Article
Chemistry, Physical
Carlos Lizandara-Pueyo, Xinyuan Fan, Carles Ayats, Miquel A. Pericas
Summary: This study involved the controlled synthesis of calcium carbonate particles surface-functionalized with azido groups, followed by copper-catalyzed alkyne-azide cycloaddition reactions to prepare novel catalytic materials. The immobilized catalyst demonstrated high selectivity and efficiency in catalyzing Michael addition reactions of aldehydes, with the added advantage of being reusable and adaptable to continuous-flow operation for increased productivity.
JOURNAL OF CATALYSIS
(2021)
Article
Plant Sciences
Carlos de Tomas, Carlos M. Vicient
Summary: Endogenous pararetroviruses (EPRVs), derived from DNA viruses of the family Caulimoviridae, are viral sequences integrated into plant genomes. This study analyzed a large number of plant genome sequences and identified 57 clusters and 13 genera of EPRVs, including a newly proposed genus called Wendovirus. There are significant differences in the abundance and distribution of EPRVs between different plant families and genera, with florendoviruses being the most abundant and widespread.
FRONTIERS IN PLANT SCIENCE
(2022)
Article
Virology
Jerry Joe E. K. Harrison, Steve Tuske, Kalyan Das, Francesc X. Ruiz, Joseph D. Bauman, Paul L. Boyer, Jeffrey J. DeStefano, Stephen H. Hughes, Eddy Arnold
Summary: The crystal structure of mature PR-RT from prototype FV shows that it can carry out protein processing and reverse transcription, but is not competent for enzyme activity. PFV PR-RT is monomeric and shares structural similarities with HIV-1 PR subunits, although it is in a configuration not suitable for enzymatic activity.
Article
Chemistry, Organic
Esra Dundar, Cihangir Tanyeli
Summary: A series of chiral bifunctional squaramide organocatalysts were evaluated for their application in Friedel-Crafts alkylation of indoles, showing high enantioselectivity and moderate yields. This new asymmetric transformation provides a simple, efficient, clean, and environmentally friendly route for chemical synthesis.
TETRAHEDRON LETTERS
(2021)
Article
Chemistry, Multidisciplinary
Yongbing Liu, Huanlin Diao, Guorong Hong, Jonathan Edward, Tao Zhang, Guoqiang Yang, Bin-Miao Yang, Yu Zhao
Summary: We have developed an enantioconvergent approach to chiral N-heterocycles using racemic diols and primary amines via cost-effective borrowing hydrogen annulation. The discovery of a chiral amine-derived iridacycle catalyst was crucial for achieving high efficiency and enantioselectivity in the one-step formation of two C-N bonds. This catalytic method provides quick access to a diverse range of enantioenriched pyrrolidines, including key precursors for valuable drugs like aticaprant and MSC 2530818.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Organic
Yang-Guang Chen, Ying Hu, Jia-Yi Liu, Ming-Sheng Xie, Hai-Ming Guo
Summary: A catalytic strategy for accessing P-stereogenic phosphinates through acylative desymmetrization of bisphenols catalyzed by chiral 4-arylpyridine-N-oxide has been reported. The process achieved high yields and enantioselectivities, leading to the synthesis of a series of chiral phosphorus compounds containing carboxylic acid drug molecules.
ORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Biochemistry & Molecular Biology
Thomas W. Kirby, Scott A. Gabel, Eugene F. Derose, Lalith Perera, Juno M. Krahn, Lars C. Pedersen, Robert E. London
Summary: This study aims to identify small molecule ligands that can interfere with the formation of active HIV-1 reverse transcriptase (RT) by understanding its maturation process. The isolated polymerase domain p51 was utilized and ligands at subdomain interfaces were identified using computational analysis and experimental techniques, with their interactions further characterized. This study provides insight into the reverse transcription process of the virus and potential new drug targets.
Article
Biochemistry & Molecular Biology
Javier Martinez del Rio, Nerea Lopez-Carrobles, Jesus I. Mendieta-Moreno, Oscar Herrera-Chacon, Adrian Sanchez-Ibanez, Jesus Mendieta, Luis Menendez-Arias
Summary: The combination of PCR and RTs has been widely used in RNA detection and gene expression analysis. Improving thermostability and nucleic acid binding affinity of RTs is crucial for enhancing the efficiency of these applications. This study investigated the effects of amino acid substitutions in the RT RNase H domain on its properties. It was found that specific substitutions resulted in loss of activity and mutations that improved cDNA synthesis efficiency also affected RNase H activity. This discovery provides evidence for a novel mechanism of RNase H inactivation.
