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PubMed Journals Articles About "Small Molecule Shows Marked Activity Against Ibrutinib Resistant" RSS

10:04 EDT 20th June 2019 | BioPortfolio

Small Molecule Shows Marked Activity Against Ibrutinib Resistant PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Small Molecule Shows Marked Activity Against Ibrutinib Resistant articles that have been published worldwide.

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Showing "Small Molecule Shows Marked Activity Against Ibrutinib Resistant" PubMed Articles 1–25 of 32,000+

The Muddied Waters of Ibrutinib Therapy.

A 37-year-old male was admitted with an atypical presentation of central nervous system (CNS) aspergillosis while on ibrutinib therapy for a CNS relapse of mantle cell lymphoma. This case highlights the importance of a high clinical suspicion of opportunistic infections in patients receiving small-molecule kinase inhibitors. This report includes a review of reported cases of Aspergillus infections in patients receiving ibrutinib and the shared features of these cases.


TAK1 is a druggable kinase for diffuse large B-cell lymphoma.

Diffuse large B-cell lymphoma (DLBCL) is the most common form of lymphoma, and up to 30% DLBCL patients eventually died by using first-line chemotherapy regimens. Currently, Bruton tyrosine kinase (BTK) inhibitor (ibrutinib) is one of the most promising medicine in clinical trials for DLBCL, to which about 25% of patients with relapsed or refractory DLBCL are responsive. Thus, it is urgent to discover new druggable targets for DLBCL, especially for patients who are unresponsive to first-line chemotherapy an...

Fluorescent peptide displacement as a general assay for screening small molecule libraries against RNA.

A prominent hurdle in developing small molecule probes against RNA is the relative scarcity of general screening methods. In this study, we demonstrate the application of a fluorescent peptide displacement assay to screen small molecule probes against four different RNA targets. The designed experimental protocol combined with statistical analysis provides a fast and convenient method to simultaneously evaluate small molecule libraries against different RNA targets and classify them based on affinity and se...


The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.

The p53 gene, a well-known tumor suppressor gene, plays a crucial role in cell cycle regulation, DNA repair, cell differentiation, and apoptosis. MDM2 exerts p53-dependent activity mainly by binding to p53 protein to form MDM2-p53 negative feedback loop. In addition, MDM2 is involved in a number of pathways that regulate cell proliferation and apoptosis, playing a p53-independent role. The p53 binding domain of MDMX bind to p53 transcriptional activation domain, inhibiting the transcriptional activity of p5...

Small molecules as inhibitors of PCSK9: Current status and future challenges.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in regulating lipoprotein metabolism by binding to low-density lipoprotein receptors (LDLRs), leading to their degradation. LDL cholesterol (LDL-C) lowering drugs that operate through the inhibition of PCSK9 are being pursued for the management of hypercholesterolemia and reducing its associated atherosclerotic cardiovascular disease (CVD) risk. Two PCSK9-blocking monoclonal antibodies (mAbs), alirocumab and evolocumab, were appro...

Dually Cross-Linked Supramolecular Hydrogel as Surface Plasmon Resonance Sensor for Small Molecule Detection.

Dually cross-linked supramolecular hydrogels (DCSH) are designed to show responsive properties while maintaining the gel structure by introducing two different kinds of cross-links. This is realized by utilizing a photo-cross-linker for permanent cross-linking and β-cyclodextrin (β-CD) and ferrocene (Fc) as host-guest recognition pair. The DCSH shows increased swelling in the presence of the small target molecule adamantane amine (Ada). Ada can break the non-covalent bonding between β-CD and Fc through c...

Identification of 2(1H)-pyrimidinones as potential EGFR T790M inhibitors for the treatment of gefitinib-resistant non-small cell lung cancer.

A new class of 2(1H)-pyrimidinone derivatives was identified as potential EGFR T790M inhibitors against TKI-resistant NSCLC. These novel compounds inhibited the EGFR T790M kinase activity at concentrations in the range of 85.3 to 519.9 nM. In particular, compound 7e exhibited the strongest activity against both EGFR (IC = 96.9 nM) and EGFR (IC = 85.3 nM) kinases in the cells. Compared with inhibitor 7e, compound 7b displayed enhanced antiproliferative activity against gefitinib-resistant H1975...

Antibacterial activity of naphthyl derived bis-(3-hydroxy-4-pyridinonate) copper(II) complexes against multidrug-resistant bacteria.

