67,352 results match your criteria potential inhibit


Gynura procumbens (Lour.) Merr. extract attenuates monocyte adherence to endothelial cells through suppression of the NF-κB signaling pathway.

J Ethnopharmacol 2022 May 16:115391. Epub 2022 May 16.

Centre for Drug and Herbal Development, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia. Electronic address:

Ethnopharmacological Relevance: Gynura procumbens (Lour.) Merr. is a herbaceous plant that grows in Malaysia and other parts of Southeast Asia. Read More

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Effective components and mechanism analysis of anti-platelet aggregation effect of Justicia procumbens L.

J Ethnopharmacol 2022 May 16:115392. Epub 2022 May 16.

Faculty of Pharmacy, Hubei University of Chinese Medicine, Wuhan, 430065, China; Key Laboratory of Traditional Chinese Medicine Resources and Chemistry of Hubei Province, Wuhan, 430065, China; Collaborative Innovation Center of Traditional Chinese Medicine of New Products for Geriatrics Hubei Province, Wuhan, 430065, China. Electronic address:

Ethnopharmacological Relevance: Justicia procumbens L. is a traditional Chinese medicine, first recorded in "Shen Nong's Herbal Classic", for the treatment of lumbar pain and fever. As a widely distributed herb, it has also been documented in India, Nepal, and Malaysia. Read More

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MicroRNAs and osteosarcoma: Potential targets for inhibiting metastasis and increasing chemosensitivity.

Biochem Pharmacol 2022 May 16:115094. Epub 2022 May 16.

Department of Clinical Biochemistry and Laboratory Medicine, School of Medicine, Tabriz University of Medical Sciences, Tabriz, Iran. Electronic address:

Osteosarcoma (OS) is the third most common cancer in young adults after lymphoma and brain cancer. Metastasis, like other cellular events, is dependent on signaling pathways; a series of changes in some proteins and signaling pathways pave the way for OS cells to invade and migrate. Ezrin, TGF-β, Notch, RUNX2, matrix metalloproteinases (MMPs), Wnt/β-catenin, and phosphoinositide 3-kinase (PI3K)/AKT are among the most important of these proteins and signaling pathways. Read More

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miR-142-5p Encapsulated by Serum-Derived Extracellular Vesicles Protects against Acute Lung Injury in Septic Rats following Remote Ischemic Preconditioning via the PTEN/PI3K/Akt Axis.

J Innate Immun 2022 May 19:1-11. Epub 2022 May 19.

Department of Critical Care Medicine, Henan Key Laboratory for Critical Care Medicine, Zhengzhou Key Laboratory for Critical Care Medicine, Henan Provincial People's Hospital, Zhengzhou University People's Hospital, Zhengzhou, China.

This study intends to investigate the effects of miR-142-5p encapsulated by serum-derived extracellular vesicles (EVs) on septic acute lung injury (ALI) following remote ischemic preconditioning (RIPC) through a PTEN-involved mechanism. ALI was induced in rats by lipopolysaccharide (LPS) injection, 24 h before which RIPC was performed via the left lower limb. Next, the binding affinity between miR-142-5p and PTEN was identified. Read More

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Intrauterine programming of cartilaginous 11β-HSD2 induced by corticosterone and caffeine mediated susceptibility to adult osteoarthritis.

Ecotoxicol Environ Saf 2022 May 16;239:113624. Epub 2022 May 16.

Division of Joint Surgery and Sports Medicine, Department of Orthopedic Surgery, Zhongnan Hospital of Wuhan University, Wuhan 430071, China; Hubei Provincial Key Laboratory of Developmentally Originated Disease, Wuhan 430071, China. Electronic address:

Our previous study reported that prenatal caffeine exposure (PCE) could induce chondrodysplasia and increase the susceptibility to osteoarthritis in offspring rats. However, the potential mechanisms and initiating factors remain unknown. This study aims to investigate whether 11β-HSD2, a glucocorticoid-metabolizing enzyme, is involved in the susceptibility of osteoarthritis induced by PCE and to further explore its potential mechanisms and initiating factors. Read More

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LY450139 Inhibited Ti-Particle-Induced Bone Dissolution via Suppressing Notch and NF-κB Signaling Pathways.

Calcif Tissue Int 2022 May 19. Epub 2022 May 19.

Shanghai Key Laboratory of Orthopaedic Implants, Department of Orthopaedic Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.

