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Journal articles on the topic 'Dual-warhead'

Author: Grafiati

Published: 14 March 2023

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1

Kim, Jisu, Ching-Hsuan Tung, and Yongdoo Choi. "Smart dual-functional warhead for folate receptor-specific activatable imaging and photodynamic therapy." Chem. Commun. 50, no. 73 (2014): 10600–10603. http://dx.doi.org/10.1039/c4cc04166f.

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2

Świderska, Karolina, Anna Szlachcic, Łukasz Opaliński, Małgorzata Zakrzewska та Jacek Otlewski. "FGF2 Dual Warhead Conjugate with Monomethyl Auristatin E and α-Amanitin Displays a Cytotoxic Effect towards Cancer Cells Overproducing FGF Receptor 1". International Journal of Molecular Sciences 19, № 7 (2018): 2098. http://dx.doi.org/10.3390/ijms19072098.

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In the rapidly developing field of targeted cancer therapy there is growing interest towards therapeutics combining two or more compounds to achieve synergistic action and minimize the chance of cancer resistance to treatment. We developed a fibroblast growth factor 2 (FGF2)-conjugate bearing two cytotoxic drugs with independent mode of action: α-amanitin and monomethyl auristatin E. Drugs are covalently attached to the targeting protein in a site-specific manner via maleimide-thiol conjugation and Cu(I)-catalyzed alkyne-azide cycloaddition. The dual warhead conjugate binds to FGF receptor 1 (

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3

Johns, Brian A., and Carl R. Johnson. "Scaffolded bis-azasugars: A dual warhead approach to glycosidase inhibition." Tetrahedron Letters 39, no. 8 (1998): 749–52. http://dx.doi.org/10.1016/s0040-4039(97)10616-5.

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4

Brouwer, Arwin J., Natalia Herrero Álvarez, Adriano Ciaffoni, Helmus van de Langemheen, and Rob M. J. Liskamp. "Proteasome inhibition by new dual warhead containing peptido vinyl sulfonyl fluorides." Bioorganic & Medicinal Chemistry 24, no. 16 (2016): 3429–35. http://dx.doi.org/10.1016/j.bmc.2016.05.042.

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5

JOHNS, B. A., and C. R. JOHNSON. "ChemInform Abstract: Scaffolded Bis-azasugars: A Dual Warhead Approach to Glycosidase Inhibition." ChemInform 29, no. 19 (2010): no. http://dx.doi.org/10.1002/chin.199819222.

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6

Bhattacharyya, Soumalya, Mangili Venkateswarulu, Jagabandhu Sahoo, Ennio Zangrando, Mrinmoy De, and Partha Sarathi Mukherjee. "Self-Assembled PtII8 Metallosupramolecular Tubular Cage as Dual Warhead Antibacterial Agent in Water." Inorganic Chemistry 59, no. 17 (2020): 12690–99. http://dx.doi.org/10.1021/acs.inorgchem.0c01777.

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7

Astrain-Redin, Nora, Irene Talavera, Esther Moreno, et al. "Seleno-Analogs of Scaffolds Resembling Natural Products a Novel Warhead toward Dual Compounds." Antioxidants 12, no. 1 (2023): 139. http://dx.doi.org/10.3390/antiox12010139.

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Nowadays, oxidative cell damage is one of the common features of cancer and Alzheimer’s disease (AD), and Se-containing molecules, such as ebselen, which has demonstrated strong antioxidant activity, have demonstrated well-established preventive effects against both diseases. In this study, a total of 39 Se-derivatives were synthesized, purified, and spectroscopically characterized by NMR. Antioxidant ability was tested using the DPPH assay, while antiproliferative activity was screened in breast, lung, prostate, and colorectal cancer cell lines. In addition, as a first approach to evaluate th

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8

Shi, Yun Bo, Sheng Fei Dong, and Zhi Jun Zhou. "Study on Measurement Method of Dynamic Linearity for High G Micro Accelerometer." Key Engineering Materials 609-610 (April 2014): 908–13. http://dx.doi.org/10.4028/www.scientific.net/kem.609-610.908.

