Engineered ipilimumab variants that bind human and mouse CTLA-4 by Brett Robison, SJ Diong, Anusha Kumar, Thomas M. Moon, Olin Chang, Bryant Chau, Christine Bee, Ishita Barman, Arvind Rajpal, Alan J. Korman, Sean West, Pavel Strop, Peter S. Lee

“…Testing of candidate monoclonal antibody therapeutics in preclinical models is an essential step in drug development. Identification of antibody therapeutic candidates that bind their human targets and cross-react to mouse orthologs is often challenging, especially for targets with low sequence homology. …”
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Proximal tubule-on-chip as a model for predicting cation transport and drug transporter dynamics by Isy Petit, Quentin Faucher, Jean-Sébastien Bernard, Perrine Giunchi, Antoine Humeau, François-Ludovic Sauvage, Pierre Marquet, Nicolas Védrenne, Florent Di Meo

“…OoC are particularly relevant at the fundamental and preclinical stages of drug development by providing more accurate assessment of key pharmacokinetic events. …”
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A Comparative Study of the Metabolic and Skeletal Response of C57BL/6J and C57BL/6N Mice in a Diet-Induced Model of Type 2 Diabetes by Elizabeth Rendina-Ruedy, Kelsey D. Hembree, Angela Sasaki, McKale R. Davis, Stan A. Lightfoot, Stephen L. Clarke, Edralin A. Lucas, Brenda J. Smith

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Synthesis and evaluation of nitrochromene derivatives as potential antileishmanial therapeutics through biological and computational studies by Niloofar Javid, Ali Asadipour, Ehsan Salarkia, Mohammad Amin Langarizadeh, Fatemeh Sharifi, Mohammad Mahdavi, Bagher Amirheidari, Aida Iraji, Hojjat Rezaiezadeh, Gholamreza Hassanpour, Yaghoub Pourshojaei

“…This integrative strategy not only enhances the reliability of the findings but also offers valuable insights that could guide future drug development efforts in combating leishmaniasis.…”
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Synthesis, Antimalarial Activity and Molecular Dynamics Studies of Pipecolisporin: A Novel Cyclic Hexapeptide with Potent Therapeutic Potential by Nety Kurniaty, Taufik Muhammad Fakih, Rani Maharani, Unang Supratman, Ace Tatang Hidayat, Nurhidanatasha Abu Bakar, Xiaoshuang Wei

“…Pipecolisporin represents a promising lead for future antimalarial drug development, with its efficacy, stability, and binding characteristics laying a solid foundation for ongoing research.…”
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Synthesis and kinetic evaluation of analogs of (E)-4-amino-3-methylbut-2-en-1-yl diphosphate, a potent inhibitor of the IspH metalloenzyme by Petit, Benoît Eric, Jobelius, Hannah, Bianchino, Gabriella Ines, Guérin, Mélina, Borel, Franck, Chaignon, Philippe, Seemann, Myriam

“…AMBPP has substantial limitations for drug development due to its poor metabolic stability. Here, we investigate the replacement of the diphosphate moiety of AMBPP by more stable mimics: sulfonate, phosphonate or phosphinophosphonate. …”
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Towards New Scaffolds for Antimicrobial Activity—In Silico/In Vitro Workflow Introducing New Lead Compounds by Maria Mangana, George Lambrinidis, Ioannis K. Kostakis, Ioanna Kalpaktsi, Marina Sagnou, Chrysoula Nicolaou, Emmanuel Mikros, Stylianos Chatzipanagiotou, Anastasios Ioannidis

“…<b>Background/Objectives</b>: The rapid evolution of bacterial resistance and the high cost of drug development have attributed greatly to the dearth in drug design. …”
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Regulatory role of S1P and its receptors in sepsis-induced liver injury by Bin Wang, Bin Wang, Xiaoyu Wu, Xiaoyu Wu, Jiangfeng Cheng, Jiangfeng Cheng, Junming Ye, Junming Ye, Hongquan Zhu, Hongquan Zhu, Xiaofeng Liu, Xiaofeng Liu

“…By elucidating the role of S1P and its receptor in the pathogenesis of sepsis liver injury, this review established a molecular targeting framework, providing novel insights into clinical and drug development.…”
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Personalized Therapy in a Patient With EGFR-Mutated NSCLC Developing Sequential CCDC6-RET Fusion and BRAF V600E Mutation as Bypass Resistance Mechanisms by Arianna Marinello, MD, Claudia Parisi, MD, Damien Vasseur, PhD, David Combarel, PharmD, Juliette Bihoreau, NP, Pernelle Lavaud, MD, Rémy Ezzedine, MD, Lodovica Zullo, MD, Luc Friboulet, PhD, Gerard Zalcman, MD, PhD, Antoine Italiano, MD, PhD, Benjamin Besse, MD, PhD, Mihaela Aldea, MD, PhD

