Article
Chemistry, Multidisciplinary
Carlo Pifferi, Leire Aguinagalde, Ane Ruiz-de-Angulo, Nagore Sacristan, Priscila Tonon Baschirotto, Ana Poveda, Jesus Jimenez-Barbero, Juan Anguita, Alberto Fernandez-Tejada
Summary: The overexpression of aberrantly glycosylated tumor-associated mucin-1 (TA-MUC1) in human cancers makes it a major target for the development of anticancer vaccines derived from synthetic MUC1-(glyco)peptide antigens. However, glycopeptide-based subunit vaccines are weakly immunogenic, requiring adjuvants and/or additional immunopotentiating approaches to generate optimal immune responses.
Article
Chemistry, Medicinal
Rakesh Pahwa, Jatin Chhabra, Raj Kumar, Rakesh Narang
Summary: This paper discusses key approaches to address resistance associated with melphalan, as well as chemical and formulation developments to enhance its characteristics and targeted profile. The rationale of the article also summarizes recent analytical methods, structure-activity relationship, pharmacokinetics, interactions, potential adverse effects, and medicinal updates of melphalan, including synthetic developments, derivatives, conjugates, and prodrugs, along with encouraging insights and research findings.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Engineering, Environmental
Xiaoxue Xie, Ting Song, Yi Feng, Hanxi Zhang, Geng Yang, Chunhui Wu, Fengming You, Yiyao Liu, Hong Yang
Summary: Cancer immunotherapy, such as cancer vaccines and immune checkpoint blockade, has shown promise in specifically targeting cancer cells. However, there are challenges including side effects, long processing time, immunosuppressive tumor microenvironment, and high cost. Multifunctional nanovaccines based on nanotechnology can overcome these challenges by efficiently delivering tumor antigens and adjuvants and inducing specific antitumor immune responses.
CHEMICAL ENGINEERING JOURNAL
(2022)
Article
Chemistry, Multidisciplinary
Qi Feng, Xiaoyue Yu, Yixue Wang, Shiyang Li, Yang Yang
Summary: Breast cancer is the leading cause of cancer-related deaths among women globally, with HER2 overexpression significantly associated with higher breast tumor proliferation rates. A self-adjuvanting MFCH401-conjugated multiple-component anti-HER2 cancer vaccine was designed to induce a stronger and more durable immune response, showing enhanced immunogenicity compared to previous two-component conjugates.
Review
Immunology
Shubhi Singh, Manisha Singh, Smriti Gaur
Summary: Probiotics, as live microorganisms, have immunomodulatory and anti-tumor properties. Research shows that oral probiotic vaccines can induce mucosal immunity and prevent enteric infections. The production of anti-inflammatory cytokines by probiotic bacteria plays a crucial role in colon cancer therapy. However, further studies are needed to explore the potential of probiotic strains as adjuvants in cancer treatment.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Lorena Simon-Gracia, Valeria Sidorenko, Ain Uustare, Ivan Ogibalov, Andrus Tasa, Olga Tshubrik, Tambet Teesalu
Summary: The novel anthracycline Utorubicin (UTO) shows promising potential as an anticancer agent, especially when formulated in nanocarriers and functionalized with a tumor-penetrating peptide (TPP). Targeted polymeric nanovesicles (PS) loaded with UTO demonstrated the highest accumulation in tumor tissues in mouse models, suggesting its potential application in precision cancer therapy. Further preclinical and clinical studies are encouraged to explore UTO as a nanocarrier payload for treating malignant diseases.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Review
Oncology
Ivan Y. Filin, Kristina V. Kitaeva, Catrin S. Rutland, Albert A. Rizvanov, Valeriya V. Solovyeva
Summary: The development of immunotherapeutic methods for oncological diseases has improved the effectiveness of standard therapies, with dendritic cell vaccines showing promise in expanding treatment options and improving indicators for cancer patients in clinical trials.
