Review
Chemistry, Inorganic & Nuclear
Debabrata Chatterjee, Olga Impert, Rudi van Eldik
Summary: The nitrogen cycle is a critical biogeochemical cycle involving redox conversions, such as nitrogen fixation and nitrification/denitrification pathways. This review focuses on the application of Ru(edta) complexes in electrochemical transformations related to the nitrogen cycle, providing mechanistic insights into their roles in nitrogen fixation and denitrification reactions.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Biochemistry & Molecular Biology
Kira V. V. Derkach, Maxim A. A. Gureev, Anastasia A. A. Babushkina, Vladimir N. N. Mikhaylov, Irina O. O. Zakharova, Andrey A. A. Bakhtyukov, Viktor N. N. Sorokoumov, Alexander S. S. Novikov, Mikhail Krasavin, Alexander O. O. Shpakov, Irina A. A. Balova
Summary: This article describes the identification of dual inhibitors of protein phosphotyrosine phosphatase 1B (PTP1B)/T-cell protein phosphotyrosine phosphatase (TC-PTP) based on the 3-(hydroxymethyl)-4-oxo-1,4-dihydrocinnoline scaffold. The compounds were evaluated for their effects on obesity-related parameters and gene expressions. The results indicate the potential of these compounds as dual inhibitors for the treatment of metabolic disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Nguyen Viet Phong, Vu Thi Oanh, Seo Young Yang, Jae Sue Choi, Byung Sun Min, Jeong Ah Kim
Summary: This study isolated 30 phloroglucinols from Dryopteris crassirhizoma and identified trimeric phloroglucinols 26-28 as potent inhibitors of PTP1B, suggesting their potential for treating type 2 diabetes.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Biochemistry & Molecular Biology
James Adams, Benjamin P. Thornton, Lydia Tabernero
Summary: The study identified unique ligand cluster distributions specific to kinase interaction motif protein tyrosine phosphatases (KIM-PTPs) and found that ligand clusters coincide with functional and substrate binding sites in these PTPs. Ligand efficiency index (LEI) analysis showed that binders in these clusters reside in a more drug-like chemical-biological space. Differences in clusters across all KIM-PTPs highlight a distinct and specific profile for each phosphatase, with potential for exploiting unexplored allosteric functional sites for drug development.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Alexander Drilon, Manish R. Sharma, Melissa L. Johnson, Timothy A. Yap, Shirish Gadgeel, Dale Nepert, Gang Feng, Micaela B. Reddy, Allison S. Harney, Mohamed Elsayed, Adam W. Cook, Christina E. Wong, Ronald J. Hinklin, Yutong Jiang, Eric N. Brown, Nickolas A. Neitzel, Ellen R. Laird, Wen - Wu, Anurag Singh, Ping Wei, Keith A. Ching, John J. Gaudino, Patrice A. Lee, Dylan P. Hartley, S. Michael Rothenberg
Summary: PF-07284892, an allosteric SHP2 inhibitor, combined with various oncogenic driver inhibitors, overcame bypass-signaling-mediated resistance in clinical settings. This combination therapy showed significant tumor and circulating tumor DNA responses, extending the duration of overall clinical benefit in patients with targeted therapy resistance in lung, colorectal, ovarian, and pancreatic cancer.
Article
Biochemistry & Molecular Biology
Evangelia Papadimitriou, Vasiliki K. Kanellopoulou
Summary: Protein tyrosine phosphatase receptor zeta 1 (PTPRZ1) is highly expressed during embryonic development but limited in adulthood. It plays a role in oligodendrocytes' survival and maturation in the central nervous system. In gliomas, PTPRZ1 is significantly upregulated and studied as a potential cancer driver and therapy target. However, its functional significance and tumor-suppressor role in other cancer types need further investigation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Physical
Anika J. Friedman, Evan T. Liechty, Levi Kramer, Ankur Sarkar, Jerome M. Fox, Michael R. Shirts
Summary: Protein tyrosine phosphatases (PTPs) are potential drug targets for various diseases, but the design of selective therapeutics is complicated. This study investigates the allosteric inhibition of PTP1B by AD, an unusually selective inhibitor. Molecular dynamics simulations suggest that AD stably interacts with the allosterically influential region of PTP1B. The binding requires a disordered alpha 7 helix, contributing to the selectivity of AD. The findings indicate the potential of AD as a scaffold for building allosteric inhibitors of PTP1B.
