Review
Biochemistry & Molecular Biology
Alina Scridon
Summary: This article comprehensively explores the complex role of platelets in hemostasis and thrombosis, discussing their importance in clinical medicine, and studying hemostatic platelet-related disorders and antithrombotic therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Medicine, General & Internal
Tomas Bolek, Matej Samos, Jakub Jurica, Lucia Stanciakova, Martin Jozef Pec, Ingrid Skornova, Peter Galajda, Jan Stasko, Marian Mokan, Peter Kubisz
Summary: The coronavirus disease (COVID-19) caused by SARS-CoV2 is associated with a higher risk of thromboembolism due to clotting disorders, platelet activation, vascular injury, and fibrinolysis changes. Studies have shown a high incidence of venous and arterial thrombosis in COVID-19 patients. The occurrence of arterial thrombosis in severe/critically ill COVID-19 patients admitted to intensive care units is estimated to be around 1%. Determining the optimal antithrombotic strategy in patients with COVID-19 is challenging due to multiple pathways of platelet activation and coagulation leading to thrombus formation. This article reviews the current understanding of antiplatelet therapy in patients with COVID-19.
JOURNAL OF CLINICAL MEDICINE
(2023)
Review
Pharmacology & Pharmacy
Gabriella Passacquale, Pankaj Sharma, Divaka Perera, Albert Ferro
Summary: Antiplatelet medications are crucial in the treatment of cardiovascular and cerebrovascular diseases, with different choices and risks depending on the specific conditions of the patients. Personalized therapy based on individual patient characteristics is essential to optimize treatment outcomes.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Review
Cardiac & Cardiovascular Systems
Gauranga Mahalwar, Ashish Kumar, Monil Majmundar, Olayinka Adebolu, Revanth Yendamuri, Nicole Lao, Nishad Barve, Rolf P. Kreutz, Grant W. Reed, Rishi Puri, Sourbha S. Dani, Ankur Kalra
Summary: The optimal antithrombotic therapy post transcatheter aortic valve replacement (TAVR) remains uncertain. A network meta-analysis of randomized controlled trials was conducted to determine the outcomes with various antithrombotic strategies. The results showed that single antiplatelet therapy (SAPT) was associated with a reduced risk of major or life-threatening bleeding compared to dual antiplatelet therapy (DAPT). Other antithrombotic strategies had similar odds of major and life-threatening bleeding compared to DAPT. There were no differences in the incidence of stroke, myocardial infarction, all-cause mortality, and cardiac mortality among the various antithrombotic strategies post TAVR.
CURRENT PROBLEMS IN CARDIOLOGY
(2022)
Article
Medicine, Research & Experimental
Barbara Poniedzialek, Joanna Rosinska, Piotr Rzymski, Marta Fiolka
Summary: This study demonstrates that the polysaccharide-protein complex from Dendrobaena veneta coelomic fluid (PPC-DV) exhibits in vitro antiplatelet and anticoagulant activities, making it a potential candidate for cardiovascular disease prevention.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Gastroenterology & Hepatology
Alan Zakko, Liam Zakko, Alyssa A. Grimshaw, Loren Laine
Summary: The use of antiplatelet monotherapy in patients undergoing sphincterotomy during ERCP is associated with an increased risk of post-procedure bleeding based on systematic review and meta-analysis. However, the quality of existing studies is limited and further high-quality research is required to confirm these findings.
DIGESTIVE DISEASES AND SCIENCES
(2022)
Article
Cardiac & Cardiovascular Systems
Darren Pan, Ada Ip, Serena Zhan, Isaac Wasserman, Daniel J. Snyder, Alexandra Z. Agathis, Nikhil Shamapant, Jeong Yun Yang, Akila Pai, Madhu Mazumdar, Hooman Poor
Summary: This study aimed to investigate the relationship between pre-hospitalization antiplatelet medication use and COVID-19 disease severity. The results showed that after adjusting for covariates, there was no association between pre-hospital antiplatelet use and the severity of COVID-19 in hospitalized patients.