FRONTIERS IN ONCOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Nadja B. B. Cech, Nicholas H. H. Oberlies
Summary: Many researchers in the natural product sciences have the dream of discovering a successful drug, but for Dr. Monroe Wall and Dr. Mansukh Wani, their efforts led to the discovery of two new drugs, taxol and camptothecin, which continue to be critical in cancer therapy today.
NATURAL PRODUCT REPORTS
(2023)
Article
Chemistry, Multidisciplinary
Chaoyu Hu, Shengjie Wu, Fei He, Deqin Cai, Zhuojia Xu, Wenjing Ma, Yating Liu, Bangguo Wei, Tiehai Li, Kan Ding
Summary: Bioactive polysaccharides are potential target molecules for drug development, but the synthesis of branched complex polysaccharides with well-defined structures is challenging. In this study, a highly branched heptadecasaccharide moiety of a native bioactive polysaccharide from Carthamus tinctorius L. was efficiently synthesized, and its biological activity in targeting galectin-3 and inhibiting pancreatic cancer cell growth was demonstrated.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Organic
Saibin Zhu, Yeji Wang, Zhongqing Wen, Yanwen Duan, Yong Huang
Summary: The study revealed that Huanglongmycin congener 14 exhibited stronger cytotoxicity against tested cancer cells, and highlighted the critical role of the C-7 ethyl group of 14 in its binding to the DNA-topoisomerase I complex.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Immunology
Shushu Zhao, Shuting Wu, Sheng Jiang, Gan Zhao, Bin Wang
Summary: This study aimed to develop an effective cancer vaccine using inactivated tumor cells and evaluate its tumor protection potential. The results showed that immunization with inactivated CMS5 cells improved tumor suppression in the CMS5 tumor model, but had no effect on the E.G7 tumor model. Dendritic cell responses to tumor antigens were critical, and the combination of inactivated tumor cells with anti-CD25 antibodies showed increased tumor prevention efficacy.
Review
Oncology
Rosmely Hernandez, Thomas R. Malek
Summary: Cancer vaccines have the potential to enhance T cell-mediated antitumor immunity and may be crucial in improving the response to current immunotherapies. However, as monotherapies, cancer vaccines have not been very effective and require the use of adjuvants and immune modulators to enhance their efficacy.
FRONTIERS IN ONCOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Wen-Hao Li, Jing-Yun Su, Yan-Mei Li
Summary: Cancer vaccines aim to enhance tumor-specific immune responses by engaging both T-cell and B-cell immunity. Different factors, including antigen selection, immune activation, vaccine delivery, and repeatable vaccination, should be considered for the rational design of therapeutic cancer vaccines. Chemical strategies such as adjuvants and nanomaterials play crucial roles in advancing the development of effective T-cell- and B-cell-based cancer vaccines.
ACCOUNTS OF CHEMICAL RESEARCH
(2022)
Article
Chemistry, Analytical
Shuaishuai Wang, Ding Liu, Jingyao Qu, He Zhu, Congcong Chen, Christopher Gibbons, Harmon Greenway, Peng Wang, Roni J. Bollag, Kebin Liu, Lei Li
Summary: A new chemoenzymatic strategy was developed to synthesize human IgG glycopeptide standards, allowing for simplified, robust, and precise absolute quantification. Implementation of this method revealed subclass-dependent alterations of serum IgG galactosylation and sialylation in colon cancer samples.
ANALYTICAL CHEMISTRY
(2021)
Review
Oncology
Cheryl Lai-Lai Chiang, Raphael Rovelli, Apostolos Sarivalasis, Lana E. Kandalaft
Summary: The overall survival of ovarian cancer patients is poor, but cancer vaccination may be a potential treatment option. T cells play a significant role in ovarian cancer, suggesting that cancer vaccines capable of eliciting antitumor T cells may be effective in treatment. Strategies for incorporating cancer vaccines into ovarian cancer standard-of-care regimens can be explored, with evidence from murine models showing promising results.