JOURNAL OF PHYSICAL CHEMISTRY B
(2022)
Article
Plant Sciences
Zheng Zhang, Zhi-Peng Shang, Yan Jiang, Zhao-Xia Qu, Ren-Yong Yang, Jing Zhang, Ye-Xi Lin, Feng Zhao
Summary: Protein tyrosine phosphatase 1B (PTP1B) is an important target for treating type 2 diabetes. However, current PTP1B inhibitors lack selectivity and bioavailability. A study on Knoxia valerianoides led to the discovery of a unique anthraquinone-coumarin hybrid with good specificity for PTP1B. Further investigation of this plant led to the isolation of nine new anthraquinone glycosides and two known ones. All compounds showed PTP1B inhibitory activities, with compounds 4 and 8 exhibiting high selectivity for PTP1B over TCPTP.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Cell Biology
Seung Un Seo, Seon Min Woo, Taeg Kyu Kwon
Summary: This study revealed that cathepsin K inhibition activates SHP2, a tyrosine phosphatase, which dephosphorylates OTUB1 and destabilizes Raptor, leading to mitochondrial dysfunction. The findings also identified Syk as an upstream tyrosine kinase required for SHP2 activation and showed that targeting the Syk/SHP2/Src/OTUB1 axis may be a potential therapeutic strategy for cancer management.
CELL DEATH & DISEASE
(2023)
Article
Biochemistry & Molecular Biology
Shun-Yi Jian, Salim Levent Aktug, Hsuan-Ti Huang, Cheng-Jung Ho, Sung-Yen Lin, Chung-Hwan Chen, Min-Wen Wang, Chun-Chieh Tseng
Summary: Micro arc oxidation (MAO) was used to modify the surface characteristics of AZ31 Mg alloy for implant applications, resulting in improved biocompatibility, corrosion resistance, and the formation of a calcium phosphate (Ca-P) containing thin film. After in-vivo implantation, the coating showed enhanced proliferation activity, better corrosion resistance, and lower roughness compared to mere MAO coatings on AZ31 alloy. This study demonstrates the potential feasibility of using MAO coatings for orthopedic implants in clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Bin Wei, Lingyan Xu, Wenjie Guo, Yuanyuan Wang, Jingjing Wu, Xiaofei Li, Xiaomin Cai, Jinbo Hu, Meijing Wang, Qiang Xu, Wen Liu, Yanhong Gu
Summary: SHP2 dephosphorylates PARP1 to simultaneously suppress DNA repair and enhance STING pathway-mediated antitumor immunity, suggesting SHP2 activation as a potential therapeutic approach in colon cancer. The combination of lovastatin and chemotherapy may enhance the efficacy of treatment by exacerbating STING pathway activation in tumor cells.
Article
Medicine, Research & Experimental
Won Jin Ho, Sarah Croessmann, Jianping Lin, Zaw H. Phyo, Soren Charmsaz, Ludmila Danilova, Aditya A. Mohan, Nicole E. Gross, Fangluo Chen, Jiajun Dong, Devesh Aggarwal, Yunpeng Bai, Janey Wang, Jing He, James M. Leatherman, Mark Yarchoan, Todd D. Armstrong, Neeha Zaidi, Elana J. Fertig, Joshua C. Denny, Ben H. Park, Zhong-Yin Zhang, Elizabeth M. Jaffee
Summary: Research has shown that PTPN22 could be a viable target for cancer immunotherapy, with the rs2476601 variant being linked to a lower risk of cancer development. Inhibiting PTPN22 was found to enhance activation of CD8(+) T cells and macrophages towards M1-like phenotypes, leading to improved antitumor efficacy. Moreover, combining PTPN22 inhibition with PD-1 blockade further boosted antitumor effects, particularly in cancer patients with the rs2476601 variant.
