Review
Neurosciences
Aziz Unnisa, Nigel H. H. Greig, Mohammad Amjad Kamal
Summary: Traumatic brain injury (TBI) is a major cause of death and morbidity, and is the focus of translational research. Apoptosis is important in the pathophysiology of TBI, and inhibiting it may improve functional recovery. Caspases, such as Caspase-3 and Caspase-9, are key mediators of cell death due to apoptosis in TBI. Understanding these apoptotic pathways and finding ways to inhibit Caspases may have significant treatment implications for TBI.
CURRENT NEUROPHARMACOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Tapas Ghosh, Shu Wang, Dharmendra Kashyap, Rohit G. Jadhav, Tanmay Rit, Hem Chandra Jha, Brian G. Cousins, Apurba K. Das
Summary: Self-assembled benzoselenadiazole (BSe)-capped tripeptide based nanofibrillar hydrogels have been developed that possess intrinsic anticancer and anti-inflammatory activities.
CHEMICAL COMMUNICATIONS
(2022)
Article
Pharmacology & Pharmacy
Zahra Madadi, Shiva Akbari-Birgani, Saeed Mohammadi, Mitra Khademy, Seyed Asadollah Mousavi
Summary: Neuroblastoma is a common malignant tumor in infants and young children, with differentiation-inducing potential. The activation of caspase-9 plays a crucial role in the differentiation process of human neuroblastoma cells, promoting a change in cell morphology and protein expression.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Nanoscience & Nanotechnology
Xiuli Zhang, Ruqing Gao, Huiyu Yan, Zijian Zhao, Jun Zhang, Weiming You
Summary: In this study, a BH3-mimic peptide was translated into a peptide-auric spheroidal nanocluster (BH3-AuNp), which improved its resistance to proteolysis and ability to penetrate cell membranes, leading to a significantly enhanced induction of apoptosis in cancer cells.
Review
Biochemistry & Molecular Biology
Jun-Hyuk Han, Jooho Park, Tae-Bong Kang, Kwang-Ho Lee
Summary: Initially classified as an apoptotic caspase, caspase-8 has now been found to play significant roles in regulating inflammatory processes. Recent research has shown its involvement in modulating inflammatory responses, inflammasome activation, cell death, and cytokine induction. This review summarizes the latest advances in understanding how caspase-8 impacts inflammatory reactions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Engineering, Biomedical
Han Yu, Shaoxing Yu, Hua Qiu, Peng Gao, Yingzhong Chen, Xin Zhao, Qiufen Tu, Minggang Zhou, Lin Cai, Nan Huang, Kaiqin Xiong, Zhilu Yang
Summary: The surface modification of extracorporeal circuits and indwelling medical devices using nitric oxide and antibacterial peptide can prevent thrombosis and infection, reducing clinical complications.
BIOACTIVE MATERIALS
(2021)
Review
Pharmacology & Pharmacy
Nicklas Osterlund, Sebastian K. T. S. Warmlander, Astrid Graslund
Summary: Cell-penetrating peptides (CPPs) derived from a prion protein (PrP) have exhibited disease-modifying properties against prion proteins and the amyloid-beta (A beta) peptide in Alzheimer's disease. These CPPs can interact with PrP/A beta and redirect their aggregation pathways, resulting in reduced cell-toxicity.
Article
Biochemistry & Molecular Biology
Xiaoman Ju, Dongmei Fan, Lingmei Kong, Qihong Yang, Yiying Zhu, Shaohua Zhang, Guifeng Su, Yan Li
Summary: Brevivin-1RL1, an AMP isolated from frog skin secretions, selectively inhibits tumor cells through induction of necrosis and caspase-dependent apoptosis. The peptide mainly targets the surface of cancer cells and could be considered as a potential candidate for the development of anti-cancer drugs.