Article
Chemistry, Organic
David Strassburger, Svenja Herziger, Katharina Huth, Moritz Urschbach, Rainer Haag, Pol Besenius
Summary: The synthesis and self-assembly of a sulfate-modified dendritic peptide amphiphile into rod-like architectures in aqueous medium was reported. The influence of ionic strength on supramolecular polymerization was studied, with physiological salt concentrations facilitating the formation of rigid supramolecular polymers. These multivalent sulfated structures exhibit affinity similar to naturally occurring L-selectin ligands.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Evangelia Bolli, Maximilian Scherger, Sana M. Arnouk, Ana Rita Pombo Antunes, David Strassburger, Moritz Urschbach, Judith Stickdorn, Karen De Vlaminck, Kiavash Movahedi, Hans Joachim Rader, Sophie Hernot, Pol Besenius, Jo A. Van Ginderachter, Lutz Nuhn
Summary: The site-specific and quantitative coupling of Toll-like receptor agonist with single chain antibody fragments can repolarize macrophages, leading to a decline in tumor growth and enhancement of anti-tumor immune responses.
Editorial Material
Polymer Science
Pol Besenius, Felix H. Schacher, Takaya Terashima
MACROMOLECULAR RAPID COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Vincent Marichez, Akihiro Sato, Peter A. Dunne, Jorge Leira-Iglesias, Georges J. M. Formon, Michaela K. Schicho, Isja de Feijter, Pascal Hebraud, Matthieu Bailleul, Pol Besenius, Munuswamy Venkatesan, J. M. D. Coey, E. W. Meijer, Thomas M. Hermans
Summary: This research demonstrates that the thermodynamic equilibrium of Gd3+-bearing supramolecular rod networks can be reversibly shifted at room temperature in a static magnetic field of up to 2 T, providing opportunities to control the structure formation of other supramolecular or coordination polymers containing paramagnetic ions.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Polymer Science
Oliver S. Stach, Katharina Breul, Christian M. Berac, Moritz Urschbach, Sebastian Seiffert, Pol Besenius
Summary: This study describes an amphiphilic peptide supramacromolecular hydrogelator with metal-ligand coordination induced gelation and thermoresponsive toughening. By incorporating different transition metal ions, soft and reversible hydrogels were formed with varying strength and viscoelastic behavior. The most dynamically stable interaction supports the formation of robust and responsive hydrogel materials.
MACROMOLECULAR RAPID COMMUNICATIONS
(2022)
Review
Chemistry, Multidisciplinary
Natascha Stergiou, Moritz Urschbach, Adele Gabba, Edgar Schmitt, Horst Kunz, Pol Besenius
Summary: Tumor-associated carbohydrate antigens are overexpressed in most common epithelial cancers, with glycosylation patterns functioning as cancer cell markers. Understanding the parameters of glycans on the MUC backbone is crucial in inducing immune responses. Efforts are being made to design synthetic MUC1/4/16 vaccines and develop cancer subunit vaccines.
Article
Materials Science, Multidisciplinary
Saikat Chakraborty, Christian M. Berac, Moritz Urschbach, Daniel Spitzer, Markus Mezger, Pol Besenius, Thomas Speck
Summary: This study investigates the morphologies and assembly kinetics of pH-responsive supramolecular polymers and develops a model to reproduce the experimental observations. The research finds that acidic and basic peptides in aqueous solution exhibit opposite aggregation states at extreme pH conditions and undergo homo-to-copolymer transition in equimolar mixtures.
ACS APPLIED POLYMER MATERIALS
(2022)
Article
Chemistry, Multidisciplinary
Libin Wu, Liang Cheng, Jing Yang, Yufei Yan, Ensong Zhang, Zdravko Kochovski, Long Li, Zhen Wang, Lianfu Deng, Yan Lu, Pol Besenius, Wenguo Cui, Guosong Chen
Summary: In this study, a new approach is proposed to enhance the stability and degradation property of protein drugs. By adding small-molecular regulator to regulate the self-assembly property of protein drugs, an active protein material with significantly enhanced bone regeneration effect is formed. This material has the advantages of high drug-loading efficiency, easy preparation, and low cost.
