorrectly listed as Nos. 2023YFC3605502 and 2020YFA0908800. The correct grant number is No. 2023YFC3605500. This article has not yet been cited by other publications.
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Design of Paromomycin and Neomycin as Sulfated and Hydrophobic Glycans to Target Heparanase-Driven Tumor Progression and Metastasis J. Med. Chem. (IF 6.8) Pub Date : 2025-05-28
Hawau Abdulsalam, Livia Philip, Kartikey Singh, Malik Farhoud, Neta Ilan, Israel Vlodavsky, Hien M. Nguyen -
Intercepting the Downstream of the Estrogen Receptor Signaling Pathway: Discovery of a Potent and Efficient SRC-3 PROTAC Degrader for Overcoming Endocrine Resistance Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2025-05-28
Jinsen Liang, Dandan Wang, Yihe Wu, Jiahao Shi, Baohua Xie, Ruijing Xiao, Jian Ni, Chao Wang, Chune Dong, Hong-Bing Shu, Shu Li, Hai-Bing Zhou -
Plasma Protein Binding as an Optimizable Parameter for In Vivo Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2025-05-28
Hongtao Zhao -
The Discovery of C7-Substituted Norbornyl Bisamides as RXFP1 Small Molecule Agonists J. Med. Chem. (IF 6.8) Pub Date : 2025-05-28
Shun Su, Michael C. Myers, Donna M. Bilder, Adam Clarke, Todd Friends, Thomas V. Petrone, Carol Ryan, Carol M. Krause, Ruihua Chen, Yi-xin Li, Matthew Fronheiser, Michael A. Galella, Anne V. Rose, Claudia N. Generaux, Lei Zhao, Jeff Bostwick, Jianqing Li, Arvind Mathur, Franck Duclos, Cort S. Madsen, Ruth R. Wexler, R. Michael Lawrence -
Adaptor-Specific Peptide Inhibitors of the Ubiquitin-Chain-Dependent Unfolding Activity of the Human p97(VCP)–UFD1–NPL4 Complex J. Med. Chem. (IF 6.8) Pub Date : 2025-05-27
Kei Okatsu, Takaya Kawaguchi, Kohei Watanabe, Yoshinori Taguchi, Reon Takeuchi, Akinori Okamoto, Yasuyuki Iwasa, Takuya Tomita, Yasushi Saeki, Yusuke Sato, Tetsuo Narumi, Shuya Fukai -
Design and Mechanistic Analysis of a Potent Bivalent Inhibitor of Transthyretin Amyloid Fibrillogenesis J. Med. Chem. (IF 6.8) Pub Date : 2025-05-27
P. Patrizia Mangione, Guglielmo Verona, Cristina Cantarutti, Paola Nocerino, Maria Chiara Mimmi, Christopher J. Swain, Diana Canetti, Sofia Giorgetti, Iain Uings, Julian D. Gillmore, Graham W. Taylor, Mark B. Pepys, Vittorio Bellotti, Alessandra Corazza -
Design, Synthesis, and Biological Evaluation of New PDE4 Inhibitors for the Treatment of Pressure Ulcers J. Med. Chem. (IF 6.8) Pub Date : 2025-05-27
Xudong Qian, Gang Li, Yan Geng, Jiaxin Chen, Jiayu Li, Yanghui Ou, Jun Wang, Wei Pan, Dengqin He, Lang Xu, Yuanhui Liu, Yali Zhang, Mengjie Li, Dandan Chen, Ligui Chen, Wen-Hua Chen, Hongliang Yao -
Regio- and Stereoselective Synthesis of Nitro-fatty Acids as NRF2 Pathway Activators Working under Ambient or Hypoxic Conditions J. Med. Chem. (IF 6.8) Pub Date : 2025-05-26
Daniel Chrenko, Jana Pereckova, Martina Zatloukalová, Jan Vacek, Jiří Pospíšil, Tomas Perecko -
Rational Design and Synthesis of Highly Stable Haloflavanone DNA Methyltransferase Inhibitors Inducing Tumor Suppressor Gene Re-expression in Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2025-05-26
Francesco Calzaferri, Hiba Daher, Julie Gilbert, Yinshan Yang, Marine Tauziet, Corinne Jallet, Yannick Bessin, Arie van der Lee, Paola Barbara Arimondo, Isabelle Krimm, Eric Julien, Marie Lopez -
Peptidomimetic Phenoxymethyl Ketone Warheads as Potent Dual-Mode Inhibitors against SARS-CoV-2 Mpro and Cathepsin J. Med. Chem. (IF 6.8) Pub Date : 2025-05-26