JOURNAL OF MOLECULAR BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Igor P. Oscorbin, Maxim L. Filipenko
Summary: Reverse transcriptases (RTs) are crucial enzymes used in modern biotechnology and molecular diagnostics, with M-MuLV RT being the most commonly used one. Improvements in M-MuLV RT can enhance its practical utility for a wide range of applications.
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL
(2021)
Article
Biology
Igor P. Oscorbin, Lidiya M. Novikova, Maxim L. Filipenko
Summary: Reverse transcriptases (RTs) are crucial enzymes used in RNA-related studies. However, the performance of different RTs in reverse-transcription loop-mediated isothermal amplification (RT-LAMP) is not well-studied. This study compared various M-MuLV RTs in RT-LAMP and found that mutated enzymes performed better overall but were more sensitive to high concentrations of NaCl. These findings are important for developing novel LAMP-based diagnostic tests.
Article
Microbiology
Ming-Tain Lai, Meizhen Feng, Min Xu, Winnie Ngo, Tracy L. Diamond, Carey Hwang, Jay A. Grobler, Daria J. Hazuda, Ernest Asante-Appiah
Summary: The combination of DOR and ISL shows a high resistance barrier against HIV-1 infection. DOR/ISL exhibits strong antiviral activity and no resistance to other drugs.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Chemistry, Organic
Katsuhiko Moriyama, Masako Kuramochi, Seiji Tsuzuki, Kozo Fujii, Takeshi Morita
Summary: This study developed a novel nitroxyl-catalyzed bromoesterification of alkenes and achieved diastereoselective bromohydroxylation.
Article
Chemistry, Organic
Sarah A. Cronin, Stephen J. Connon
Summary: This study introduces a novel approach to catalytic, alcoholytic kinetic resolution of oxazinones using a stereochemically dense cinchona alkaloid-based catalyst. The catalyst enables highly enantiodiscriminatory ring-opening of oxazinones equipped with electrophilic aryl units, leading to the generation of orthogonally protected beta-amino acids for the first time.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Satavisha Kayal, Jun Kikuchi, Naoya Shinagawa, Shigenobu Umemiya, Masahiro Terada
Summary: This study achieved a highly efficient and enantioselective reaction through the use of a co-catalyst system, resulting in enantioenriched compounds and the recovery of the starting material. It provides a new synthetic method for the synthesis of multifunctional compounds.
Article
Biochemical Research Methods
Thomas Leichtfried, Helga Reisenzein, Siegrid Steinkellner, Richard A. Gottsberger
Summary: The study found that slight modifications of the reverse transcription step in the real-time PCR assay can significantly improve the detection limit, especially for certain plant viruses. This discovery could enhance the sensitivity in detecting viroids and benefit regulatory outcomes for national plant protection organizations.
