Article
Food Science & Technology
Nassim Salem Adrar, Khodir Madani, Sabah Adrar
Summary: Bradykinin and polyphenols may have a dual role in health; encapsulation of polyphenols could potentially reduce their binding affinity to bradykinin receptors, alleviating pain caused by bradykinin. This work falls within basic science, providing a potential biochemical mechanism of polyphenols' pharmacological action on pain sensation induced by bradykinin.
Article
Endocrinology & Metabolism
Elizabeth K. M. Johnstone, Mohammed Akli Ayoub, Rebecca J. Hertzman, Heng B. See, Rekhati S. Abhayawardana, Ruth M. Seeber, Kevin D. G. Pfleger
Summary: This study investigated the heteromerization of AT(2) and B-2 receptors in HEK293FT cells. The results demonstrated the functional interaction between these receptors and the differences in signaling, providing important evidence for studying GPCR pharmacology and signaling diversity.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Review
Medicine, Research & Experimental
Indiara Brusco, Maria Fernanda Pessano Fialho, Gabriela Becker, Evelyne Silva Brum, Amanda Favarin, Lara Panazzolo Marquezin, Patrick Tuzi Serafini, Sara Marchesan Oliveira
Summary: Kinins are endogenous peptides that play an essential role in physiological and pathological processes by activating two transmembrane receptors. This review summarizes the current understanding of the involvement of kinin receptors and their potential therapeutic applications in various painful conditions. The pharmacological actions and clinical potential of kinin receptor antagonists and other targeting molecules are also discussed.
Article
Medicine, General & Internal
Shunsuke Takahagi, Michihiro Hide, Yumi Aoyama, Atsushi Fukunaga, Hiroyuki Murota
Summary: This study aims to evaluate the effectiveness of icatibant in treating sweating-induced dermal pain and to establish the role of bradykinin in pain induction. The methods include a randomized controlled study to evaluate the efficacy of icatibant injection in treating sweating-induced dermal pain. The findings may contribute to a better understanding of the underlying mechanisms of dermal pain and suggest potential treatment options.
Article
Chemistry, Medicinal
Yongtao Li, Wenwei Lin, William C. Wright, Sergio C. Chai, Jing Wu, Taosheng Chen
Summary: Researchers identified PXR agonists, antagonists, and partial agonist/partial antagonists based on specific scaffold of a human PXR antagonist SPA70. These compounds showed divergent cellular activities and interactions, providing novel chemical tools for studying human PXR.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Gabriela Becker, Maria Fernanda Pessano Fialho, Indiara Brusco, Sara Marchesan Oliveira
Summary: Cisplatin is a commonly used chemotherapy drug for solid tumors, but its effectiveness is limited by neurotoxic side effects such as peripheral neuropathy. This study investigates the role of kinin B-1 and B-2 receptors in cisplatin-induced peripheral neuropathy in mice. The results suggest that targeting these receptors may be a potential strategy for treating the painful symptoms caused by cisplatin treatment.
Review
Biochemistry & Molecular Biology
Mansour Haddad, Federica Cherchi, Mohammad Alsalem, Yousef M. Al-saraireh, Saba Madae'en
Summary: This review presents new findings on the role of adenosine and its receptors in neuropathic and inflammatory pain. Adenosine receptor ligands have shown promising efficacy and safety in clinical research and could be used as therapeutic targets for various pain disorders. The review also discusses the latest studies on adenosine receptor ligands in different pain models and the potential of newly synthesized allosteric adenosine receptor modulators.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Cell Biology
Marco Sisignano, Michael J. M. Fischer, Gerd Geisslinger
Summary: The proton-sensing G-protein coupled receptors, including GPR4, TDAG8, OGR1, and G2A, act as cellular sensors of acidification with varying pH detection capabilities. While initially thought to detect acidic cellular environments in inflammation, recent studies reveal their diverse roles in tumor biology, cardiovascular physiology, asthma, mechanosensation, and other processes. Each receptor has unique properties and potential roles in various physiological and pathophysiological conditions, highlighting the need for further research on their biological and pharmacological contexts.