In this work, we report the synthesis and characterization of three novel copper(II) complexes of naphthyl derived 3-hydroxy-4-pyridinone chelators. Their antibacterial activity against several Gram-positive and Gram-negative reference strains and multidrug-resistant clinical isolates was assessed through determination of the minimum inhibitory concentration (MIC). The complex Cu(naph1pp) shows the highest antibacterial activity, including against multidrug-resistant isolates, nonetheless, being more active...

The effect of naringenin on the pharmacokinetics of ibrutinib in rat: a drug-drug interactions study.

The aim of this study was to investigate the effect of naringenin on the pharmacokinetics of ibrutinib in rats. A simple and sensitive quantitation method based on ultra-high performance liquid chromatography-Q-Exactive Orbitrap tandem mass spectrometry was developed and validated for t determination of ibrutinib in rat plasma. The samples were extracted using ethyl acetate containing 1% triethylamine and the separated on a Waters ACQUITY UPLC BEH C column with acetonitrile and water containing 0.1% formic ...

Ibrutinib increases the risk of hypertension and atrial fibrillation: Systematic review and meta-analysis.

Ibrutinib is an oral covalent inhibitor of Bruton's tyrosine kinase approved for the treatment of patients with chronic lymphocytic leukemia (CLL), mantle cell lymphoma and Waldenstrӧm's macroglobulinemia. Ibrutinib has an increased risk of atrial fibrillation but the mechanism is unknown, and hypertension may play a role in the pathogenesis of this adverse drug reaction.

Small Molecule Potentiation of Gram-positive Selective Antibiotics Against Acinetobacter baumannii.

In 2016, the World Health Organization deemed antibiotic resistance one of the biggest threats to global health, food security, and development. The need for new methods to combat infections caused by antibiotic resistant pathogens will require a variety of approaches to identifying effective new therapeutic strategies. One approach is the identification of small molecule adjuvants that potentiate the activity of antibiotics of demonstrated utility, whose efficacy is abated by resistance, both acquired and ...

Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells.

Inhibition of ubiquitin ligases with small molecule remains a very challenging task, given the lack of catalytic activity of the target and the requirement of disruption of its interactions with other proteins. Siah1/2, which are E3 ubiquitin ligases, are implicated in melanoma and prostate cancer and represent high-value drug targets. We utilized three independent screening approaches in our efforts to identify small-molecule Siah1/2 inhibitors: Affinity Selection-Mass Spectrometry, a protein thermal shift...

An inhibitory compound produced by a soil isolate of Rhodococcus has strong activity against the veterinary pathogen R. equi.

Complete genome sequencing of dozens of strains of the soil bacterium Rhodococcus has revealed the presence of many cryptic biosynthetic gene clusters, presumably dedicated to the production of small molecules. This has sparked a renewed interest in this underexplored member of the Actinobacteria as a potential source of new bioactive compounds. Reported here is the discovery of a potent inhibitory molecule produced by a newly isolated strain of Rhodococcus, strain MTM3W5.2. This small inhibitory molecule s...

Small molecule targeting of RNA structures in neurological disorders.

Aberrant RNA structure and function operate in neurological disease progression and severity. As RNA contributes to disease pathology in a complex fashion, that is, via various mechanisms, it has become an attractive therapeutic target for small molecules and oligonucleotides. In this review, we discuss the identification of RNA structures that cause or contribute to neurological diseases as well as recent progress toward the development of small molecules that target them, including small molecule modulato...

Randomized Phase III Trial of Ibrutinib and Rituximab Plus Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone in Non-Germinal Center B-Cell Diffuse Large B-Cell Lymphoma.

Ibrutinib has shown activity in non-germinal center B-cell diffuse large B-cell lymphoma (DLBCL). This double-blind phase III study evaluated ibrutinib and rituximab plus cyclophosphamide, doxorubicin, vincristine, and prednisone (R-CHOP) in untreated non-germinal center B-cell DLBCL.

Triarylmethane Fluorophores Resistant to Oxidative Photobluing.

Spectral stability of small-molecule fluorescent probes is required for correct interpretation and reproducibility of multicolor fluorescence imaging data, in particular under high (de)excitation light intensities of super-resolution imaging or in single-molecule applications. We propose a synthetic approach to a series of spectrally stable rhodamine fluorophores based on sequential Ru- and Cu-catalyzed transformations, evaluate their stability against photobleaching and photoconversion in context of other ...

Urinary bactericidal activity of colistin and azidothymidine combinations against mcr-1 positive colistin-resistant Escherichia coli.