Article
Health Care Sciences & Services
Yoonsuk Jung, Eui Im, Jinhee Lee, Hyeah Lee, Changmo Moon
Summary: This study compared the performance of FITs for CRC detection between users and non-users of antiplatelet agents and warfarin using a large-scale population-based database. It found that users of antiplatelet agents had lower positive predictive values for CRC detection compared to non-users, while there were no significant differences for warfarin users.
JOURNAL OF PERSONALIZED MEDICINE
(2021)
Article
Oncology
Chern-Horng Lee, Chiu-Yi Hsu, Tzung-Hai Yen, Tsung-Han Wu, Ming-Chin Yu, Sen-Yung Hsieh
Summary: This study aimed to assess the efficacy and safety of long-term aspirin use in cirrhotic patients. The results showed that long-term aspirin use significantly reduced the incidence of hepatocellular carcinoma and overall mortality, without increasing the risk of gastrointestinal bleeding.
Review
Surgery
Yoon Suk Jung, Eui Im, Chan Hyuk Park
Summary: The use of antithrombotic agents significantly lowered the PPV of FIT for detecting advanced colorectal neoplasia, potentially increasing false positives.
SURGICAL ENDOSCOPY AND OTHER INTERVENTIONAL TECHNIQUES
(2022)
Article
Biochemistry & Molecular Biology
Si-Yuan Zhou, Lei Li, Enzehua Xie, Mei-Xi Li, Jian-Hua Cao, Xiu-Bin Yang, Da-Yong Wu
Summary: To prevent the failure of small-diameter vascular grafts caused by platelet aggregation and the coagulant system, researchers prepared a heparin-aspirin compound and grafted it onto the surface of a polycaprolactone/polyurethane composite tube. This compound provided both anticoagulant and antiplatelet functions, promoted endothelial cell adhesion and proliferation, and showed more effectiveness in reducing platelet activation and preventing thrombosis compared to heparin.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemical Research Methods
Chi-Ju Kim, Jungmin Kim, Jonathan Sabate del Rio, Dong Yeob Ki, Junyoung Kim, Yoon-Kyoung Cho
Summary: Platelet function tests are crucial in diagnosing inherited platelet function disorders and monitoring antiplatelet therapies. Light transmission aggregometry (LTA) is considered the gold standard, but lacks standardization and requires a large volume of blood. A centrifugal microfluidic disc has been developed to automate LTA testing from a small blood sample, producing more precise results in a shorter time.
Review
Cell Biology
Marta Brambilla, Paola Canzano, Alessia Becchetti, Elena Tremoli, Marina Camera
Summary: COVID-19 is a pandemic caused by SARS-CoV-2 infection, leading to inflammation and thrombosis. Targeting the altered platelet activation state may be beneficial, with some antiplatelet drugs showing promising results.
Review
Clinical Neurology
Frederick Ewbank, Jacqueline Birks, Diederik Bulters
Summary: There is an association between aspirin use and subarachnoid hemorrhage in patients with intracranial aneurysms, but this protective relationship is not seen in the general population. Prospective randomized studies are required to further investigate the effect of aspirin on unruptured intracranial aneurysms.
INTERNATIONAL JOURNAL OF STROKE
(2022)
Article
Cardiac & Cardiovascular Systems
Guiomar Mendieta, Shamir Mehta, Usman Baber, Dominick J. Angiolillo, Carlo Briguori, David Cohen, Timothy Collier, George Dangas, Dariusz Dudek, Javier Escaned, Robert Gil, Birgit Vogel, Davide Cao, Alessandro Spirito, Kurt Huber, Adnan Kastrati, Upendra Kaul, Ran Kornowski, Mitchell W. Krucoff, Vijay Kunadian, David J. Moliterno, E. Magnus Ohman, Gennaro Sardella, Samantha Sartori, Samin Sharma, Richard Shlofmitz, P. Gabriel Steg, Ya-Ling Han, Stuart Pocock, C. Michael Gibson, Roxana Mehran
Summary: In high-risk patients, ticagrelor monotherapy reduces bleeding events without increasing the risk of ischemic events compared to dual antiplatelet therapy. The benefit of ticagrelor monotherapy is consistent across different bleeding and ischemic risk levels.
JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Gaurangkumar C. Brahmbhatt, Tushar R. Sutariya, Hiralben D. Atara, Narsidas J. Parmar, Vivek K. Gupta, Irene Lagunes, Jose M. Padron, Prashant R. Murumkar, Mange Ram Yadav
MOLECULAR DIVERSITY
(2020)
Correction
Neurosciences
Anshuman Sinha, Riyaj S. Tamboli, Brashket Seth, Ashish M. Kanhed, Shashi Kant Tiwari, Swati Agarwal, Saumya Nair, Rajani Giridhar, Rajnish Kumar Chaturvedi, Mange Ram Yadav
MOLECULAR NEUROBIOLOGY
(2019)
Review
Pharmacology & Pharmacy
Prashant R. Murumkar, Rahul B. Ghuge, Monica Chauhan, Rahul R. Barot, Sharmishtha Sorathiya, Kailash M. Choudhary, Karan D. Joshi, Mange Ram Yadav
EXPERT OPINION ON DRUG DISCOVERY
(2020)
Article
Biochemistry & Molecular Biology
Dushyant Patel, Nirav R. Patel, Ashish M. Kanhed, Divya M. Teli, Kishan B. Patel, Prashant D. Joshi, Sagar P. Patel, Pallav M. Gandhi, Bharat N. Chaudhary, Navnit K. Prajapati, Kirti Patel, Mange Ram Yadav
BIOORGANIC CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Ashish M. Kanhed, Dushyant Patel, Divya M. Teli, Nirav R. Patel, Mahesh T. Chhabria, Mange Ram Yadav
Summary: COVID-19 is a worldwide pandemic caused by the novel coronavirus, requiring structural and non-structural proteins for replication mainly by the main protease (Mpro). Systematic screening of approved drug library and Asinex BioDesign library identified potential antiviral agents, with structural modifications needed for stability and safety.Screenings of the libraries resulted in molecules with promising interactions with the target protein Mpro, categorized into different classes for further drug development.
MOLECULAR DIVERSITY
(2021)
Article
Biochemistry & Molecular Biology
Dushyant Patel, Nirav R. Patel, Ashish M. Kanhed, Divya M. Teli, Kishan B. Patel, Pallav M. Gandhi, Sagar P. Patel, Bharat N. Chaudhary, Dharti B. Shah, Navnit K. Prajapati, Kirti Patel, Mange Ram Yadav
ACS CHEMICAL NEUROSCIENCE
(2020)
Article
Biochemistry & Molecular Biology
Kishan B. Patel, Dushyant Patel, Nirav R. Patel, Ashish M. Kanhed, Divya M. Teli, Bhumi Gandhi, Bhavik S. Shah, Bharat N. Chaudhary, Navnit K. Prajapati, Kirti Patel, Mange Ram Yadav
Summary: Carbazole-based derivatives were designed, synthesized, and evaluated for their inhibitory activity against cholinesterase, antioxidant properties, and metal chelating abilities. Two compounds showed promising ChE inhibitory activity and specific copper ion chelating ability, along with strong interactions with the active sites of ChE enzymes. These compounds also demonstrated significant in silico drug-like pharmacokinetic properties.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Honnavalli Yogish Kumar, Prashant R. Murumkar, B. P. Srinivasan, Vijay Pawar, M. R. Yadav
Summary: This study reported the design, synthesis, and cytotoxicity studies of a series of derivatives, with two compounds showing remarkable cytotoxicity and inducing cell cycle arrest and apoptosis in leukemia cancer cells.
