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[PDF] Top 20 Protease-Activated Drug Development

Has 10000 "Protease-Activated Drug Development" found on our website. Below are the top 20 most common "Protease-Activated Drug Development".

Protease-Activated Drug Development

Protease-Activated Drug Development

... be activated by the acidic conditions found in the tumor microenvironment ...be activated by glycosaminoglycans while cathepsins B, L and S are secreted in active form ... See full document

23

Expression of Protease-Activated Receptor 1 and 2 and Anti-Tubulogenic Activity of Protease-Activated Receptor 1 in Human Endothelial Colony-Forming Cells

Expression of Protease-Activated Receptor 1 and 2 and Anti-Tubulogenic Activity of Protease-Activated Receptor 1 in Human Endothelial Colony-Forming Cells

... The development of the endothelial phenotype was assessed by immunoblotting for the endothelial markers von Willebrand Factor (VWF), VEGFR2 and CD31 (Figure ... See full document

10

Protein targets of inflammatory serine proteases and cardiovascular disease

Protein targets of inflammatory serine proteases and cardiovascular disease

... from activated leuko- cytes and mast cells or generated through the coagulation ...phenotypes. Protease-activated receptors (PARs) mediate serine protease effects; however, these proteases ... See full document

17

Doxorubicin-loaded protease-activated near-infrared fluorescent polymeric nanoparticles for imaging and therapy of cancer

Doxorubicin-loaded protease-activated near-infrared fluorescent polymeric nanoparticles for imaging and therapy of cancer

... MDA-MB-231 cells were plated on eight-well Lab-Tek chambered coverslips at a density of 50,000 cells per well in 0.3 mL media. Cells grew under normal culture condi- tions for 24 hours prior to beginning the studies. ... See full document

26

Protease activated receptors 1 and 4 mediate activation of human platelets by thrombin

Protease activated receptors 1 and 4 mediate activation of human platelets by thrombin

... activates platelets has been an important goal. Iterations around PAR1’s tethered ligand sequence SFLLRN have already led to the development of potent peptide-based antagonists (27). These antagonists blocked ... See full document

10

Design, Synthesis, and Evaluation of Novel Protease-Activated Receptor 2 (PAR2)-Targeting Imaging Agents for Cancer

Design, Synthesis, and Evaluation of Novel Protease-Activated Receptor 2 (PAR2)-Targeting Imaging Agents for Cancer

... Since multiple reports have shown that Class II peptides can have improved potency and affinity for PAR2 compared to Class I peptides, they were also investigated for the development of PAR2-targeting PET imaging ... See full document

137

Hypoxia-activated prodrugs and redox-responsive nanocarriers

Hypoxia-activated prodrugs and redox-responsive nanocarriers

... be activated in tumor hypoxic tissue, which can avoid nonspecificity of current antineoplastic agents to minimize side effects and benefit to clinical ...and drug cytotoxicity side effects, few drugs could ... See full document

24

Thrombin promotes fibronectin secretion by bone marrow mesenchymal stem cells via the protease-activated receptor mediated signalling pathways

Thrombin promotes fibronectin secretion by bone marrow mesenchymal stem cells via the protease-activated receptor mediated signalling pathways

... Thrombin is a potent regulator for the functionality of many kinds of cells. In the present study, it is found that thrombin could enhance the secretion of FN by human MSCs, and thrombin-treated MSCs maintain their ... See full document

11

The Impact of Individual Human Immunodeficiency Virus Type 1 Protease Mutations on Drug Susceptibility Is Highly Influenced by Complex Interactions with the Background Protease Sequence

The Impact of Individual Human Immunodeficiency Virus Type 1 Protease Mutations on Drug Susceptibility Is Highly Influenced by Complex Interactions with the Background Protease Sequence

... for protease inhibitor (PI) resistance necessitates a better under- standing of the molecular basis of resistance ...Synthetic protease sequences were cloned in a wild-type HIV-1 background to generate a ... See full document

9

Mucosal sensitization to German cockroach involves protease-activated receptor-2

Mucosal sensitization to German cockroach involves protease-activated receptor-2

... This is the first to address the role of PAR-2 in mediat- ing allergic airway inflammation and AHR using a physi- ologically relevant allergen administered in a physiologically relevant manner. A few groups have explored ... See full document

10

Discovery of Anti-2019-nCoV Agents from 38 Chinese Patent Drugs toward Respiratory Diseases via Docking Screening

Discovery of Anti-2019-nCoV Agents from 38 Chinese Patent Drugs toward Respiratory Diseases via Docking Screening

... antiviral drug discovery and development ...main protease is likely to be required to mediate viral replication and transcription through extensive cleavage of two replicase ...main protease ... See full document

26

Characterization of a human immunodeficiency virus type 1 variant with reduced sensitivity to an aminodiol protease inhibitor.