Miriam R.B. Porzberg, G.J. Mirjam Groenewold, Heyrhyoung Lyoo, Alexander K.M.H. Jakob, Willem H.C. Titulaer, Lorenzo Cavina, Katrien C.K. Poelaert, Marleen Zwaagstra, Cindy E.J. Dieteren, Jaap G.H. Lemmers, S. Hakim Hamdani, Bernd N.M. van Buuren, Bart Ackerschott, Johannes Platteeuw, Joey Michorius, Byron E.E. Martina, Martin C. Feiters, Daniel Gironés, Frank J.M. van Kuppeveld, Martijn J. van Hemert -
The Logic of Chemical Optimization J. Med. Chem. (IF 6.8) Pub Date : 2025-05-26
David C. Kombo, Matthew J. LaMarche -
Grapefruit Extracellular-Vesicle-Derived Nanodrug Loading Three-Functional Platinum(IV) Conjugates with Enhanced Targeting and TME Modulating Properties J. Med. Chem. (IF 6.8) Pub Date : 2025-05-26
Yan Chen, Shuaiqi Feng, Lanjie Li, Guiqin Liu, Qingshan Ma, Zhifang Liu, Yanna Zhao, Qingpeng Wang -
Developing Dual-State Emission Berberine Derivatives as Theranostic Agents by Reducing Nonradiative Transition Pathways J. Med. Chem. (IF 6.8) Pub Date : 2025-05-25
Fuquan Xie, Beibei Xu, Peng Chen, Yushan Qin, Wenbin Pei, Jiangquan Li, Tianhui Hu, Qi Gao, Siying Chen, Yandong Zhang, Defa Li, Zhongjian Xie -
Intestinal Secretion Is a Potentially Important Clearance Mechanism for Low Metabolic Clearance Compounds J. Med. Chem. (IF 6.8) Pub Date : 2025-05-25
Murali Subramanian, Deepak Ahire, Rakshit Tanna, Zaikuan Josh Yu, Kelly Wang, Wei Wang, Gillian Smith, Xingrong Liu -
Discovery and Characterization of a First-in-Class LIV1-TLR7/8 Immunomodulatory Conjugate with Robust Myeloid Activation and Antitumor Activity J. Med. Chem. (IF 6.8) Pub Date : 2025-05-24
Sayumi Yamazoe, Yam Poudel, Emanuela Sega, Anandaroop Mukhopadhyay, Radha Ramakrishnan, Okechukwu Ukairo, Scot Liu, Rahima Akter, Keerthi Sadanala, Kathryn Que, Qinqin Cheng, Srikanth Kotapati, Madhura Deshpande, Matthew Cox, Shishir Chourey, Anuradha Gupta, James Kempson, Kumar Pabbisetty, Mahammed Kaspady, Debabrata Bhattasali, Shiuhang Yip, Dauh-Rurng Wu, Deepa Pookot, Yvonne Li, Alexander Kozhich -
Discovery of Orally Potent Small-Molecule CD73 Inhibitor for Cancer Immunotherapy J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Lifang Cen, Weijie Ren, Jiajie Yu, Ming Cheng, Xiangying Kong, Wenxin Yan, Luhua Wang, Xinyue Li, Jing Liu, Zhen Wang, Shiqi Wu, Xiaomeng Sun, Ping Wei, Hongfeng Gu, Qihua Zhu, Yi Zou, Yungen Xu -
Discovery and Characterization of Potent, Selective, and Orally Bioavailable 7-Azaindazole AXL Receptor Tyrosine Kinase Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Corinne N. Foley, Shiwei Qu, Srinivas Reddy Paladugu, Manjunath Lamani, Rebecca Grange, Ehesan U. Sharif, Joice Thomas, Pradeep Nareddy, Guiling Zhao, Yu Chen, Xiaoning Zhao, David Green, Hsin-Ting Huang, Lixia Jin, Susan L. Paprcka, Ester Fernandez-Salas, Jay P. Powers, Manmohan R. Leleti, Dillon H. Miles -
Discovery of AB801, a Potent and Selective Inhibitor of AXL Receptor Tyrosine Kinase for Use in Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Dillon H. Miles, Manjunath Lamani, Srinivas Reddy Paladugu, Shiwei Qu, Corinne N. Foley, Ehesan U. Sharif, Joice Thomas, Pradeep Nareddy, Joel W. Beatty, Balint Gal, Guiling Zhao, Rebecca Grange, Stefan G. Shaqfeh, Ada Chen, Hema Singh, Yue Tong Lee, Xiaoning Zhao, David Green, Hsin-Ting Huang, Elaine Ginn, Lixia Jin, Susan L. Paprcka, Ester Fernández-Salas, Lian Zhou, Jordon Johnson, Lilian Adeojo -
Molecular-Level Strategy from Bottom-Up to Acquire High-Efficiency Antimicrobial Peptides J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Chu Wang, Jingyao Guo, Jiaming Zhang, Chenxi Hou, Yunmo Xue, Xiaofeng Han, Yan Chen, Mingxin Wang, Qian Ma, Xiaolin Lu -