JOURNAL OF VIROLOGICAL METHODS
(2021)
Article
Biochemistry & Molecular Biology
Dongdong Zhang, Yujiao Liu, Ziyi Luo, Yanling Chen, Anjie Xu, Yuxing Liang, Balu Wu, Xiqin Tong, Xiaoyan Liu, Hui Shen, Li Liu, Yongchang Wei, Haibing Zhou, Yi Liu, Fuling Zhou
FREE RADICAL BIOLOGY AND MEDICINE
(2020)
Article
Cell Biology
Pan Huang, Nan Zheng, Hai-bing Zhou, Jian Huang
MOLECULAR AND CELLULAR BIOCHEMISTRY
(2020)
Article
Oncology
Lijie Zhao, Xin Han, Jianfeng Lu, Donna McEachern, Shaomeng Wang
Article
Biochemistry & Molecular Biology
Wei Wang, Yuzhi Lu, Enhui Chen, Kang Shen, Jun Li
Summary: A series of imidazo [1,2-a] pyridines designed from gossypol modification based on Groebke-Blackburn-Bienayme reaction were discovered as potent Bcl-2 inhibitors, showing good anti-proliferative activities for 7 human cancer cell lines. Compound 4 demonstrated the ability to suppress antiapoptotic proteins Bcl-2 and Bcl-X-L, with a possible binding model illustrated by molecular modeling.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Weiguo Xiang, Lijie Zhao, Xin Han, Chong Qin, Bukeyan Miao, Donna McEachern, Yu Wang, Hoda Metwally, Paul D. Kirchhoff, Lu Wang, Aleksas Matvekas, Miao He, Bo Wen, Duxin Sun, Shaomeng Wang
Summary: This study identifies a promising AR degrader for the treatment of advanced prostate cancer, which demonstrates potent inhibition in cell lines with AR gene amplification or mutations and shows good oral bioavailability in mice.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Xin Han, Lijie Zhao, Weiguo Xiang, Chong Qin, Bukeyan Miao, Donna McEachern, Yu Wang, Hoda Metwally, Lu Wang, Aleksas Matvekas, Bo Wen, Duxin Sun, Shaomeng Wang
Summary: This study outlines strategies for discovering highly potent PROTAC degraders of androgen receptor (AR) with excellent oral pharmacokinetics, successfully identifying compound ARD-2128 as the most effective in inhibiting tumor growth in mice with good oral bioavailability.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Xufang Chen, Dan Li, Yang Li, Weiting Zhan, Chao Huang, Rongsheng Chen, Wei Wang, Hongwei Ni, Paul K. Chu
Summary: A short-brush NiFeOxHy film with an edge-abundant, subcrystalline, and Ni3+-rich structure was designed and prepared on a Ni foam with a trace amount of Pt introduced to enhance water electrolysis performance. The short-brush NiFeOxHy film exhibited better OER activity than conventional nanosheets, while the Pt-modified materials showed effective HER catalytical activity. The alkaline electrolyzer composed of these electrodes required only 1.54 V to achieve a current density of 10 mA cm(-2).
APPLIED SURFACE SCIENCE
(2022)
Article
Chemistry, Multidisciplinary
Wei Wang, Yuzhi Lu, Juncheng Ge, Niya Liu
Summary: This study presents a practical and scalable route for the synthesis of 1,1'-dideoxygossypol from natural polyphenol product gossypol. The key steps involve regioselective deacetylation and reductive removal of hydroxyl groups. The study demonstrates that hydroxyl groups are not necessary for antitumor activities and that 1,1'-dideoxygossypol has improved aqueous solubility compared to gossypol.
Review
Medicine, Research & Experimental
Xiaojuan Jia, Xin Han
Summary: Inhibition of androgen receptor (AR) has been extensively studied for treating prostate cancer, but resistance mechanisms limit its efficacy. Small-molecule PROTAC AR degraders have emerged as a new therapeutic strategy to overcome resistance mechanisms. In the last two decades, potent PROTAC AR degraders have shown promising results in preclinical and clinical trials, with ARV-110 demonstrating good clinical effects in patients with mCRPC. This highlights the high clinical value of PROTAC strategy in treating human diseases. This review summarizes the recent advances in the development of potential clinical-stage PROTAC AR degraders.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Biochemistry & Molecular Biology
Kexin Wang, Qiuzi Li, Yufeng Fan, Pingping Fang, Haibing Zhou, Jian Huang
Summary: Abnormal glycometabolism has become a fundamental research topic in tumor biology due to the poor metabolic conditions promoting the emergence of the Warburg effect (WE) phenotype. This study investigated the potential of Oxabicycloheptene sulfonate (OBHS), a selective estrogen receptor modulator, in targeting breast cancer glycometabolism. The results revealed that OBHS inhibits the expression of glucose transporter 1 (GLUT1) via the PI3K/Akt signaling pathway, leading to the suppression of breast cancer progression and proliferation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Xin Han, Lijie Zhao, Weiguo Xiang, Bukeyan Miao, Chong Qin, Mi Wang, Tianfeng Xu, Donna McEachern, Jianfeng Lu, Yu Wang, Hoda Metwally, Chao-Yie Yang, Paul D. D. Kirchhoff, Lu Wang, Aleksas Matvekas, John Takyi-Williams, Bo Wen, Duxin Sun, Mark Ator, Robert Mckean, Shaomeng Wang
Summary: We report the discovery of ARD-2051, a highly potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 demonstrates strong AR protein degradation activity and effectively suppresses AR-regulated genes in prostate cancer cell lines. It shows good oral bioavailability and pharmacokinetic profile in animal models. In addition, ARD-2051 inhibits tumor growth and exhibits no signs of toxicity in mice, making it a promising therapeutic option for AR+ human cancers.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Xin Han, Yi Sun
Summary: This review focuses on the discovery and development of orally available anti-cancer PROTAC degraders, summarizing the strategies applied to this end, which may provide a reference for the future discovery of new oral-available PROTAC degraders for the treatment of various human diseases.
