Article
Agriculture, Multidisciplinary
Zhiqiang Lu, Xiaomeng Xu, Dongmei Li, Na Sun, Songyi Lin
Summary: The study demonstrated that sea cucumber peptides can prevent memory impairment by increasing the acetylation level of histones and affecting memory-related pathways. This neuroprotective effect is achieved through regulating post-transcriptional hippocampal protein acetylation.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Francisco Ramos-Martin, Claudia Herrera-Leon, Viviane Antonietti, Pascal Sonnet, Catherine Sarazin, Nicola D'Amelio
Summary: K11 is a synthetic peptide that shows potential for excellent antibacterial properties, selectively destabilizing bacterial biomimetic membranes and torqueing the surface of their bilayers. This may indicate additional biological activities.
Article
Chemistry, Multidisciplinary
Peng Chen, Jie Sun, Chengjun Zhu, Guanghui Tang, Wei Wang, Manyi Xu, Menghua Xiang, Chong-Jing Zhang, Zhi-Min Zhang, Liqian Gao, Shao Q. Yao
Summary: This study presents a general approach to develop cell-active covalent inhibitors of protein kinases by targeting the conserved catalytic lysine residue using key SuFEx and salicylaldehyde-based imine chemistries. The strategy was validated by successfully developing covalent inhibitors against BCR-ABL kinase, which showed high selectivity and potency. The salicylaldehyde-containing A5 compound is the first reversible covalent ABL inhibitor with prolonged residence time and minimal off-target effects.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Cell Biology
Michela Falco, Raffaella Meazza, Claudia Alicata, Paolo Canevali, Aura Muntasell, Cristina Bottino, Lorenzo Moretta, Daniela Pende, Miguel Lopez-Botet
Summary: This study characterized the specificity of an anti-KIR monoclonal antibody and identified the amino acids relevant for its recognition. The antibody exclusively reacted with KIR2DL1 and bound to a conformational epitope including M44, which is crucial for HLA-C K80 recognition by KIR2DL1. The findings of this study provide valuable information for further understanding the specificity of the antibody and its reactivity.
Article
Oncology
Xiaoqiang Chai, Jianfei Guo, Ruizhao Dong, Xuan Yang, Chao Deng, Chuanyuan Wei, JiaJie Xu, Weiyu Han, Jiacheng Lu, Chao Gao, Dongmei Gao, Cheng Huang, Aiwu Ke, Shuangqi Li, Huanping Li, Yingming Tian, Zhongkai Gu, Shuxian Liu, Hang Liu, Qilong Chen, Feng Liu, Jian Zhou, Jia Fan, Guoming Shi, Feizhen Wu, Jiabin Cai
Summary: This study characterized the role of lysine acetylation in hepatocellular carcinoma, revealing multiple acetylation sites and their changes in different tissues. The study also found a correlation between acetylation levels and prognosis in HCC patients.
CLINICAL AND TRANSLATIONAL MEDICINE
(2021)
Article
Chemistry, Multidisciplinary
Fanny Laporte, Yves Chenavier, Alexandra Botz, Christelle Gateau, Colette Lebrun, Sarah Hostachy, Claude Vidaud, Pascale Delangle
Summary: This study proposes a simple and efficient fluorescence-based method to assess the affinity of proteins and peptides for uranyl, providing a reliable and reproducible assessment for understanding the toxicity of this cation and developing decorporation strategies.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Biochemistry & Molecular Biology
Yu Imai, Glenn Hauk, Jeffrey Quigley, Libang Liang, Sangkeun Son, Meghan Ghiglieri, Michael F. Gates, Madeleine Morrissette, Negar Shahsavari, Samantha Niles, Donna Baldisseri, Chandrashekhar Honrao, Xiaoyu Ma, Jason J. Guo, James M. Berger, Kim Lewis
Summary: The antimicrobial resistance crisis necessitates the development of new antibiotics. In this study, a novel antimicrobial compound called evybactin was discovered from Photorhabdus noenieputensis, which exhibited potent and selective antibacterial activity against Mycobacterium tuberculosis. Evybactin was found to target DNA gyrase and utilized a promiscuous transporter, BacA, to enter the bacterial cell.