Review
Pharmacology & Pharmacy
Maria I. Avrutsky, Carol M. Troy
Summary: Caspase-9, known for its role in apoptosis initiation, also plays a role in cellular differentiation, immune response, and mitochondrial function, and is linked to various diseases. Targeting supraphysiological Caspase-9 activation could be a viable approach for therapeutic interventions. However, there are still gaps in understanding the mechanistic implications of Caspase-9 in different pathologies.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Environmental Sciences
Mabrouk Attia Abd Eldaim, Eman Ragab Barakat, Mohamed Alkafafy, Samy Ahmed Abd Elaziz
Summary: The study assessed the preventive potential of silymarin against lead-induced hepatorenal toxicity in rats by modulating oxidative stress, lipid oxidation, pathological changes in liver and kidney tissues, improving the antioxidant defense system of the liver and kidneys, and reducing pro-apoptotic gene expression in liver tissue.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Ikumi Nakashima, Shoji Saito, Eiichi Akahoshi, Shigeki Yagyu, Mitsuko Sugano-Ishihara, Yozo Nakazawa
Summary: Breast cancer is a complex disease with unique molecular subtypes. The combination of tumor-tropic lipid nanoparticles and inducible caspase-9 mRNA shows promise as a potential treatment strategy for refractory breast cancer.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Genetics & Heredity
Shijun Yang, Caixia Tan, Xuerong Sun, Xiong Tang, Xiao Huang, Fan Yan, Guangxiang Zhu, Qin Wang
Summary: This study investigates the mechanisms of metamorphosis in the Chinese giant salamander, focusing on the role of caspase genes and the effect of thyroid hormone treatment. The results show that caspase genes play a key role in the loss of external gills, and thyroid hormone treatment can accelerate this process.
Article
Engineering, Biomedical
Shixian Lv, Meilyn Sylvestre, Kefan Song, Suzie H. Pun
Summary: Melittin, the primary peptide component in bee venom, has anti-tumor activity but its practical application is hindered by hemolytic activity and instability. Use of D-amino acids in place of L-amino acids reduces immunogenicity of melittin, allowing for safer delivery and maintaining cytolytic potential. D-melittin micelles show cytotoxicity in a pH-dependent manner, inducing immunogenic cell death and demonstrating potential for cancer immunotherapy. The study presents a new strategy for systemic delivery of cytotoxic peptides in cancer treatment.
Article
Environmental Sciences
Zhuanxu Ouyang, Bijing Yang, Jiangnan Yi, Shanshan Zhu, Suge Lu, Yingwei Liu, Yangwei Li, Yuanliang Li, Khalid Mehmood, Riaz Hussain, Muhammad Ijaz, Jianying Guo, Zhaoxin Tang, Ying Li, Hui Zhang
Summary: This study revealed the harmful effects of sodium fluoride on liver tissues of ducks, including promoting apoptosis and altering the expression levels of key genes.
ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY
(2021)
Article
Chemistry, Multidisciplinary
Ha Rin Kim, Young Seok Cho, Seung Woo Chung, Jeong Uk Choi, Yoon Gun Ko, Seong Jin Park, Sang Yoon Kim, Youngro Byun
Summary: This article describes a tumoral caspase-3 mediated peptide-doxorubicin conjugates (PDC) switch therapy for targeting metastatic triple-negative breast cancer. The therapy utilizes two different caspase-3 cleavable PDCs to induce apoptosis in tumor cells and target tumor sites, resulting in enhanced tumor-specific apoptosis amplification and potent therapeutic efficacy.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Chemistry, Organic
Cynthia Crifar, Fenja L. Ducker, Sacha Nguyen Thanh, Vanessa Kairouz, William D. Lubell
JOURNAL OF ORGANIC CHEMISTRY
(2019)
Article
Chemistry, Organic
N. D. Prasad Atmuri, William D. Lubell
JOURNAL OF ORGANIC CHEMISTRY
(2020)
Review
Biochemistry & Molecular Biology
Caroline Proulx, Jinqiang Zhang, David Sabatino, Sylvain Chemtob, Huy Ong, William D. Lubell
Article
Chemistry, Organic
Yousra Hamdane, Pradeep S. Chauhan, Suresh Vutla, Mukandila Mulumba, Huy Ong, William D. Lubell
Summary: Fifteen N-aminoimidazolone (Nai) dipeptides with different 5-position side-chain groups were synthesized through regioselective proline-catalyzed reactions and acid-mediated dehydration. Introducing 5-aryl-Nai dipeptides into CD36 receptor peptide ligands provided insights into the conformation responsible for binding affinity and anti-inflammatory activity.