Editorial Material
Pharmacology & Pharmacy
Petr Pavek
Summary: This study utilized 3D human hepatocyte spheroids as a model for CYP450 enzyme induction, demonstrating high sensitivity and specificity. The authors identified a noncanonical PXR-mediated CYP3A4 induction mechanism, highlighting the importance of using 3D primary human hepatocyte spheroids in preclinical induction testing.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Pharmacology & Pharmacy
Vanessa Pereira, Juri Aparicio Arias, Amadeu Llebaria, Cyril Goudet
Summary: Neuropathic pain is a challenging condition to manage. In this study, the role of the amygdala in regulating neuropathic pain was investigated. The activation of mGlu4 receptors in the amygdala was found to alleviate sensory and depressive-like symptoms in a mouse model of neuropathy.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Cell Biology
Delia I. Fernandez, Marijke J. E. Kuijpers, Johan W. M. Heemskerk
Summary: Platelets are stimulated to increase Ca2+ levels through G-protein coupled receptors or ITAM-linked receptors. There are significant differences in Ca2+ signaling between different receptor types, and simultaneous stimulation of both types of receptors can lead to a highly enforced Ca2+ rise.
Article
Microbiology
Tesfaye Rufael Chibssa, Melaku Sombo, Jacqueline Kasiiti Lichoti, Tajelser Idris Badri Adam, Yang Liu, Yazeed Abd Elraouf, Reingard Grabherr, Tirumala Bharani K. Settypalli, Francisco J. Berguido, Angelika Loitsch, Mesfin Sahle, Giovanni Cattoli, Adama Diallo, Charles Euloge Lamien
Summary: The study revealed a high genetic similarity among East African isolates of Lumpy skin disease virus (LSDV), with the exception of one isolate showing mixed features between LSDV Neethling vaccine and field isolates. Further analysis of various genes indicated differences from previously described LSDV variants carrying a 12-nucleotide insertion in the GPCR gene.
Review
Biochemistry & Molecular Biology
Flaminia Coluzzi, Maria Sole Scerpa, Monica Rocco, Diego Fornasari
Summary: Opioids, commonly used for pain management, may face challenges in crossing the blood-brain barrier due to the presence of transporters such as P-gp. This can lead to opioid tolerance and altered transport of other drugs. P-gp expression can also be influenced by opioids, affecting pain management and drug interactions. Understanding the interactions between P-gp and opioids is important in clinical practice.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Neurosciences
Luke Grundy, Ashlee Caldwell, Sonia Garcia-Caraballo, David Grundy, Nick J. Spencer, Xinzhong Dong, Joel Castro, Andrea M. Harrington, Stuart M. Brierley
Summary: This study demonstrates the functional expression of MrgprA3 and MrgprC11 in bladder afferents for the first time. Activation of these receptors triggers hypersensitivity to distension, which is a critically valuable factor for therapeutic target development.
JOURNAL OF NEUROSCIENCE
(2021)
Article
Chemistry, Medicinal
Rong Yang, Zhenxing Chen, Fuda Xie, Mingxiang Xie, Na Liu, Ziren Su, Jiangyong Gu, Ruizhi Zhao
Summary: The study investigated the inhibitory effect of (+)-borneol and (-)-borneol on P-glycoprotein (Pgp) in reversing mitoxantrone (MTO) resistance. The results showed that both borneol enantiomers could enhance the efficacy of MTO in cancer cells by reducing the protein expression of Pgp and interfering with the binding affinity between MTO and Pgp in the drug-binding pocket. Using molecular docking and dynamics simulations, the study identified key amino acid residues responsible for borneols' ability to reverse MTO resistance through noncompetitive inhibition.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2021)
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)