JOURNAL OF CLINICAL INVESTIGATION
(2021)
Article
Chemistry, Medicinal
Alena Mrkvicova, Eva Peterova, Ivan Nemec, Radka Krikavova, Darina Muthna, Radim Havelek, Petra Kazimirova, Martina Rezacova, Pavel Starha
Summary: This study synthesized nine half-sandwich Rh(III) and Ru(II) complexes and investigated their antiproliferative activity in human cancer cell lines. The Rh(III) complex 6 showed high activity in ovarian cancer cells, including those resistant to the conventional drug cisplatin, with promising selectivity and a unique mechanism of action. It reduced DNA synthesis and upregulated CDKN1A expression, but did not induce p21 expression. The study concluded that complex 6 exhibited high antiproliferative activity through a p21-independent mechanism of action.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Joseph Farahany, Yoshikazu Tsukasaki, Amitabha Mukhopadhyay, Manish Mittal, Saroj Nepal, Chinnaswamy Tiruppathi, Asrar B. Malik
Summary: CD38 inhibits NLRP3 activation and can prevent endotoxemic ALI, suggesting it as a potential therapeutic target.
AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY
(2022)
Article
Polymer Science
Dejene Assefa Anito, Tian-Xiong Wang, Hai-Peng Liang, Xuesong Ding, Bao-Hang Han
Summary: The transformation of organic molecules into compounds of interest by the utilization of solar energy is an innovative approach that is attracting a lot of attention from material scientists. Introducing potent chelation sites onto a porous matrix is imperative for effectively recycling cost-prohibitive catalysts.
Review
Pharmacology & Pharmacy
Aviva Levina, Debbie C. Crans, Peter A. Lay
Summary: Injections of highly cytotoxic or immunomodulating drugs directly into inoperable tumors is a growing clinical procedure that utilizes established Pt-based drugs. This method is advantageous for unstable anticancer metal complexes that cannot be administered intravenously. The injected hydrophobic metal-containing complexes are quickly taken up by cancer cells, causing cell death, while their non-toxic decomposition products have low systemic toxicity when released into the bloodstream.
Article
Biochemistry & Molecular Biology
Aviva Levina, Anthony R. M. Chetcuti, Peter A. Lay
Summary: Ruthenium complexes are important in the development of metal-based anticancer drugs. This study investigates the interactions of the anticancer drugs KP1019 and [Ru-III(nta)(2)](3-) with transferrin in biological media and their cellular uptake in human hepatoma cells. The results show that the mode of transferrin binding and cellular uptake of ruthenium depend on the nature of the ruthenium complex and the availability of iron binding sites on transferrin, as well as the presence of competing proteins.