Aseptic loosening of the prosthesis caused by wear-particle-induced osteolysis is a long-term complication and one of the most common reasons for the failure of joint implants. The primary cause of aseptic loosening of the prosthesis is overactive bone resorption caused by wear-particle-activated osteoclasts in both direct and indirect ways. Therefore, drugs that can inhibit differentiation and bone resorption of osteoclasts need investigation as a potential therapeutic strategy to prevent and treat peri-prosthetic osteolysis and thereby prolong the service life of the prosthesis. Read More

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Life without blood: Molecular and functional analysis of hirudins and hirudin-like factors of the Asian non-hematophagous leech Whitmania pigra.

J Thromb Haemost 2022 May 19. Epub 2022 May 19.

Department of Animal Physiology, Zoological Institute and Museum, University of Greifswald, Greifswald.

Background: Several leech species of the genera Hirudo, Hirudinaria and Whitmania are widely used in Traditional Chinese Medicine for the oral treatment of disorders associated with blood stasis. Among them, the non-hematophagous leech Whitmania pigra expresses a variety of components that have the potential to act on the vertebrate blood coagulation system.

Objective: Whether or not the thrombin inhibitor hirudin, probably the most prominent leech-derived anticoagulant, is actually present in Whitmania pigra, is still a matter of debate. Read More

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extract induces apoptosis by inhibiting the activation of AKT in SW480 human colon cancer cells.

Pharm Biol 2022 Dec;60(1):915-930

Guangxi Key Laboratory of Efficacy Study on Chinese Materia Medica, Guangxi University of Chinese Medicine, Nanning, People's Republic of China.

Context: Markgr. (Gnetaceae) is used to treat rheumatic arthralgia and bruises in the clinic.

Objective: To exam the activity and mechanism of extract (GME) against colon cancer cells SW480. Read More

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December 2022

Mercury: selenium interactions and health implications.

Neurotoxicology 2020 Dec 14;81:294-299. Epub 2020 Oct 14.

University of North Dakota, Grand Forks, North Dakota, USA. Electronic address:

Measuring the amount of mercury present in the environment or food sources may provide an inadequate reflection of the potential for health risks if the protective effects of selenium are not also considered. Selenium's involvement is apparent throughout the mercury cycle, influencing its transport, biogeochemical exposure, bioavailability, toxicological consequences, and remediation. Likewise, numerous studies indicate that selenium, present in many foods (including fish), protects against mercury exposure. Read More

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December 2020

[Effect of Met kinase inhibitor BMS-777607 on proliferation and apoptosis of tongue cell line CAL 27 squamous cell carcinoma].

Shanghai Kou Qiang Yi Xue 2021 Dec;30(6):573-578

The Second Affiliated Hospital and College of Stomatology of Jinzhou Medical University. Jinzhou 121004, China. E-mail:

Purpose: To investigate the effect of Met kinase inhibitor BMS-777607 on proliferation and apoptosis of tongue squamous cell carcinoma cell line CAL27.

Methods: The effect of BMS-777607 on proliferation of CAL27 was detected by MTT method, clone formation assay and EdU cell imaging. Morphological changes of apoptosis of CAL27 cells induced by BMS-777607 were observed by Heochst33342 staining. Read More

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December 2021

Paeoniflorin Can Improve Acute Lung Injury Caused by Severe Acute Pancreatitis through Nrf2/ARE Pathway.

Authors:
Yanyan Hu Wei Yang

Comput Math Methods Med 2022 9;2022:5712219. Epub 2022 May 9.

Department of Gastroenterology, Xiangyang Central Hospital, Affiliated Hospital of Hubei University of Arts and Science, Xiangyang 441021, China.

Objective: To evaluate the potential therapeutic effect of paeoniflorin on acute lung injury induced by severe acute pancreatitis (SAP) and to initially explore the possible protective mechanisms of paeoniflorin.

Method: The SAP lung injury rat model was established by retrograde injection of 5% sodium taurocholate to the cholangiopancreatic duct. H&E staining was used to detect pathological changes in rat lung tissue. Read More

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The Multiple Biological Functions of Dipeptidyl Peptidase-4 in Bone Metabolism.

Front Endocrinol (Lausanne) 2022 2;13:856954. Epub 2022 May 2.

Department of Endocrinology and Metabolism, Laboratory of Endocrinology and Metabolism, West China Hospital, Sichuan University, Chengdu, China.

