Article
Chemistry, Multidisciplinary
George J. Saunders, Andrei K. Yudin
Summary: The passive membrane permeability of macrocycles can be greatly improved by incorporating heterocyclic grafts. However, the permeability does not scale linearly with the number of heterocycles, highlighting the subtleties of the conformation-property relationship in this class of molecules.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Alex Nazzaro, Brandon Lu, Nicholas Sawyer, Andrew M. Watkins, Paramjit S. Arora
Summary: Mimics of protein secondary and tertiary structure can be used as inhibitors of biomolecular interactions. By replacing inter-beta-strand hydrogen bonds with hydrogen bond surrogates (HBS), we have designed a minimal mimic of a protein beta-sheet without the need for natural or synthetic beta-turns. A bioinformatics survey of protein beta-sheets revealed an abundance of aromatic-aromatic, cation-p and ionic interactions, which we incorporated into our design. Experimental techniques like circular dichroism, NMR spectroscopy, and X-ray crystallography support our design.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Medicinal
Adrian Krzyzanowski, Lea Marie Esser, Anthony Willaume, Renaud Prudent, Christoph Peter, Peter't Hart, Herbert Waldmann
Summary: The PRMT5-MEP50 methyltransferase is a major target for the development of anticancer drugs. Researchers have designed and synthesized a new peptide compound that specifically inhibits the interaction between PRMT5 and adaptor proteins RioK1 and pICln. This new inhibitor has great potential for further biological investigations.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Christopher Berube, Alexandre Borgia, Normand Voyer
Summary: We report the first total synthesis of the macrocyclic decapeptide stylopeptide II, which was achieved using an efficient methodology with oxime resin as solid support. The synthesis was performed at gram-scale without the generation of any detectable undesired side products, demonstrating the general applicability and large-scale synthesis acceleration of this method.
TETRAHEDRON LETTERS
(2022)
Article
Oncology
Yuchen Zhang, Michael B. Ware, Mohammad Y. Zaidi, Amanda N. Ruggieri, Brian M. Olson, Hannah Komar, Matthew R. Farren, Ganji Purnachandra Nagaraju, Chao Zhang, Zhengjia Chen, Juan M. Sarmiento, Rafi Ahmed, Shishir K. Maithel, Bassel F. El-Rayes, Gregory B. Lesinski
Summary: Studies show that Hsp90 inhibition can limit inflammatory signals, reprogram the PDAC tumor microenvironment, and enhance sensitivity to PD-1 blockade. Hsp90 inhibitors directly affect PSC/CAF growth and enhance the efficacy of anti-PD-1 blockade in vivo.
MOLECULAR CANCER THERAPEUTICS
(2021)
Article
Biochemistry & Molecular Biology
Keyvan Pedrood, Maedeh Sherafati, Maryam Mohammadi-Khanaposhtani, Mohammad Sadegh Asgari, Samanesadat Hosseini, Hossein Rastegar, Bagher Larijani, Mohammad Mahdavi, Parham Taslimi, Yavuz Erden, Sevilay Gunay, Ilhami Gulcin
Summary: Novel quinazolinone derivatives were synthesized and evaluated for their inhibitory activities against various metabolic enzymes, showing high inhibitory activities. The most potent compounds against each enzyme were selected to evaluate their interaction modes in the active site, while cytotoxicity assays demonstrated that these compounds do not exhibit significant cytotoxic effects on cancer cell lines.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Medicinal
Muhammad Ibrahim, Abdul Latif, Ammara, Akbar Ali, Alany Ingrid Ribeiro, Umar Farooq, Farhat Ullah, Ajmal Khan, Ahmed Al-Harrasi, Manzoor Ahmad, Mumtaz Ali
Summary: A series of artificial macrocycles based on a 4,4'-sulfonyldiphenol intermediate were successfully synthesized through a multistep procedure involving oxidation, etherification, and ring closure, yielding 15 macrocycles characterized through modern spectroscopic techniques. Some of these macrocycles demonstrated significant AChE and BChE inhibition, highlighting their potential importance in studying interactions with various enzymatic targets.
DRUG DEVELOPMENT RESEARCH
(2021)
Article
Chemistry, Inorganic & Nuclear
Paulpandiyan Rajakkani, Arunadevi Alagarraj, Senthil A. Gurusamy Thangavelu
Summary: A new tetraaza macrocyclic Knoevenagel Schiff base and its metal complexes were synthesized and characterized, showing potential biological activities and binding properties with DNA. Multiple spectroscopic and analytical techniques were used to study the compounds, including experiments to determine the type of binding with nucleic acids.
INORGANIC CHEMISTRY COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Eray Caliskan, Alpaslan Kaplan, Guldeniz Sekerci, Irfan Capan, Suat Tekin, Sultan Erkan, Kenan Koran, Sueleyman Sandal, Ahmet O. Gorgulu
Summary: In this study, a series of tripeptides based on tyrosine amino acids were synthesized, and their cytotoxicity properties against various cancer cell lines were determined. The compounds exhibited significant decreases in cell viability and were found to induce DNA damage. Docking studies revealed interactions between the compounds and target proteins, and ADME analysis identified molecules with high biological activity against biological receptors.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Armagan Gunsel, Bilge Yazar, Parham Taslimi, Yavuz Erden, Tugba Taskin-Tok, Hasan Piskin, Ahmet T. Bilgicli, M. Nilufer Yarasir, Ilhami Gulcin
Summary: In this study, a novel starting material was synthesized and its structure was verified. Several new phthalocyanine compounds were synthesized and characterized using various spectroscopic methods. These compounds showed inhibitory effects on acetylcholinesterase and alpha-glycosidase enzymes, and exhibited normal cytotoxic effects on cancer cells.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biology
Erich Stefan, Richard Obexer, Susanne Hofmann, Khanh Vu Huu, Yichao Huang, Nina Morgner, Hiroaki Suga, Robert Tampe
Summary: The study identified high-affinity peptidic macrocycles through RaPID technology, which selectively bind to the ABC transport complex and display potent inhibitory effects. These macrocycles can block the transporter during conformational switching induced by ATP binding, revealing some fundamental principles of ABC transport.