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Linearity, dynamic linearity particularly, is an important parameter in measuring the performance of an accelerometer. The Hopkinson bar has been widely used in calibration of high g accelerometer and other high overloading conditions. Based on one-dimension stress wave theory and superposition theory of elastic waves, designed a Dual Warhead Hopkinson bar to demarcate the dynamic linear parameters of high g micro accelerometer accurately. A finite element model for Hopkinson bar calibration system was created, ANSYS/LS-DYNA was employed to simulate the operation process of Hopkinson bar, and

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9

Chinthakindi, Praveen K., Kimberleigh B. Govender, A. Sanjeeva Kumar та ін. "A Synthesis of “Dual Warhead” β-Aryl Ethenesulfonyl Fluorides and One-Pot Reaction to β-Sultams". Organic Letters 19, № 3 (2017): 480–83. http://dx.doi.org/10.1021/acs.orglett.6b03634.

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10

Vineberg, Jacob G., Edison S. Zuniga, Anushree Kamath, Ying-Jen Chen, Joshua D. Seitz, and Iwao Ojima. "Design, Synthesis, and Biological Evaluations of Tumor-Targeting Dual-Warhead Conjugates for a Taxoid–Camptothecin Combination Chemotherapy." Journal of Medicinal Chemistry 57, no. 13 (2014): 5777–91. http://dx.doi.org/10.1021/jm500631u.

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11

Mohapatra, Saswat, Abhijit Saha, Prasenjit Mondal, et al. "Synergistic Anticancer Effect of Peptide-Docetaxel Nanoassembly Targeted to Tubulin: Toward Development of Dual Warhead Containing Nanomedicine." Advanced Healthcare Materials 6, no. 2 (2016): 1600718. http://dx.doi.org/10.1002/adhm.201600718.

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12

Krzyscik, Mateusz Adam, Łukasz Opaliński, and Jacek Otlewski. "Novel Method for Preparation of Site-Specific, Stoichiometric-Controlled Dual Warhead Conjugate of FGF2 via Dimerization Employing Sortase A-Mediated Ligation." Molecular Pharmaceutics 16, no. 8 (2019): 3588–99. http://dx.doi.org/10.1021/acs.molpharmaceut.9b00434.

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13

Shi, Yunbo, Zhicai Yang, Zongmin Ma, et al. "The Development of a Dual-Warhead Impact System for Dynamic Linearity Measurement of a High-g Micro-Electro-Mechanical-Systems (MEMS) Accelerometer." Sensors 16, no. 6 (2016): 840. http://dx.doi.org/10.3390/s16060840.

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14

Thiyagarajan, Durairaj, Sudeep Goswami, Chirantan Kar, Gopal Das, and Aiyagari Ramesh. "A prospective antibacterial for drug-resistant pathogens: a dual warhead amphiphile designed to track interactions and kill pathogenic bacteria by membrane damage and cellular DNA cleavage." Chemical Communications 50, no. 56 (2014): 7434. http://dx.doi.org/10.1039/c4cc02354d.

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15

Ailawadhi, Sikander, Asher Alban Akmal Chanan-Khan, Jennifer Layton Peterson, et al. "Treatment free remission (TFR) and overall response rate (ORR) results in patients with relapsed/refractory Waldenstrom’s macroglobulinemia (WM) treated with CLR 131." Journal of Clinical Oncology 39, no. 15_suppl (2021): 7561. http://dx.doi.org/10.1200/jco.2021.39.15_suppl.7561.

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7561 Background: Phospholipid ethers (PLE) provide a novel mechanism to specifically target tumor cells leveraging high lipid raft content in their cell membranes. PLE/phospholipid drug conjugates are specifically designed to have high affinity to lipid rafts which upon binding results in trans-membrane flipping with the ability to deliver an attached warhead directly to the cytosol. CLR 131 (I-131-CLR1404) is a novel PLE molecule armed with I-131 resulting in targeted tumor cell radiotherapy which is being examined in relapsed or refractory WM through an open-label, Phase 2 trial, CLOVER-1 (N

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16

Manda, Sudhakar, Na Keum Lee, Dong-Chan Oh, and Jeeyeon Lee. "Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src." Molecules 25, no. 8 (2020): 1948. http://dx.doi.org/10.3390/molecules25081948.

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A focused PROTAC library was developed to degrade both IGF-1R and Src proteins, which are associated with various cancers. PROTACs with IGF-1R and Src degradation potentials were synthesized by tethering different inhibitor warhead units and the E3 ligase (CRBN) recruiting-pomalidomide with various linkers. The designed PROTACs 12a–b inhibited the proliferation and migration of MCF7 and A549 cancer cells with low micromolar potency (1–5 μM) in various cellular assays.