Self-Assembling Imidazolium Nanoaggregates Trigger a Unique Dynamin-Dependent Cell Death via Cytoplasmic Vacuolization and Mitochondrial Dysfunction in Human Lung Adenocarcinoma J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Sayari Dewan, Himanshu Sonker, Kajal Chaudhary, Saloni Agrawal, Ayushi Chaudhary, Ashwini Kumar, Bhumika Agrahari, Ritika Gautam Singh -
A Predictive Model for Thiol Reactivity of N-Heteroaryl α-Methylene−γ-Lactams─A Medicinally Relevant Covalent Reactive Group J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Mariah C. Meehan, Grace E. Scofield, Corrinne E. Stahl, Jacob A. Wolfe, W. Seth Horne, Peng Liu, Kay M. Brummond -
HighPlay: Cyclic Peptide Sequence Design Based on Reinforcement Learning and Protein Structure Prediction J. Med. Chem. (IF 6.8) Pub Date : 2025-05-23
Huitian Lin, Cheng Zhu, Tianfeng Shang, Ning Zhu, Kang Lin, Chengyun Zhang, Xiang Shao, Xudong Wang, Hongliang Duan -
Exploring Long Arm Amide-Linked Side Chains in the Design of Antifungal Azole Inhibitors of Sterol 14α-Demethylase (CYP51) J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Marwa Alsulaimany, Mikhail V. Keniya, Rehab S. Alanazi, Yasmeen N. Ruma, Carwyn S. Hughes, Arwyn T. Jones, Joel D. A. Tyndall, Josie E. Parker, Brian C. Monk, Claire Simons -
Design, Synthesis, and Biological Evaluation of Selective PAK4 Degrader for the Treatment of Lung Tumor Metastasis J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Hanxun Wang, Peilu Song, Yujie Wang, Hanqing Xu, Lanlan Shen, Zhuo Qi, Lu Chen, Lanyan Ma, Zhijian Wang, Xingqi Hu, Wanqing Wang, Na Li, Yage Yu, Yinli Gao, Mingyu Xia, Dongmei Zhao, Jian Wang, Maosheng Cheng -
A DNA-Mediated Lysosomal Degradation Strategy for Targeted Degradation of PD-L1 Protein J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Wenjing Huang, Can Yang, Sizhu Cheng, Shuyue Fu, Xinyu Chen, Yaojin Zhu, Honggang Hu, Fei Gao, Shipeng He -
A “Ligand First” Approach toward Selective, Covalent JNK2/3 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Valentin R. Wydra, Nicole Plank, Stefan Zwirner, Roland Selig, Alexander Rasch, Benedikt Masberg, Michael Lämmerhofer, Lars Zender, Pierre Koch, Wolfgang Albrecht, Stefan Laufer -
Development of Orally Bioavailable Octahydroindole-Based Peptidomimetic Derivative as a Broad-Spectrum Inhibitor against HCoV-OC43 and SARS-CoV-2 J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Shulei Hu, Yumin Zhang, Chenchen Wang, Jian Li, Haixia Su, Xiong Xie, Jiang Wang, Jinlin Wang, Junyuan Cao, Xiaofei He, Yechun Xu, Leike Zhang, Wenhao Dai, Hong Liu -
Discovery of THB Derivates as Ferroptosis Inhibitors for the Treatment of Acute Kidney Injury by Targeting VDAC J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Shengkuan Peng, Wenhao Zhang, Qiaoyi Sun, Wenqiang Zhang, Yadong Chen, Zhicheng Lv, Zhihang Fang, Xian Wei, Tao Lu, Guo Chen, Yu Jiao -
Steric Hindrance-Engineered Redox-Responsive Disulfide-Bridged Homodimeric Prodrug Nanoassemblies for Spatiotemporally Balanced Cancer Chemotherapy J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Tian Liu, Fengli Xia, Yi Zheng, Hongying Xiao, Yuanhao Yu, Jianbin Shi, Shuo Wang, Xianbao Shi, Zhonggui He, Jin Sun, Bingjun Sun -
Targeting the 5-HT2A Receptor for Developing Psychedelic Drugs and Beyond J. Med. Chem. (IF 6.8) Pub Date : 2025-05-22
Saghir Ali, Xiaochen Tian, Kathryn A. Cunningham, Jia Zhou
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