Article
Chemistry, Multidisciplinary
Kateryna Kostenkova, Aviva Levina, Drew A. Walters, Heide A. Murakami, Peter A. Lay, Debbie C. Crans
Summary: Two new series of complexes with pyridine-containing Schiff bases were synthesized and their chemical properties and stability were studied. One of the complexes exhibited good anti-proliferative activity in cell culture media, showing high selectivity towards glioblastoma cells and potential for drug treatment.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Multidisciplinary
Serene Kuramarohit, Andria M. Yaourtis, Annie Nguyen, Michelle L. Wood, Aviva Levina, Peter A. Lay
Summary: Using IncuCyte Zoom imaging proliferation assays, it was observed that treatment with sub-toxic doses of [GaQ(3)] caused morphological changes and inhibition of cell migration in triple-negative human breast cancer cells. The addition of a trace amount of Cu(II) dramatically increased the cytotoxicity of [GaQ(3)]. The findings suggest the potential use of metal complexes in cancer therapy and the importance of ligand binding of essential metal ions for their cytotoxicity.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Inorganic & Nuclear
Aviva Levina, Canan Uslan, Heide Murakami, Debbie C. Crans, Peter A. Lay
Summary: Limited stability of transition-metal complexes in biological media has hindered their medicinal applications but also created potential for novel cancer treatments. This study found that two V(V) complexes decomposed in cell culture medium, but still showed high antiproliferative activities in breast cancer cells, with different mechanisms of action. Complex 1 is a suitable candidate for further development as an anticancer drug delivered via intratumoral injections.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Kartika Wardhani, Aviva Levina, Biyun Sun, Georges E. R. Grau, F. Richard Keene, J. Grant Collins, Peter A. Lay
Summary: Using a new photoluminescent polypyridylruthenium(II) stain, researchers have uncovered previously unknown interactions between extracellular vesicles (EVs) released from lipopolysaccharide-stimulated THP-1 monocytes and the blood-brain barrier (BBB). These findings shed light on the impact of bacteria-induced immune response on BBB and provide insights into human brain diseases.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Inorganic & Nuclear
Liam J. J. Stephens, Elena Dallerba, Jenisi T. A. Kelderman, Aviva Levina, Melissa V. V. Werrett, Peter A. A. Lay, Massimiliano Massi, Philip C. C. Andrews
Summary: This study synthesized and characterized twelve Re(i) tricarbonyl diimine complexes with thiotetrazolato ligands. The tetrazolato ligand can bind to the Re(i) center through either the S atom or the N atom, with most complexes being bound to the N atom. In solution, the complexes exist as an equilibrating mixture of linkage isomers. The complexes exhibit photoluminescent properties, with emission wavelengths dependent on the nature of the diimine ligand.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Multidisciplinary
Serene Kuramarohit, Andria M. Yaourtis, Annie Nguyen, Michelle L. Wood, Aviva Levina, Peter A. Lay
Summary: This study demonstrates the potential use of a metal complex, GaQ(3), in differentiation anti-cancer therapy. It also shows that the cytotoxicity of GaQ(3) is strongly linked to the binding of essential metal ions, such as Cu(II), in the medium. These findings suggest that appropriate delivery mechanisms of such complexes and their ligands could lead to a powerful new approach for cancer chemotherapy.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Polymer Science
Aviva Levina, Boer Wang, Peter A. Lay
Summary: Transferrin (Tf) plays a crucial role in transporting Fe(III) into cells, but its biological function in binding and delivering other metal ions remains controversial. This study investigated the effect of non-Fe(III) metal ion binding on the conformation of Tf using urea-polyacrylamide gel electrophoresis (urea-PAGE). The results showed that metal ions like In(III), V(III), and Cr(III) caused a closed Tf conformation similar to Fe(III)-Tf, while Ga(III) and V(IV) did not. Only In(III) increased the proportion of closed Tf conformation in whole serum. These findings suggest that Tf may not act as a natural carrier for metal ions other than Fe(III), but it can bind exogenous metal ions in serum and prevent their entry into cells, reducing their toxicity.
Review
Chemistry, Multidisciplinary
Dan He, Yawen Li, Fuwen Zhao, Yuze Lin
Summary: High trap density in organic solar cells leads to localized charge carriers and reduced carrier lifetime, limiting device efficiency. This feature article summarizes the recent advances of trap suppression by material design and device engineering.
