Article
Chemistry, Multidisciplinary
Douglas A. Rose, Joseph W. Treacy, Zhongyue J. Yang, Jeong Hoon Ko, K. N. Houk, Heather D. Maynard
Summary: This article describes a new class of traceless linkers based on ortho- or para-hydroxybenzylamines, which can modulate the release rate by introducing electron-donating substituents. The optimization of linker design was carried out with mechanistic insights and computational calculations, resulting in the development of a faster self-immolative linker. These traceless linkers showed effectiveness for reversible bioconjugation applications.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Medicinal
Yingge Wang, Moran Sun, Yuyang Wang, Jinling Qin, Yixin Zhang, Yingyue Pang, Yongfang Yao, Hua Yang, Yongtao Duan
Summary: A novel series of compounds designed as tubulin/HDAC dual-targeting inhibitors demonstrated potent anti-proliferative activities against human cancer cell lines, while also inhibiting tubulin polymerization and specific HDAC activity. These compounds were found to act through various cellular mechanisms to achieve anti-tumor and anti-angiogenic effects.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Hongyan Yang, Lan Wang, Libo Yuan, Heng Du, Boyuan Pan, Kui Lu
Summary: In this study, a series of hybrid peptides were designed by connecting an antimicrobial peptide Ce(1-8) with a lipopolysaccharide-targeting peptide Lf(28-34) via different linkers. The results showed that the linkers played a crucial role in the antimicrobial activity of the hybrid peptides against Gram-negative bacteria. Among these hybrid peptides, peptide CL5 with a dipeptide rigid linker exhibited excellent activity and selectivity against Gram-negative bacteria. It was found that the interaction of the peptides with LPS was crucial for their antimicrobial activity. Mechanistic studies revealed that peptide CL5 disrupted the integrity of bacterial membranes, leading to the death of Gram-negative bacterial cells. This study highlights the importance of linker selection in the design of hybrid peptides and provides a foundation for the development of antimicrobial peptides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Matt Timmers, Wouter Peeters, Niels J. Hauwert, Cristianne J. F. Rijcken, Tina Vermonden, Ingrid Dijkgraaf, Rob M. J. Liskamp
Summary: The site-specific attachment of the reactive TMTHSI-click handle to the N-terminus of peptides and proteins is described in this article. The resulting constructs can be used in strain-promoted azide alkyne cycloaddition for reaction with azide-containing proteins. The article also discusses the N-terminal specific attachment of the reactive TMTHSI-click handle to peptides and proteins, followed by strain-promoted cycloaddition with azide-containing peptides, proteins, nucleic acids, or other azide compounds.
CHEMICAL COMMUNICATIONS
(2023)
Review
Oncology
Claudia Ollauri-Ibanez, Itziar Astigarraga
Summary: Cancer is a major cause of death in children, and targeting angiogenesis as a strategy for cancer treatment has shown mixed clinical benefits. Due to the rarity and heterogeneity of pediatric cancers, studies on antiangiogenic drugs often involve a small number of patients and further research is necessary.
Article
Chemistry, Analytical
Ying Chen, Bin Liu, Zhengbo Chen, Xia Zuo
Summary: Enrichment techniques for phosphopeptides often involve interactions between phosphate groups and metal ions or metal oxides. In this study, an electrochemical sensor based on TiO2 NPs was designed to detect phosphopeptides in protein samples pretreated with AuNPs, showing high sensitivity and a wide linear concentration range. Additionally, TiO2 and GO composite materials were synthesized to enhance the detection capability, with the uniformly dispersed anatase crystal TiO2 and GO composite-modified electrode exhibiting a lower detection limit.
ANALYTICAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Alfredo Cruz-Gregorio, Ana Karina Aranda-Rivera, Edda Sciutto, Gladis Fragoso, Jose Pedraza-Chaverri
Summary: Cancer is the fourth leading cause of death worldwide, and although cancer mortality has decreased in recent years, some forms of cancer are resistant to immunotherapies. Antitumor and immunomodulatory peptides are a promising approach due to their ability to activate immune cells and have fewer side effects. The regulation of the redox state, which has been poorly studied, plays a crucial role in the immune system's response to these peptides. This review focuses on understanding the redox state regulated by these peptides in cancer development and its potential as a therapy.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
(2022)
Article
Chemistry, Multidisciplinary
Wenyi Li, Feng Lin, Andrew Hung, Anders Barlow, Marc-Antoine Sani, Rita Paolini, William Singleton, James Holden, Mohammed Akhter Hossain, Frances Separovic, Neil M. O'Brien-Simpson, John D. Wade
Summary: Antimicrobial peptides (AMPs) are effective against drug-resistant bacteria and possess immunomodulatory activity. Dimerization of AMPs using bifunctional tethers enhances their antimicrobial activity, especially against multidrug-resistant bacteria.
Article
Biophysics
Wu Di, Yang Shuai, Wang Bo, Tan Wei, Jinpeng He, Guowen Qian, Youwen Deng
Summary: The study focuses on the preparation of PLLA/SBA15NH2-ZOL scaffold via selective laser sintering technology, which can address the challenges of bone defect and tumor recurrence in postoperative treatment of bone tumors. The scaffold has the ability of local release of zoledronate (ZOL) to inhibit osteosarcoma cell proliferation and induce osteoclast differentiation through competitive binding of RANK.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Chemistry, Multidisciplinary
Dmytro Honcharenko, Kristina Druceikaite, Malgorzata Honcharenko, Martin Bollmark, Ulf Tedebark, Roger Stromberg
Summary: The report describes a simplified methodology for multiple labeling of oligonucleotides on a solid support, utilizing novel linkers with orthogonal functionalities to allow for attachment of varied moieties. The versatility of the approach is demonstrated through synthesis of oligonucleotide multiconjugates with different functional entities.
Review
Pharmacology & Pharmacy
Ting Xu, Zhen-Hao Li, Ting Liu, Cai-Hong Jiang, Ya-Juan Zhang, Hui Li, Ying Jiang, Juan Zhao, Wen-Jing Guo, Jia-Yuan Guo, Lu Wang, Jia-Xuan Li, Jing Shen, Gao-Wa Jin, Ze-Wei Zhang, Quan-Fu Li
Summary: In recent years, more attention has been paid to the dynamic changes in skeletal muscles during antitumor drug therapy. These changes focus on the increasing or decreasing levels of skeletal muscles during or at the end of the entire treatment course.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Polymer Science
Antonela Gallastegui, Maria Emilia Zambroni, Carlos A. Chesta, Rodrigo E. Palacios, Maria Lorena Gomez
Summary: The research focused on developing novel water-soluble eco-friendly hybrid photoinitiator systems, which showed higher polymerization rates and versatility in photopolymerization applications.
Article
Chemistry, Organic
Ayumi Uchino, Chihiro Tsukano, Tsuneo Imamoto, Kazuhiro Irie
Summary: Two new alkyl bridged-tris-alpha-amino acids with Fmoc protecting groups have been designed and synthesized as new flexible linkers for trimer models, providing an alternative approach to mimic trimers with higher flexibility than reported options.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Biochemical Research Methods
Jared T. Miller, Caitlin N. Vitro, Siteng Fang, Samantha R. Benjamin, L. Nathan Tumey
Summary: The study found that novel linkers (AsnAsn) have better stability and efficacy, enhancing drug delivery applications for ADCs and SMDCs.
BIOCONJUGATE CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Himalaya Singh, Annaram Thirupathi, Bishwaprava Das, Manojkumar Janni, Renu Kumari, Sandeep Singh, Mamunur Rashid, Mohammad Wahajuddin, Musuvathi Motilal Balamurali, Kumaravelu Jagavelu, Saravanan Peruncheralathan
Summary: The study demonstrates that 2,3-ACBTs inhibit angiogenesis by regulating the Akt/Src signaling pathway and disrupting cytoskeletal filaments of endothelial cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)