Dipeptidyl peptidase-4 (DPP4) is a ubiquitously occurring protease involved in various physiological and pathological processes ranging from glucose homeostasis, immunoregulation, inflammation to tumorigenesis. Recently, the benefits of DPP4 inhibitors as novel hypoglycemic agents on bone metabolism have attracted extensive attraction in many studies, indicating that DPP4 inhibitors may regulate bone homeostasis. The effects of DPP4 on bone metabolism are still unclear. Read More

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Two Liberibacter Proteins Combine to Suppress Critical Innate Immune Defenses in Citrus.

Front Plant Sci 2022 2;13:869178. Epub 2022 May 2.

Biolab, New Mexico Consortium, Los Alamos, NM, United States.

We adopted a systems-based approach to determine the role of two Liberibacter asiaticus (Las) proteins, and Effector 3, in Huanglongbing (HLB) pathogenesis. While a published work suggests the involvement of these Las proteins HLB pathogenesis, the exact structure-based mechanism of their action has not been elucidated. We conducted the following experiments to determine the structure-based mechanisms of action. Read More

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Zinc Transporter ZmLAZ1-4 Modulates Zinc Homeostasis on Plasma and Vacuolar Membrane in Maize.

Front Plant Sci 2022 2;13:881055. Epub 2022 May 2.

Key Laboratory of Biology and Genetic Improvement of Maize in Southwest Region, Ministry of Agriculture, Maize Research Institute, Sichuan Agricultural University, Chengdu, China.

Zinc is an essential micronutrient for plant growth and development, and functions as a cofactor for hundreds of transcription factors and enzymes in numerous biological processes. Zinc deficiency is common abiotic stress resulting in yield loss and quality deterioration of crops, but zinc excess causes toxicity for biological systems. In plants, zinc homeostasis is tightly modulated by zinc transporters and binding compounds that uptake/release, transport, localize, and store zinc, as well as their upstream regulators. Read More

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Matrix Metalloproteinases in Chemoresistance: Regulatory Roles, Molecular Interactions, and Potential Inhibitors.

J Oncol 2022 9;2022:3249766. Epub 2022 May 9.

Centre for Virus and Vaccine Research, School of Medical and Life Sciences, Sunway University, Selangor 47500, Malaysia.

Cancer is one of the major causes of death worldwide. Its treatments usually fail when the tumor has become malignant and metastasized. Metastasis is a key source of cancer recurrence, which often leads to resistance towards chemotherapeutic agents. Read More

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8-azaadenosine and 8-chloroadenosine are not selective inhibitors of ADAR.

Cancer Res Commun 2021 Nov;1(2):56-64

Department of Medicine, Division of Molecular Oncology, Washington University School of Medicine, Saint Louis, Missouri, USA.

The RNA editing enzyme ADAR, is an attractive therapeutic target for multiple cancers. Through its deaminase activity, ADAR edits adenosine to inosine in dsRNAs. Loss of ADAR in some cancer cell lines causes activation of the type I interferon pathway and the PKR translational repressor, leading to inhibition of proliferation and stimulation of cell death. Read More

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November 2021

Protective Effects of Tiaoganquzhi Decoction in Treating inflammatory Injury of Nonalcoholic Fatty liver Disease by Promoting CGI-58 and Inhibiting Expression of NLRP3 Inflammasome.

Front Pharmacol 2022 2;13:851267. Epub 2022 May 2.

Beijing Hospital of Traditional Chinese Medicine, Capital Medical University, Beijing, China.

Tiaoganquzhi Decoction (TGQZD) is a traditional Chinese herbal formulation demonstrated to be a clinically effective treatment for nonalcoholic fatty liver disease (NAFLD), although details concerning its clinical mechanism are poor. This study aimed to explore the mechanism of TGQZD on improvement of inflammatory damage and dyslipidemia caused by NAFLD through the CGI-58/ROS/NLRP3 inflammasome pathway. In our research, the protective effects of TGQZD on HFD-induced liver injury in rats and using lipopolysaccharide (LPS)+palmitate (PA)-stimulated HepG-2 cells model. Read More

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In silico evaluation of atazanavir as a potential HIV main protease inhibitor and its comparison with new designed analogs.

Comput Biol Med 2022 Jun 15;145:105523. Epub 2022 Apr 15.

Departamento de Fisica & IFISUR (UNS-CONICET), Universidad Nacional del Sur, Av. Alem 1253, 8000, Bahia Blanca, Argentina.