ADVANCED MATERIALS
(2022)
Article
Polymer Science
Jonas C. Koelsch, Christian M. Berac, Francisco Lossada, Oliver S. Stach, Sebastian Seiffert, Andreas Walther, Pol Besenius
Summary: This study reports a biobased vitrimer prepolymer synthesized from renewable resources. The obtained vitrimer materials, which are based on cross-linkers, show elastomeric properties and can be easily controlled in terms of rheological properties and recycled. The findings provide a sustainable solution for vitrimer networks that were previously limited to epoxy-based networks.
Article
Polymer Science
Yani Zhao, Jan Rothoerl, Pol Besenius, Peter Virnau, Kostas Ch. Daoulas
Summary: We investigate the effect of helicity in isolated polymers on the topological chirality of their knots with computer simulations. The corrugation of the helix is adjusted via the radius R of a spherical, hard excluded volume around each WLC segment. Statistical analysis of conformations forming the simplest chiral knots demonstrates that knots formed by helices with a given sense prefer one handedness over the other.
Article
Chemistry, Multidisciplinary
Adele Gabba, Riem Attariya, Sandra Behren, Christian Pett, Joost C. van der Horst, Hajime Yurugi, Jin Yu, Moritz Urschbach, Juan Sabin, Gabriel Birrane, Edgar Schmitt, Sandra J. van Vliet, Pol Besenius, Ulrika Westerlind, Paul V. Murphy
Summary: The expression and glycosylation patterns of mucin on cancer cells differ from healthy cells, making them attractive targets for immunotherapy. In this study, a modular tripartite vaccine targeting macrophage galactose-type lectin (MGL) on antigen presenting cells was prepared using solid phase peptide synthesis. The vaccine induced a higher antibody response against tumor-associated carbohydrate antigens (TACAs) compared to TACAs alone, highlighting its potential as an anticancer vaccine.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Biochemistry & Molecular Biology
Tobias A. A. Bauer, Irina Alberg, Lydia A. A. Zengerling, Pol Besenius, Kaloian Koynov, Bram Slutter, Rudolf Zentel, Ivo Que, Heyang Zhang, Matthias Barz
Summary: Core cross-linked polymeric micelles (CCPMs) are designed to improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation, and offer prolonged circulation times. CCPM stability was tuned by using bifunctional or trifunctional cross-linkers and varying the cross-linkable polymer block length. The circulation time and biodistribution of CCPMs can be enhanced by using trivalent peptide cross-linkers.
Article
Polymer Science
Marius Thomas, Vanessa Lewe, Jonas Koelsch, Moritz Urschbach, Jessica Erlenbusch, Oliver Sven Stach, Pol Besenius
Summary: We investigated the kinetics of assembly of an Au(i)-metallopeptide amphiphile, which forms long and rigid nanofibers. By developing a precise preparation protocol, we measured the concentration-dependent assembly kinetics and found that nucleation-elongation dominates the supramolecular polymerisation process. We observed significant differences in assembly behavior and morphology in aqueous media with as low as 1 vol% organic solvent compared to pure buffer.
Article
Polymer Science
Long Li, Libin Wu, Moritz Urschbach, David Strassburger, Xiaomei Liu, Pol Besenius, Guosong Chen
Summary: Glycopeptide supramolecular polymers displaying multivalent carbohydrates have great potential for immune relevant biomaterials. However, the diversity and complexity of carbohydrates have hindered the development of glycopeptide supramolecular monomers. Therefore, a modular platform for presenting various carbohydrates and generating supramolecular polymers with variable functionality is highly desired.
Article
Chemistry, Organic
Friedrich Stricker, Jonas Christopher Koelsch, Sebastian B. Beil, Sebastian Preiss, Siegfried R. Waldvogel, Till Opatz, Pol Besenius
Summary: This study established a convenient approach for the synthesis of foldable redox-active flavin peptide conjugates. It was demonstrated that azidolysine side-chains can be readily functionalised with an alkyne-bearing flavine derivative using a model beta-hairpin oligopeptide motif. The folding equilibrium of the peptide backbone and the redox behavior of the flavin moieties remained intact after the conjugation.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