NATURE CHEMICAL BIOLOGY
(2022)
Article
Biology
Tanya R. McKitrick, Steffen M. Bernard, Alexander J. Noll, Bernard C. Collins, Christoffer K. Goth, Alyssa M. McQuillan, Jamie Heimburg-Molinaro, Brantley R. Herrin, Ian A. Wilson, Max D. Cooper, Richard D. Cummings
Summary: The novel lamprey antibody, O6, was developed to explore the expression of 3-O-sulfated galactose on glycoproteins in humans. The study revealed that O6 can identify various human tissues, consistent with the expression of corresponding sulotransferases (GAL3ST-2 and GAL3ST-3).
COMMUNICATIONS BIOLOGY
(2021)
Article
Chemistry, Medicinal
Guanghui Tang, Wei Wang, Xuan Wang, Ke Ding, SoFong Cam Ngan, Jiao-Yu Chen, Siu Kwan Sze, Liqian Gao, Peiyan Yuan, Xiaoyun Lu, Shao Q. Yao
Summary: This study describes the design and synthesis of a series of potential covalent inhibitors targeting EGFR's catalytically conserved lysine. Compound 26 showed excellent in vitro potency and selectivity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Lan Zhang, Yao Chen, Zhijia Li, Congcong Lin, Tongtong Zhang, Guan Wang
Summary: Histone methylation is a common and dynamic histone modification that regulates gene transcription by changing chromatin structure. Lysine demethylases play a vital role in maintaining epigenetic factors and are involved in various diseases, including cancer. Recent advancements have led to the discovery of inhibitors that disrupt lysine demethylation, particularly focusing on JmjC-domain-containing histone lysine demethylases (KDM2-7). This review discusses their structures, biological roles, representative inhibitors, and therapeutic potential, offering insights into the development of JmjC-KDM inhibitors.
DRUG DISCOVERY TODAY
(2023)
Article
Biochemistry & Molecular Biology
Tianfu Yu, Fengqi Zhou, Wei Tian, Ran Xu, Binbin Wang, Ailiang Zeng, Zhijun Zhou, Min Li, Yingyi Wang, Junxia Zhang
Summary: GBM, the most lethal primary brain tumor, contains a subpopulation of GSCs which are regulated by EZH2. The study found that EZH2 interacts with HP1BP3 to activate the expression of WNT7B, resulting in increased TMZ resistance and stemness in GBM cells. Inhibition of the WNT7B pathway can overcome TMZ resistance in GSCs.
Article
Multidisciplinary Sciences
Aditi Mukherjee, Zakir Hossain, Esteban Erben, Shuai Ma, Jun Yong Choi, Hee-Sook Kim
Summary: The study identifies a compound, JC-229, that selectively targets TbRPA1 in Trypanosoma brucei and inhibits its DNA binding activity. This compound has high toxicity to T. brucei cells but mild toxicity to human cells. The findings provide insights towards developing highly specific inhibitors for the treatment of African trypanosomiasis.
NATURE COMMUNICATIONS
(2023)
Article
Chemistry, Organic
Alok Shaurya, Graham A. E. Garnett, Melissa J. Starke, Mark C. Grasdal, Charlotte C. Dewar, Anton Y. Kliuchynskyi, Fraser Hof
Summary: The study reports an effective N,N-dimethyllysine (Kme2)-selective host and investigates its binding behavior in solution, as well as the relationship between its unusual conformational dynamics and guest-binding properties.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Health Care Sciences & Services
Chia-Hsiang Chen, Ailing Huang, Yu-Shu Huang, Ting-Hsuan Fang
Summary: Schizophrenia is a complex genetic disorder involving many common variants with modest effects and rare mutations with high penetrance. Identifying rare mutations associated with schizophrenia can help establish molecular diagnosis, elucidate pathogenesis, and provide genetic counseling.
JOURNAL OF PERSONALIZED MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Thomas Lohr, Kai Kohlho, Gabriella T. Heller, Carlo Camilloni, Michele Vendruscolo
Summary: The stabilization of native states of proteins is a powerful drug discovery strategy. This study reveals that a small molecule can stabilize the intrinsically disordered state of the A beta 42 peptide associated with Alzheimer's disease through a disordered binding mechanism. This mechanism involves both enthalpic gain from local interactions and entropic gain from global effects.
ACS CHEMICAL NEUROSCIENCE
(2022)
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)