Characterization of a human immunodeficiency virus type 1 variant with reduced sensitivity to an aminodiol protease inhibitor.

... HIV-1 protease is responsible for the specific cleavage of both Gag and Gag-Pol polyproteins and is also required for the assembly and maturation of infectious virions; hence, it is an- other important anti-HIV-1 ... See full document

5

Protease-activated receptor-2 : a novel pathogenic pathway in a murine model of osteoarthritis

Protease-activated receptor-2 : a novel pathogenic pathway in a murine model of osteoarthritis

... Two previously described models of joint instability were employed. 7 The principal model used involved destabilisation of the medial meniscus by section of the medial menisco-tibial ligament (MMTL), which results in ... See full document

16

Threshold Extension of Gallium Arsenide/Aluminum Gallium Arsenide Terahertz Detectors and Switching in Heterostructures

Threshold Extension of Gallium Arsenide/Aluminum Gallium Arsenide Terahertz Detectors and Switching in Heterostructures

... under development by ...new drug-design principles and synthetic ...by protease or inhibitor name (decided by the user), the files of complexes are placed in a ... See full document

193

Protease Activated Receptor-1 Deficiency Diminishes Bleomycin-Induced Skin Fibrosis

Protease Activated Receptor-1 Deficiency Diminishes Bleomycin-Induced Skin Fibrosis

... We used a bleomycin-induced model of skin fibrosis that largely mimics human scleroderma (23). Indeed, der- mal thickening is accompanied by depo- sition of dense packed collagen fibrils that are extensively cross linked ... See full document

7

Neutrophil-targeted, protease-activated pulmonary drug delivery blocks airway and systemic inflammation

Neutrophil-targeted, protease-activated pulmonary drug delivery blocks airway and systemic inflammation

... hydrophobic drug administration to airway PMNs. The protease-sensitive design of the N-in-M system not only allows the microgel to provide the needed aerodynamic size for deposition and geometric size to ... See full document

9

Biochemical Defects of Mutant nudel Alleles Causing Early Developmental Arrest or Dorsalization of the Drosophila Embryo

Biochemical Defects of Mutant nudel Alleles Causing Early Developmental Arrest or Dorsalization of the Drosophila Embryo

... serine protease domain that is specifically required for ventral ...the protease domain of ...the protease domain is required for dorsoventral patterning and that the Nudel protease is ... See full document

11

Modulation of protease-activated receptor expression by Porphyromonas gingivalis in human gingival epithelial cells

Modulation of protease-activated receptor expression by Porphyromonas gingivalis in human gingival epithelial cells

... are activated by their agonist enzymes, thrombin and trypsin or trypsin-like enzymes, in gingival ...growth, development, inflamma- tion, tissue repair and pain ... See full document

8

In Silico Drug Designing of Protease Inhibitors to Find the Potential Drug Candidate for HIV1

In Silico Drug Designing of Protease Inhibitors to Find the Potential Drug Candidate for HIV1

... HIV protease is one of the most important approaches for the therapeutic intervention in HIV infection and their development is regarded as major success of design, HIV attacks on the CD4+ (T helper cells ... See full document

5

Virological Response to Highly Active Antiretroviral Therapy in Patients Infected with Human Immunodeficiency Virus Type 2 (HIV 2) and in Patients Dually Infected with HIV 1 and HIV 2 in The Gambia and Emergence of Drug Resistant Variants

Virological Response to Highly Active Antiretroviral Therapy in Patients Infected with Human Immunodeficiency Virus Type 2 (HIV 2) and in Patients Dually Infected with HIV 1 and HIV 2 in The Gambia and Emergence of Drug Resistant Variants

... Drug development, susceptibility tests, and drug resistance studies have focused almost exclusively on HIV-1; limited work has been done on ...enzymes protease and reverse transcriptase (RT), ... See full document

9

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