CELL REPORTS PHYSICAL SCIENCE
(2022)
Article
Chemistry, Analytical
Qiuyu Meng, Xiaoyu Ma, Baohua Xie, Xiaofei Deng, Jian Huang, Hai-Bing Zhou, Chune Dong
Article
Chemistry, Multidisciplinary
Qiuyu Meng, Baohua Xie, Xiaoyu Ma, Zhiye Hu, Fuling Zhou, Hai-Bing Zhou, Chune Dong
CHEMICAL COMMUNICATIONS
(2020)
Article
Oncology
Jun Wu, Jing Yan, Pingping Fang, Hai-Bing Zhou, Kaiwei Liang, Jian Huang
Article
Chemistry, Organic
Faiza Diaba, Gisela Trenchs
Summary: The first violet light-mediated synthesis of gamma- and delta-lactams from N-alkenyl trichloroacetamides is reported in this paper. The reactions are conducted in tetrahydrofuran or 2-methyltetrahydrofuran as the sole solvent without catalysts or additives, under non-anhydrous conditions in an air atmosphere where the solvent serves as the radical initiator.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Feroze Hussain, Sajjad Ahmed, Ashiq Hussain Padder, Qazi Naveed Ahmed
Summary: This study reports a novel and efficient one-pot synthesis method for mixed phosphorotrithioates, which does not require supplementary additives and shows broad applicability.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Hyunjin Oh, Ikyon Kim
Summary: A new 1,2,4-triazole-pyrrolo[1,2-a]pyrazine hybrid system, 6-acylpyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, was synthesized using a catalyst-free method. This method involved sequential exposure of pyrrole-2-carbonitrile-derived substrates to DMF-DMA and acyl hydrazide, resulting in the formation of acylated pyrazine and 1,2,4-triazole rings, enabling the installation of various substituents at specific positions on the core skeleton.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Ming Yan, Si-fan Wang, Yong-po Zhang, Jin-zhong Zhao, Zhuo Tang, Guang-xun Li
Summary: Here we developed an efficient photocatalytic approach for the convenient preparation of sulfinamides. The reaction allows for the gram-scale preparation of sulfinamides and the one-pot synthesis of various sulfonyl amides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Farzaneh Bandehali-Naeini, Zahra Tanbakouchian, Noushin Farajinia-Lehi, Nicolas Mayer, Morteza Shiri, Martin Breugst
Summary: Two tandem catalytic systems were developed for the synthesis of novel 3,4-disubstituted maleimides using the same Ugi adducts. Different maleimide structures can be synthesized using either Pd or Cu catalysis.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Article
Chemistry, Organic
Tanya Raghava, Anjan Chattopadhyay, Subhadeep Banerjee, Nivedita Sarkar
Summary: Amine substitution of two ortho fluorine atoms of tetrafluoroterephthalonitrile through SNAr chemistry is easily achievable. But further fluorine substitution is only possible under forcing conditions, yielding valuable fluorophores for bioimaging.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)
Review
Chemistry, Organic
Anju Chadha, Santosh Kumar Padhi, Selvaraj Stella, Sowmyalakshmi Venkataraman, Thangavelu Saravanan
Summary: Alcohol dehydrogenases are enzymes that use cofactors for oxidation or reduction reactions of alcohols or carbonyl compounds. They are utilized in green chemistry and have applications in the production of pharmaceuticals. Recombinant enzymes have solved the challenge of producing purified enzymes in large quantities. Engineered alcohol dehydrogenases have been used in asymmetric synthesis in industry. Various methods have been established for regenerating expensive cofactors to make the enzymatic process more efficient and economically viable.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2024)