MOLECULAR DIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
M. R. Suryawanshi, A. M. Kanhed, V. M. Kulkarni, S. H. Bhosale, M. R. Yadav
Summary: In this study, a hit molecule with antidepressant activity was discovered and modified chemically to obtain different derivatives. The synthesized compounds showed moderate to good antidepressant activity, with the most potent compound exhibiting better potential than standard drugs. Molecular dynamics and acute oral toxicity tests were also performed.
MOLECULAR DIVERSITY
(2022)
Article
Chemistry, Multidisciplinary
Mange Ram Yadav, Mukesh Kumar, Prashant R. Murumkar
Summary: Gene therapy has the potential to address a wide range of health issues, but the lack of a suitable vector is a major obstacle. Gemini amphiphiles show promise in transfection efficiency, although they exhibit concentration-dependent toxicity in MTT assays.
Article
Oncology
Kaushik Neogi, Prashant R. Murumkar, Priyanshu Sharma, Poonam Yadav, Mallika Tewari, Devarajan Karunagaran, Prasanta Kumar Nayak, Mange Ram Yadav
Summary: In this study, novel 4,7-disubstituted 8-methoxyquinazoline derivatives were designed as potential cytotoxic agents against cancers by inhibiting the protein-protein interactions of beta-catenin/TCF4. The most potent compound (18B) showed significant cytotoxicity, inducing apoptosis and inhibiting cell migration in HCT116 and HepG2 cells. Mechanistic studies revealed that compound (18B) downregulated the beta-catenin/TCF4 signaling pathway, protein expression, and mRNA levels of c-MYC andCyclin D1. It also exhibited cytotoxicity against primary human gallbladder cancer cells. These findings suggest that compound (18B) is a promising lead molecule for anticancer therapy targeting the beta-catenin/TCF4 signaling pathway.
TRANSLATIONAL ONCOLOGY
(2022)
Article
Chemistry, Physical
Drishti Panjwani, Shruti Patel, Deepak Mishra, Viral Patel, MangeRam Yadav, Abhay Dharamsi, Asha Patel
Summary: This study developed and characterized biotin-streptavidin conjugated bovine serum albumin nanoparticles containing Gefitinib using the desolvation method. The nanoparticles exhibited monodispersity and a negatively charged surface. They showed high drug loading and sustained drug release at physiological pH. In cytotoxicity studies, these nanoparticles demonstrated better cell growth inhibition and reduced side effects compared to other formulations of Gefitinib.
JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Physical
Atul N. Khadse, Hardik H. Savsani, Rupesh V. Chikhale, Rahul B. Ghuge, Dixit R. Prajapati, Goshiya Kureshi, Prashant R. Murumkar, Kirti V. Patel, Sadhana J. Rajput, Mange Ram Yadav
Summary: Direct inhibition of FXa has been proven effective in anticoagulation with minimal bleeding risks. A novel series of anthranilamide derivatives were designed and synthesized to improve selectivity and physicochemical properties. These compounds showed potent FXa inhibitory activities and high selectivity over thrombin, as well as good anticoagulant activity and safety in animal models.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Ashish M. Kanhed, Dushyant V. Patel, Nirav R. Patel, Anshuman Sinha, Priyanka S. Thakor, Kishan B. Patel, Navnit K. Prajapati, Kirti V. Patel, Mange Ram Yadav
Summary: To confront the complex pathogenesis of Alzheimer's disease, the development of multitarget-directed ligands has emerged as a promising approach. In this study, a series of indoloquinoxaline derivatives were designed and synthesized for Alzheimer's disease. The synthesized compounds exhibited moderate to good cholinesterase inhibitory activity and compound 9f was identified as the most potent and selective BuChE inhibitor. Compound 9f also showed self-induced Aβ(1-42) aggregation inhibitory activity and favorable in silico ADMET properties. These findings suggest that compound 9f has potential as a multitarget-directed ligand for developing novel anti-AD drugs.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Multidisciplinary
Riyaj S. Tamboli, Mahesh M. Shidore, Radha Charan Dash, Ashish M. Kanhed, Nirav R. Patel, Shailesh R. Shah, Mangeram Ram Yadav
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)