Starting three decades ago and spreading rapidly around the world, acquired immunodeficiency syndrome (AIDS) is an infectious disease distinct from other contagious diseases by its unique ways of transmission. Over the past few decades, research into new drug compounds has been accompanied by extensive advances, and the design and manufacture of drugs that inhibit virus enzymes is one way to combat the AIDS virus. Since blocking enzyme activity can kill a pathogen or correct a metabolic imbalance, the design and use of enzyme inhibitors is a new approach against viruses. Read More

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Computational screening of natural compounds as putative quorum sensing inhibitors targeting drug resistance bacteria: Molecular docking and molecular dynamics simulations.

Comput Biol Med 2022 Jun 12;145:105517. Epub 2022 Apr 12.

Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia; Center of Artificial Intelligence in Precision Medicines, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.

Quorum sensing (QS) is a bacterial communication strategy controlling cells density, biofilm formation, virulence, sporulation, and survival. Since QS is considered a virulence factor in drug-resistant pathogenic bacteria, inhibition of QS can contribute to control the spread of these bacteria. We propose in this study to test in silico, 19 natural compounds for their potential to inhibit QS transcriptional regulators of Pseudomonas aeruginosa (LasR and PqsE) and Chromobacterium violaceum (CviR and CviR'). Read More

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Synthesis of macromolecular Astragalus polysaccharide-nano selenium complex and the inhibitory effects on HepG2 cells.

Int J Biol Macromol 2022 May 15. Epub 2022 May 15.

College of Food Science and Engineering, Tianjin University of Science and Technology, Tianjin 300457, China. Electronic address:

In the present study, the previously obtained macromolecuar-weight Astragalus polysaccharide (average molecular weight of 1.61 × 10 Da) was used as a stabilizer and dispersing agent for nano-composites preparation by modifying selenium nanoparticles, and then the anti-hepatoma activity on HepG2 cells was investigated as well. Results showed that the nano-composites were obtained under polysaccharide concentration of 2 mg/mL and selenium/polysaccharide mass ratio of 1:15, and exhibited symmetrical spheroid with an average diameter of 62. Read More

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Discovery of 4-methoxy-N-(1-naphthyl)benzenesulfonamide derivatives as small molecule dual-target inhibitors of tubulin and signal transducer and activator of transcription 3 (STAT3) based on ABT-751.

Bioorg Chem 2022 May 10;125:105864. Epub 2022 May 10.

Department of Colorectal Surgery, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325035, China; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China. Electronic address:

Overexpressed tubulin and continuously activated STAT3 play important roles in the development of many cancers and are potential therapeutic targets. A series of 4-methoxy-N -(1-naphthalene) benzenesulfonamide derivatives were designed and optimized based on β-tubulin inhibitor ABT-751 to verify whether STAT3 and tubulin dual target inhibitors have better antitumor effects. Compound DL14 showed strong inhibitory activity against A549, MDA-MB-231 and HCT-116 cells in vitro with IC values of 1. Read More

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ITGBL1 transcriptionally inhibited by JDP2 promotes the development of pancreatic cancer through the TGF-beta/Smad pathway.

Braz J Med Biol Res 2022 16;55:e11989. Epub 2022 May 16.

Department of Pancreatic and Biliary Surgery, The First Hospital of China Medical University, Shenyang, Liaoning, China.

Pancreatic cancer (PC) is one of the malignant tumors with the worst prognosis worldwide because of a lack of early diagnostic markers and efficient therapies. Integrin, beta-like 1 (ITGBL1) is a β-integrin-related extracellular matrix protein and is reported to promote progression of some types of cancer. Nevertheless, the function of ITGBL1 in PC is still not clear. Read More

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Mode of action of potential biocontrol agents against species and .

Mycologia 2022 May 18:1-11. Epub 2022 May 18.

Swift Current Research and Development Centre, Agriculture and Agri-Food Canada, Box 1030, Swift Current, Saskatchewan S9H 3X2, Canada.

The antagonistic activities of three potential biocontrol agents (BCAs), , and , were tested in vitro against the target fungi , and . In vitro dual-culture assay revealed that the BCAs were able to inhibit the mycelial growth of most of the target fungi, with the most common mode of action being mycoparasitism. After 5 d of incubation, depending on the host-parasite interface, biotrophic mycoparasitism was observed via attachment structures on , and . Read More

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Interactions between Salivary Proteins and Dietary Polyphenols: Potential Consequences on Gastrointestinal Digestive Events.

J Agric Food Chem 2022 May 18. Epub 2022 May 18.

INRAE, UR BIA, F-35653 Le Rheu, France.