Article
Cell Biology
Marie-France Dorion, Mukandila Mulumba, Shuya Kasai, Ken Itoh, William D. Lubell, Huy Ong
Summary: This study reveals that the CD36 ligand MPE-001 protects RPE cells from oxidative stress by promoting autophagy. MPE-001 reduced oxidative stress and cell apoptosis induced by NaIO3, restored autophagic flux, and this protective effect was associated with an increase in mature autophagosomes.
OXIDATIVE MEDICINE AND CELLULAR LONGEVITY
(2021)
Article
Chemistry, Medicinal
Ragnhild G. Ohm, Mukandila Mulumba, Ramesh M. Chingle, Ahsanullah, Jinqiang Zhang, Sylvain Chemtob, Huy Ong, William D. Lubell
Summary: Expanding cyclic peptide diversity through A(3)-macrocyclization and introducing new components has shown the importance of triple bonds and residues like N-epsilon-allyl lysine in high CD36 binding affinity, aiding in the development of ideal CD36 modulators to curb macrophage-driven inflammation.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Anh Minh Thao Nguyen, Skye Brettell, Noelie Douanne, Claudia Duquette, Audrey Corbeil, Emanuella F. Fajardo, Martin Olivier, Christopher Fernandez-Prada, William D. Lubell
Summary: The study demonstrated that derivatives with a single methyl group in N-methylated lipopeptides exhibit higher activity against various strains of leishmaniasis protozoan and have relatively high potency against resistant strains. Additionally, the systematic study of the effects of methylation and turn geometry on anti-parasitic activity revealed the importance of an extended conformer about the central residues and conformational mobility by tertiary amide isomerization and turn geometry at the extremities of the active peptides.
Article
Chemistry, Organic
Ramakotaiah Mulamreddy, Xin Hou, Sylvain Chemtob, William D. Lubell
Summary: The synthesis of 6-hydroxymethyl indolizidin-2-one amino acids from L-serine involves 10 steps, including intramolecular ring opening and lactam formation. X-ray analyses showed ideal peptide geometry, and the analogue exhibited inhibitory activity on myometrial contractility within a prostaglandin-F-2 alpha receptor modulator.
Article
Biochemistry & Molecular Biology
Ramakotaiah Mulamreddy, William D. Lubell
Summary: This paper reports the synthesis of 5- and 7-hydroxy indolizidin-2-one N-(Boc)amino acids from L-serine, and discusses their potential in peptide mimicry.
Editorial Material
Biochemistry & Molecular Biology
William D. Lubell
Article
Chemistry, Medicinal
Xiaozheng Wei, Sitan Diarra, Antoine Douchez, Juliana C. Cunico Dallagnol, Terence E. Hebert, David Chatenet, William D. Lubell
Summary: The study of Urotensin II receptor (UT) modulators can help us understand the roles of the endogenous cyclic peptide ligands urotensin II (UII) and urotensin II-related peptide (URP) in disease etiology. By designing and synthesizing a series of compounds, selective modulators of hUII and URP activities were discovered, which can affect biological processes such as vasoconstriction.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Anh Minh Thao Nguyen, Moran Shalev-Benami, Chloe Rosa-Teijeiro, Ana Victoria Ibarra-Meneses, Ada Yonath, Anat Bashan, Charles L. Jaffe, Martin Olivier, Christopher Fernandez-Prada, William D. Lubell
Summary: A strategy for preparing potent anisomycin derivatives with reduced host toxicity has been revealed by assessing structure-activity relationships for anti-protozoan activity. Different modifications of the alcohol, amine, and aromatic functional groups have been studied, and it was found that introducing substituents at the para-phenol moiety of anisomycin can maintain the anti-protozoan potency without significant loss of activity against the host.
Article
Chemistry, Organic
Zhihong Luo, Lei Xu, Xiaomin Tang, Xuejun Zhao, Tong He, William D. Lubell, Jinqiang Zhang
Summary: In this study, novel all-hydrocarbon cross-linked aza-stapled peptides were designed and synthesized for the first time. These peptides exhibited increased anti-tumor activity, binding affinities, and cell membrane permeability compared to their linear counterparts.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Fatemeh M. Mir, Marco Crisma, Claudio Toniolo, William D. Lubell
Article
Chemistry, Multidisciplinary
Fatemeh M. Mir, Marco Crisma, Claudio Toniolo, William D. Lubell
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)