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17

Chen, Xiaojuan, Huiliang Li, Qianmeng Lin, et al. "Structure-based design of a dual-warhead covalent inhibitor of FGFR4." Communications Chemistry 5, no. 1 (2022). http://dx.doi.org/10.1038/s42004-022-00657-9.

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AbstractThe fibroblast growth factor 19 (FGF19)/fibroblast growth factor receptor 4 (FGFR4) signaling pathways play critical roles in a variety of cancers, such as hepatocellular carcinoma (HCC). FGFR4 is recognized as a promising target to treat HCC. Currently, all FGFR covalent inhibitors target one of the two cysteines (Cys477 and Cys552). Here, we designed and synthesized a dual-warhead covalent FGFR4 inhibitor, CXF-009, targeting Cys477 and Cys552 of FGFR4. We report the cocrystal structure of FGFR4 with CXF-009, which exhibits a dual-warhead covalent binding mode. CXF-009 exhibited stron

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18

Guo, Xiao-Jun, and He-Ming Wen. "Performance Analysis and Optimization of a Dual Warhead System." International Journal of Nonlinear Sciences and Numerical Simulation 13, no. 1 (2012). http://dx.doi.org/10.1515/ijnsns-2011-0100.

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AbstractIn modern warfare earth penetrating weapons are often used to defeat enemy’s hardened and deeply buried targets such as aircraft shelters and bunkers. A dual warhead system (DWS) is one of such weapons composed of a forward shaped charge (FSC) and a following through warhead (FTW). In this paper, an analytical model is first proposed to analyze the penetration of an FTW into concrete targets with pre-drilled holes and a DWS is then optimized in order to achieve its best penetration performance. The effects of various parameters on the performance of a dual warhead system penetrating a

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19

Guo, Xiao-Jun, and He-Ming Wen. "Performance Analysis and Optimization of a Dual Warhead System." International Journal of Nonlinear Sciences and Numerical Simulation 13, no. 1 (2012). http://dx.doi.org/10.1515/ijnsns-2011-100.

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AbstractIn modern warfare earth penetrating weapons are often used to defeat enemy’s hardened and deeply buried targets such as aircraft shelters and bunkers. A dual warhead system (DWS) is one of such weapons composed of a forward shaped charge (FSC) and a following through warhead (FTW). In this paper, an analytical model is first proposed to analyze the penetration of an FTW into concrete targets with pre-drilled holes and a DWS is then optimized in order to achieve its best penetration performance. The effects of various parameters on the performance of a dual warhead system penetrating a

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20

Chen, Xiaojuan, Huiliang Li, Qianmeng Lin, et al. "Author Correction: Structure-based design of a dual-warhead covalent inhibitor of FGFR4." Communications Chemistry 5, no. 1 (2022). http://dx.doi.org/10.1038/s42004-022-00672-w.

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21

Moreira, Wilfried, Sridhar Santhanakrishnan, Brian W. Dymock, and Thomas Dick. "Bortezomib Warhead-Switch Confers Dual Activity against Mycobacterial Caseinolytic Protease and Proteasome and Selectivity against Human Proteasome." Frontiers in Microbiology 8 (April 27, 2017). http://dx.doi.org/10.3389/fmicb.2017.00746.

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22

Cheng, Lin, Shichao Zhou, Shaoqing Zhou, et al. "Dual inhibition of CDK12/CDK13 targets both tumor and immune cells in ovarian cancer." Cancer Research, July 20, 2022. http://dx.doi.org/10.1158/0008-5472.can-22-0222.

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Abstract Therapeutic perturbation of cyclin-dependent kinase 12 (CDK12) is proposed to have pleiotropic effects in ovarian cancer, including direct cytotoxicity against tumor cells and indirect induction of immunogenicity that confer synthetic sensitivity to immune-based treatment. However, formal testing of this hypothesis has been hindered by an insufficient mechanistic understanding of CDK12 and its close homolog CDK13, as well as generally unfavorable pharmacokinetics of available CDK12/CDK13 covalent inhibitors. In this study, we employed an innovative arsenous warhead modality to develop

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23

Mohapatra, Saswat, Abhijit Saha, Prasenjit Mondal, et al. "Antimitoic Peptides: Synergistic Anticancer Effect of Peptide-Docetaxel Nanoassembly Targeted to Tubulin: Toward Development of Dual Warhead Containing Nanomedicine (Adv. Healthcare Mater. 2/2017)." Advanced Healthcare Materials 6, no. 2 (2017). http://dx.doi.org/10.1002/adhm.201770011.

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