Article
Oncology
Xiaohui Wang, Jun Zhang, Zhijian Han, Liheng Ma, Yumin Li
Summary: A novel probe, F-18-NOTA-Dimer-San A, was developed for PET imaging of Hsp90 expression in pancreatic cancer and has the potential to discriminate pancreatic cancer from inflammatory mass.
Article
Oncology
Katharina M. Ewers, Shilpa Patil, Waltraut Kopp, Juergen Thomale, Tabea Quilitz, Anna Magerhans, Xin Wang, Elisabeth Hessmann, Matthias Dobbelstein
Summary: Pancreatic cancer cells show varied sensitivities to cisplatin, with some being sensitive due to high expression of GATA6 and microRNA 200, while others can be sensitized by inhibiting HSP90. The combination of cisplatin and HSP90 inhibitors has shown promise in improving treatment outcomes for PDAC.
Article
Biochemistry & Molecular Biology
Xinyi Wang, Xin Ai, Zehui Zhu, Mingxin Zhang, Fei Pan, Zichen Yang, Ou Wang, Liang Zhao, Lei Zhao
Summary: Peptides derived from sesame could potentially inhibit the activity of pancreatic lipase, reducing triglyceride absorption and preventing obesity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Chemistry, Physical
B. N. Nippu, R. Sandeep Kumar Jain, Abdul Rahman, H. M. Kumaraswamy, N. D. Satyanarayan
Summary: This study designed and synthesized novel tetrazole fused quinoline bridged isatin molecules with biodynamic activity, which showed higher cytotoxicity against pancreatic cancer cell lines in vitro and suggested potential for further evaluation.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Anna Aiello, Ernesto Fattorusso, Paolo Luciano, Marialuisa Menna, Marco A. Calzado, Eduardo Munoz, Francesco Bonadies, Marcella Guiso, Maria Filomena Sanasi, Gianfranco Cocco, Rosario Nicoletti
BIOORGANIC & MEDICINAL CHEMISTRY
(2010)
Article
Chemistry, Medicinal
Andrew Scribner, David Houck, Zhuhui Huang, Sarah Mosier, Michael Peel, Bernard Scorneaux
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2010)
Article
Chemistry, Multidisciplinary
James L. Carr, Daniel A. Offermann, Mary D. Holdom, Philip Dusart, Andrew J. P. White, Andrew J. Beavil, Robin J. Leatherbarrow, Stephen D. Lindell, Brian J. Sutton, Alan C. Spivey
CHEMICAL COMMUNICATIONS
(2010)
Article
Agriculture, Multidisciplinary
Chun-Hsu Pan, I-Chun Hsieh, Fon-Chang Liu, Wen-Tsong Hsieh, Ming-Jyh Sheu, Ayano Koizumi, Chieh-Hsi Wu
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2010)
Article
Biochemical Research Methods
Yadollah Yamini, Mohammad Rezaee, Alireza Khanchi, Mohammad Faraji, Abolfazl Saleh
JOURNAL OF CHROMATOGRAPHY A
(2010)
Article
Engineering, Chemical
M. C. Campo, F. D. Magalhaes, A. Mendes
JOURNAL OF MEMBRANE SCIENCE
(2010)
Article
Plant Sciences
Ashootosh Tripathi, Jonathan Puddick, Michele R. Prinsep, Matthias Rottmann, Lik Tong Tan
JOURNAL OF NATURAL PRODUCTS
(2010)
Article
Chemistry, Physical
Atsushi Yoshizawa, Ayumi Nishizawa, Kazuhito Takeuchi, Yoichi Takanishi, Jun Yamamoto
JOURNAL OF PHYSICAL CHEMISTRY B
(2010)
Article
Chemistry, Multidisciplinary
Alberto Plaza, Jessica L. Keffer, Giuseppe Bifulco, John R. Lloyd, Carole A. Bewley
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2010)
Article
Biochemical Research Methods
Ellen Tenstad, Anna Tourovskaia, Albert Folch, Ola Myklebost, Edith Rian
Article
Chemistry, Multidisciplinary
Stephanie E. McCalla, Anubhav Tripathi
Article
Biochemistry & Molecular Biology
David Y. -K. Chen, Qiang Kang, T. Robert Wu
Article
Chemistry, Organic
Jing Xu, Eduardo J. E. Caro-Diaz, Emmanuel A. Theodorakis
Article
Chemistry, Organic
Srivari Chandrasekhar, Ambadi Sudhakar
Article
Biochemical Research Methods
Alberto Sanchez-Guijo, Olimpio Montero
RAPID COMMUNICATIONS IN MASS SPECTROMETRY
(2010)