CHEMICAL COMMUNICATIONS
(2024)
Review
Chemistry, Multidisciplinary
Olivier Monfort, Arshitha Madhusudhan, Martin Motola
Summary: This article presents the advantages of coupling photocatalysis and Fenton-based processes for environmental remediation and discusses their synergy. It critically examines the simultaneous triggering of these two processes and provides insights into research approaches. The study aims to enhance understanding of this complex process and highlight the potential integration of new catalysts in current wastewater treatment technology.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Manideepa Dhar, Chittaranjan Mishra, Avijit Das, Uttam Manna
Summary: An approach of 'polymerization of monomers in its aggregated form' has been introduced to tailor the water wettability of fibrous and porous substrates, achieving hydrophobicity to superhydrophobicity transition, as well as patterned wettability. This facile chemical method provides a durable coating with adjustable and patterned wettability for various potential applications.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Saswat Ranjan Bhoi, Chhanda Debnath, Shikha Gandhi
Summary: In this article, a novel catalytic reaction using Pd(0) and Bronsted acid is reported for the synthesis of biologically important imidazolidinone-fused N-heterocycles through redox-neutral intramolecular N-allylation of indoles and pyrroles with alkynes. This atom-economical method is applicable to a wide range of substrates and eliminates the need for leaving groups or oxidizing agents commonly used in traditional allylation reactions.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Longkun Chen, Mingshuai Zhang, Meichen Liu, Zhuoyuan Liu, Yuetong Qiu, Zhilai Zhang, Fuchao Yu, Jiuzhong Huang
Summary: In this study, an efficient Rh(III)-catalyzed selective mono- and dual-C-H bond functionalization/cyclization with iodonium ylide as the sole coupling partner was demonstrated. Fused benzodiazepine skeletons were obtained in excellent yields, providing an improved approach to dual C-H unsymmetrical functionalization.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Alice Kennett, Sven Epple, Gabriella van der Valk, Irene Georgiou, Evelyne Gout, Romain R. Vives, Angela J. Russell
Summary: This study presents the design and synthesis of sulfated disaccharide inhibitors based on IdoA(2S)-GlcNS(6S), which showed potent inhibition of Sulf-2. The results suggest that IdoA(2S)-GlcNS(6S) is the shortest fragment size required for effective inhibition of Sulfs, and a trisulfated disaccharide is identified as the minimal fragment size of heparan sulfate for effective endosulfatase inhibition.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Mauro Garbini, Andrea Brunetti, Riccardo Pedrazzani, Magda Monari, Massimo Marcaccio, Giulio Bertuzzi, Marco Bandini
Summary: The self-adaptability of galvanostatic electrolysis was found to be helpful in a multistage chemo- and diastereoselective electrochemically promoted cyclodimerization of chalcones. Through a series of reductive events, densely functionalized cyclopentanes with five contiguous stereocenters were obtained (25 examples, yields up to 95%, dr values up to >20:1). Further experimental and electrochemical investigations indicated the crucial role of dynamic kinetic resolution of the aldol intermediate in the reaction mechanism.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Dhananjay S. Nipate, Neha Meena, Prakash N. Swami, Krishnan Rangan, Anil Kumar
Summary: In this study, the synthesis of functionalized benzo[a]phenazines and indazolo[2,3-a]quinolines was achieved through Rh(III)-catalyzed oxidative annulation of 2-arylquinoxalines and 2-aryl-2H-indazoles with allyl alcohols. The method showed a wide substrate scope, excellent functional group tolerance, good to high yields of annulated products, and the capability for scaled-up synthesis. A tentative mechanism of the annulation reaction was proposed based on a preliminary mechanistic investigation.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Ruonan Zhang, Abudukadi Tudi, Xia Yang, Xuping Wang, Zhihua Yang, Shujuan Han, Shilie Pan
Summary: A new lead tellurium borate material with a unique fundamental building block [B4O10] was synthesized and found to exhibit high birefringence. The structure-property relationship was discussed using first-principles calculations.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Amresh Kumar Singh, Baishali Thakurta, Anupam Giri, Monalisa Pal
Summary: This study introduces three key concepts for the quick synthesis of large-scale high-quality 2D materials films and their utilization in device fabrication.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Multidisciplinary
Reina Hagiwara, Shun Nishimura, Kosuke Okeyoshi
Summary: A copolymer-conjugated nanocatalytic system has been developed to improve electron transfer and enhance photoinduced H2 generation.
CHEMICAL COMMUNICATIONS
(2024)