A phase 1 clinical study was performed to assess pharmacokinetics and safety of IV administration of colistin-methanesulfonate (CMS) and azidothymidine (AZT) alone and in combination. Seven healthy subjects received 3-times (q12) 1h-IV-infusions of 4, 2 and 2 million international units (MIU) CMS co-administered with 200, 100 and 100 mg AZT, respectively. In the ex vivo study, urinary bactericidal titer (UBT) and time-kill curve determinations were performed in artificial urine, spiked with colistin-sulpha...

Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction.

Protein-protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin ligases are critical to cellular function. There is significant therapeutic potential in the development of small molecules that modulate these interactions; however, rational design of small molecule enhancers of PPIs remains elusive. Herein, we report the prospective identification and rational design of potent small molecules that enhance the interaction between an oncogenic transcription factor, β-Catenin, and i...

Ruthenium(II) polypyridyl complex Ru(phen)dppz-idzo as a colorimetric molecular "light switch" and powerful stabilizer for the RNA triplex poly(U)·poly(A)*poly(U).

The interaction of [Ru(phen)dppz-idzo] (phen = 1,10-phenanthroline, dppz-idzo = dppz-imidazolone) with triplex RNA poly(U)·poly(A)*poly(U) was carried out by using spectroscopic and viscometric techniques in this work. Luminescent titrations suggest that [Ru(phen)dppz-idzo] shows better selectivity for poly(U)·poly(A)*poly(U) compared with poly(U)·poly(A) and poly(U), this complex exhibits a "light switch" effect with an emission enhancement factor of about 123 in the presence of poly(U)·poly(A)...

The Syk inhibitor R406 is a modulator of P-glycoprotein (ABCB1)-mediated multidrug resistance.

In a previously published study, higher levels of spleen tyrosine kinase (Syk) were observed in recurrent post-chemotherapy ovarian cancers compared to primary tumors. Syk inhibition was found to stabilize microtubules and potentiate paclitaxel activity in cellular models of taxane-resistant ovarian cancers. We further studied the effects of Syk inhibition on paclitaxel activity in Syk(+) ovarian cancer cell models and in variants selected for taxane resistance. Syk inhibition was accomplished using RNAi an...

General Pharmacokinetic Features of Small-Molecule Compounds Exhibiting Target-Mediated Drug Disposition (TMDD): A Simulation-Based Study.

Although target-mediated drug disposition (TMDD) can occur in both large- and small-molecule compounds, TMDD in small-molecule compounds has received much less attention due to its lower prevalence. To facilitate the identification of nonlinear pharmacokinetics of small-molecule compounds caused by TMDD, a comprehensive simulation was conducted in the current study to provide the general pharmacokinetic features of small-molecule compounds exhibiting TMDD. Various conditions, including single escalating int...

Transient Incomplete Separation Facilitates Finding Accurate Equilibrium Dissociation Constant of Protein-Small Molecule Complex.

Current practical methods for finding the equilibrium dissociation constant, Kd, of protein-small molecule complexes are mainly biosensoric and calorimetric. They have inherent sources of inaccuracy; immobilization of molecules on sensors and heat of side reactions often lead to dramatic errors in Kd. We introduce "accurate constant via transient incomplete separation" (ACTIS), a non-biosensoric and non-calorimetric approach for finding Kd, which appears to be free of inherent sources of inaccuracy. Concept...

Ibrutinib discontinuation in patients with relapsed or refractory chronic lymphocytic leukemia treated in a compassionate use program: A report from the Polish Adult Leukemia Study Group (PALG).

Development of a novel class of drugs, the B-cell receptor-signaling inhibitors, including ibrutinib, has been a major achievement in the therapy of refractory or relapsed chronic lymphocytic leukemia (CLL). However, the CLL patients who have discontinued the ibrutinib treatment in clinical trials have been reported to have poor prognosis.

PAK4 regulates stemness and progression in endocrine resistant ER-positive metastatic breast cancer.

Despite the effectiveness of endocrine therapies to treat estrogen receptor-positive (ER+) breast tumours, two thirds of patients will eventually relapse due to de novo or acquired resistance to these agents. Cancer Stem-like Cells (CSCs), a rare cell population within the tumour, accumulate after anti-estrogen treatments and are likely to contribute to their failure. Here we studied the role of p21-activated kinase 4 (PAK4) as a promising target to overcome endocrine resistance and disease progression in E...

Ibrutinib and Venetoclax for First-Line Treatment of CLL.

Ibrutinib, an inhibitor of Bruton's tyrosine kinase, and venetoclax, an inhibitor of B-cell lymphoma 2 protein, have been approved for patients with chronic lymphocytic leukemia (CLL). Preclinical investigations have indicated potential synergistic interaction of their combination.


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