Tumor Supernatant Derived from Hepatocellular Carcinoma Cells Treated with Vincristine Sulfate have Therapeutic Activity.

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Vincristine sulfate (VCR), a commonly used chemotherapeutic agent, kills cancer cells as well as the normal cells for its cytotoxicity. But it is still unclear whether it can exert therapeutic […]

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Safety of Nebulized Colistin Solution as Adjunctive Treatment of Lower Respiratory Tract Infections.

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Systemic colistin is often utilized for management of drug resistant lower respiratory tract infections (LRTI). Nebulized administration of colistin allows direct instillation of active agent to maximize concentrations and limit […]

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Optimizing pharmacology studies in pregnant and lactating women using lessons from HIV: a consensus statement.

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Information on the extent of drug exposure to mothers and infants during pregnancy and lactation normally becomes available years after regulatory approval of a drug. Clinicians face knowledge gaps on […]

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The GABAB receptor positive allosteric modulator COR659: in vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives.

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We report an in vitro phase I metabolism study on COR659 (1), a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of […]

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Enhanced cellular uptake of platinum by a tetracationic Pt(II) nanocapsule and its implications to cancer treatment.

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Despite the known limitations of cisplatin chemotherapy, the treatment of cancer by platinum-based drugs remains the method of choice for many oncologists. The advancement in drug delivery formulations and protocols […]

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Biocompatibility and mechanical properties evaluation of chitosan films containing an N-acylhydrazonic derivative.

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The N-acylhydrazone subunit is considered a privileged structure in medicinal chemistry for its importance in pharmaceutical research. Also, alternative methods to deliver these molecules have a great pharmaceutical interest. Therefore, […]

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A New Drug Testing Platform Based on 3D Tri-culture in Lab-on-a-chip Devices.

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Drug discovery has a 90% rate of failure because preclinical platforms for drug testing do not mimic the in vivo conditions. Doxorubicin (DOX) is a commonly used drug to treat […]

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The GABAB receptor positive allosteric modulator COR659: in vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives.

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We report an in vitro phase I metabolism study on COR659 (1), a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of […]

» Read more

Enhanced cellular uptake of platinum by a tetracationic Pt(II) nanocapsule and its implications to cancer treatment.

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Despite the known limitations of cisplatin chemotherapy, the treatment of cancer by platinum-based drugs remains the method of choice for many oncologists. The advancement in drug delivery formulations and protocols […]

» Read more

Biocompatibility and mechanical properties evaluation of chitosan films containing an N-acylhydrazonic derivative.

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The N-acylhydrazone subunit is considered a privileged structure in medicinal chemistry for its importance in pharmaceutical research. Also, alternative methods to deliver these molecules have a great pharmaceutical interest. Therefore, […]

» Read more

A New Drug Testing Platform Based on 3D Tri-culture in Lab-on-a-chip Devices.

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Drug discovery has a 90% rate of failure because preclinical platforms for drug testing do not mimic the in vivo conditions. Doxorubicin (DOX) is a commonly used drug to treat […]

» Read more

In Silico Toxicity Evaluation of Salubrinal and its Analogues.

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This paper reports on a comprehensive in silico toxicity assessment of Salubrinal and its analogues containing a cinnamic acid residue or quinoline ring using the online servers admetSAR, ADMETlab, ProTox, […]

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Changing the Clinical Paradigm of Hydroxyurea Treatment for Sickle Cell Anemia through Precision Medicine.

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Sickle cell anemia (SCA) is a common and devastating inherited blood disorder, affecting millions of people across the world. Without treatment, SCA results in tremendous morbidity and early mortality. Hydroxyurea […]

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Heterologous expression of biologically active Mambalgin-1 peptide as a new potential anticancer, using a PVX-based viral vector in Nicotiana benthamiana.

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Mambalgin-1 is a peptide that acts as a potent analgesic through inhibiting acid-sensing ion channels (ASIC) in nerve cells. Research has shown that ASIC channels are involved in the proliferation […]

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Ester Derivatives of Phyllohydroquinone Effectively Deliver the Active Form of Vitamin K1 Topically, Owing to Their Non-Photosensitivity.

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Topical application of phylloquinone (PK) is beneficial to the skin; however, its topical use is limited in Europe owing to its photosensitive properties such as photodegradation and phototoxicity. We evaluated […]

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Comparison and identification of metabolic profiling of bicyclol in rats, dogs and humans in vitro and in vivo.

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Bicyclol, a novel hepatoprotective agent, has been widely used to treat chronic viral hepatitis and drug-induced liver injury (DILI). However, its metabolic characteristics remains to be explored, especially in humans. […]

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Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.

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Cancer is a heterogeneous disease, and its treatment requires the identification of new ways to thwart tumor cells. Amongst such emerging targets are glucose transporters (GLUTs, SLC2 family), which are […]

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Cinnamic acid derivatives as chemosensitising agents against DOX-treated lung cancer cells – involvement of carbonyl reductase 1.

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Doxorubicin (DOX) therapy is limited by both cancer cells resistance and cardiotoxicity. DOX biotransformation to doxorubicinol (DOXol) by reductases enzymes (mainly by CBR1; carbonyl reductase 1) is a key process […]

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Fluorinated benzylidene indanone exhibits antiproliferative activity through modulation of microtubule dynamics and antiangiogenic activity.

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The application of fluorine in drug design has been understood significantly by the medicinal chemists in recent years. Modulation of tubulin-microtubule dynamics is one of the most effective targets for […]

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Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2C9 and HLA-B Genotypes and Phenytoin Dosing: 2020 Update.

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Phenytoin is an antiepileptic drug with a narrow therapeutic index and large inter-patient pharmacokinetic variability, partly due to genetic variation in CYP2C9. Furthermore, the variant allele HLA-B*15:02 is associated with […]

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Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2C19 and Proton Pump Inhibitor Dosing.

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Proton pump inhibitors (PPIs) are widely used for acid suppression in the treatment and prevention of many conditions including gastroesophageal reflux disease, gastric and duodenal ulcers, erosive esophagitis, H. pylori […]

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Protective Effects of Δ9-Tetrahydrocannabinol Against Enterotoxin-induced Acute Respiratory Distress Syndrome is Mediated by Modulation of Microbiota.

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Staphylococcal enterotoxin-B (SEB) is one of the most potent bacterial superantigens that exerts profound toxic effects by inducing cytokine storm. When SEB is inhaled, it can cause Acute Respiratory Distress […]

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Quantitative Systems Toxicology Modeling Predicts that Reduced Biliary Efflux Contributes to Tolvaptan Hepatotoxicity.

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Patients with autosomal dominant polycystic kidney disease (ADPKD) exhibit enhanced susceptibility to tolvaptan hepatotoxicity relative to other patient populations. In a rodent model of ADPKD, the expression and function of […]

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The low-expression programming of 11β-HSD2 mediates osteoporosis susceptibility induced by prenatal caffeine exposure in male offspring rats.

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Prenatal caffeine exposure (PCE) can cause developmental toxicity of long bones in offspring, but the long-term effects and the underlying mechanism has not been fully clarified. Here, we investigated the […]

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