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Molecular Mechanism of Local Drug Delivery with Paclitaxel-Eluting Membranes in Biliary and Pancreatic Cancer: New Application for an Old Drug by Sookhee Bang, Sung Ill Jang, Su Yeon Lee, Yi-Yong Baek, Jieun Yun, Soo Jin Oh, Chang Woo Lee, Eun Ae Jo, Kun Na, Sugeun Yang, Don Haeng Lee, Dong Ki Lee

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Cissus quadrangularis L. hexane extract infused glyoxal cross-linked chitosan-collagen scaffold elicits early osteoinduction by Praseetha R. Nair, P.S. Unnikrishnan, Sachin J. Shenoy, G.S. Sailaja

“…Background: The induction of osteoblast activity by natural materials would possibly eliminate toxicity concerns and can serve as a better approach for regenerative drug development studies. Cissus quadrangularis Linn. (CQ) extract is a good source of β-sitosterol, phytoestrogens, β-carotene, flavonoids, etc., and aqueous CQ extract is traditionally used for bone fracture healing. …”
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Exploring the Anticancer Potential of MonoHER (7-Mono-O-(β-Hydroxyethyl)-Rutoside): Mitochondrial-Dependent Apoptosis in HepG2 Cells by Chujie Li, Yue Wang, Jian Liang, Guido R. M. M. Haenen, Yonger Chen, Zhengwen Li, Ming Zhang, Ludwig J. Dubois

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Protective and Ameliorative Effects of Hydroethanolic Extract of Piper nigrum (L.) Stem against Antiretroviral Therapy-Induced Hepatotoxicity and Dyslipidemia in Wistar Rats by Doreen Enyang, Mubo A. Sonibare, Armelle D. Tchamgoue, Lauve R. Y. Tchokouaha, Fanta S. Yadang, Gael N. Nfor, Christelle W. Kom, Patrick D. H. Betote, Cedric F. Tchinda, Steveng S. K. Tiogo, Gabriel A. Agbor

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In Silico Identification of New Anti-SARS-CoV-2 Main Protease (Mpro) Molecules with Pharmacokinetic Properties from Natural Sources Using Molecular Dynamics (MD) Simulations and Hi... by Harrison Onyango, Patrick Odhiambo, David Angwenyi, Patrick Okoth

“…Unfortunately, the traditional drug development methods are time-consuming and expensive. …”
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Enhanced Generation of Human Induced Pluripotent Stem Cells from Peripheral Blood and Using Their Mesoderm Differentiation Ability to Regenerate Infarcted Myocardium by Ju-Young Kim, Han-Mo Yang, Joo-Eun Lee, Mika Jeon, Sang-Bum Bang, Jihye You, Joonoh Kim, Jaewon Lee, Jin Hur, Hyo-Soo Kim

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Structural insights into dynamics of the BMV TLS aminoacylation by Wen Yang, Ran Yi, Jing Yao, Yongxiang Gao, Shanshan Li, Qingguo Gong, Kaiming Zhang

“…These findings not only enhance our knowledge of virus-host interactions but also offer potential targets for antiviral drug development.…”
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Dissecting Causal Relationships Between Antihypertensive Drug, Gut Microbiota, and Type 2 Diabetes Mellitus and Its Complications: A Mendelian Randomization Study by He Zheng, Shiping Wu, Wenbin Wang, Weida Qiu, Yingqing Feng

“…Findings provide novel targets for the treatment of T2DM and its complications, emphasize the importance of KCNJ11 and SLC12A2 in future drug development, and highlight the significant mediating role of the genus Ruminococcus.…”
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Ketamine effects on resting state functional brain connectivity in major depressive disorder patients: a hypothesis-driven analysis based on a network model of depression by Kasper Recourt, Joop Van Gerven, Joop Van Gerven, Nadieh Drenth, Jeroen van der Grond, Kantaro Nishigori, Nic J. Van Der Wee, Gabriël E. Jacobs, Gabriël E. Jacobs

“…Analyzing functional connectivity based on a neurocircuitry model of a specific CNS disease and drug action may be an effective approach that could result in a more targeted analysis in future pharmaco-fMRI studies in CNS drug development.…”
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The protoplast two-way fusions and fusant characteristics of Antrodia cinnamomea and Cordyceps militaris by Wei-Kuang Lai, Yang-Chang Wu, Tai-Sheng Yeh, Chun-Ren Hsieh, Yi-Hong Tsai, Chien-Kei Wei, Chi-Ying Li, Ying-Chen Lu, Fang-Rong Chang

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Caution when using network partners for target identification in drug discovery by Dandan Tan, Yiheng Chen, Yann Ilboudo, Kevin Y.H. Liang, Guillaume Butler-Laporte, J. Brent Richards

“…However, recent data indicate that leveraging human genetic evidence to identify and validate these targets significantly increases the likelihood of success in drug development. Two recent papers from Open Targets claimed that around half of US Food and Drug Administration-approved drugs had targets with direct human genetic evidence. …”
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