The present review documents the current knowledge and hypotheses on how polyphenols-saliva interactions may modulate the bioaccessibility or bioavailability of nutrients and highlights research prospects in the field. After an updated description of the different classes of dietary polyphenols and their modifications by food processing or digestion, an overview of interactions between salivary proteins and polyphenols (with an emphasis on tannins) is provided. studies show that the solubility of salivary protein-tannin complexes in gastric conditions depends on the degree of tannin polymerization, while complexes are partly solubilized by bile salts. Read More

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Melatonin Alleviates Liver Fibrosis by Inhibiting Autophagy.

Curr Med Sci 2022 May 17. Epub 2022 May 17.

Department of Gastroenterology, First Affiliated Hospital of Anhui Medical University, Key Laboratory of Digestive Disease of Anhui Province, Hefei, 230022, China.

Objective: Melatonin has been reported to suppress inflammation and alleviate liver fibrosis, but its effect on autophagy in liver fibrosis has not been studied. This study investigated the effect of melatonin on autophagy in an animal model of liver fibrosis and the hepatic stellate cell (HSC)-T6 cell line.

Methods: The model was established in rats through carbon tetrachloride treatment, and melatonin was administered at three doses (2. Read More

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Isoliquiritigenin ameliorates advanced glycation end-products toxicity on renal proximal tubular epithelial cells.

Environ Toxicol 2022 May 18. Epub 2022 May 18.

Cardiovascular and Mitochondria Related Diseases Research Center, Hualien Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Hualien, Taiwan.

Diabetic nephropathy is a serious chronic complication affecting at least 25% of diabetic patients. Hyperglycemia associated advanced glycation end-products (AGEs) increase tubular epithelial-myofibroblast transdifferentiation (TEMT) and extracellular matrix synthesis and thereby causes renal fibrosis. The chalcone isoliquiritigenin, found in many herbs of Glycyrrhiza family, is known for potential health-promoting effects. Read More

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[Tumor membrane-encapsulated nanoparticles delivering programmed death 1 small interfering RNA enhance anti-tumor immunity in mouse oral squamous cell carcinoma].

Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi 2022 Apr;38(4):295-301

Department of Maxillofacial Surgery, the Second Affiliated Hospital of Hainan Medical College, Haikou 570311, China.

Objective To determine whether tumor cell membrane-encapsulated nanoparticles carrying programmed death 1 small interfering RNA (PD-1 siRNA) can target tumor tissues to inhibit the growth of oral squamous cell carcinoma, and whether it can trigger the anti-tumor immune response at the tumor site. Methods Membrane-siRNA nanoparticles(M-SNPs) was prepared by double emulsification solvent evaporation method and mechanical extrusion method. The morphology of M-SNPs was observed by transmission electron microscope. Read More

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MicroRNA-206 inhibits HCV proliferation through depressing ACC1 lipid synthesis signaling pathway.

J Viral Hepat 2022 May 18. Epub 2022 May 18.

Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan, China.

MicroRNAs are considered to play important roles in cell biological and pathological progress. microRNA-206 (miR-206) was reported to participate in lipogenesis, and lipid droplets were necessary for the life cycle of HCV proliferation. Whether miR-206 was associated with HCV proliferation and the potential mechanism are not clear. Read More

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Computational studies on potential new anti-Covid-19 agents with a multi-target mode of action.

J King Saud Univ Sci 2022 May 13:102086. Epub 2022 May 13.

Department of Chemistry, G. M. University, Sambalpur, Odisha, India.

A compound that could inhibit multiple targets associated with SARS-CoV-2 infection would prove to be a drug of choice against the virus. Human receptor-ACE2, receptor binding domain (RBD) of SARS-CoV-2 S-protein, Papain-like protein of SARS-CoV-2 (PLpro), reverse transcriptase of SARS-CoV-2 (RdRp) were chosen for in silico study. A set of previously synthesized compounds () were docked into the active sites of the targets. Read More

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Potential mechanisms of resistance to current anti-thrombotic strategies in Multiple Myeloma.

Cancer Drug Resist 2022 7;5(1):214-228. Epub 2022 Mar 7.

Irish Centre for Vascular Biology, School of Pharmacy and Biomolecular Sciences, Royal College of Surgeons in Ireland, Dublin D02YNVV, Ireland.

Multiple Myeloma (MM) is a common haematological malignancy that is associated with a high rate of venous thromboembolism (VTE) with almost 10% of patients suffering thrombosis during their disease course. Recent studies have shown that, despite current thromboprophylaxis strategies, VTE rates in MM remain disappointingly high. The pathophysiology behind this consistently high rate of VTE is likely multifactorial. Read More

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