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Showing 1-30 of 431 results for "C9754" within Papers
I Grattagliano et al.
Clinical pharmacology and therapeutics, 95(1), 89-97 (2013-07-23)
Familial Mediterranean fever (FMF), an inherited autosomal recessive disorder, is characterized by sporadic, paroxysmal attacks of fever and serosal inflammation, lasting 1-3 days. Patients may develop renal amyloidosis, arthritis, serositis, and skin and oral lesions. Diagnosis is based on clinical
Giuseppe La Regina et al.
Journal of medicinal chemistry, 54(24), 8394-8406 (2011-11-03)
New arylthioindoles (ATIs) were obtained by replacing the 2-alkoxycarbonyl group with a bioisosteric 5-membered heterocycle nucleus. The new ATIs 5, 8, and 10 inhibited tubulin polymerization, reduced cell growth of a panel of human transformed cell lines, and showed higher
Bing-Hua Su et al.
Oncotarget, 6(35), 38308-38326 (2015-10-31)
Conditionally replicating adenoviruses (CRAds), or oncolytic adenoviruses, such as E1B55K-deleted adenovirus, are attractive anticancer agents. However, the therapeutic efficacy of E1B55K-deleted adenovirus for refractory solid tumors has been limited. Environmental stress conditions may induce nuclear accumulation of YB-1, which occurs
Isabel Lozoya-Agullo et al.
Journal of pharmaceutical sciences, 104(9), 3136-3145 (2015-04-22)
Our aim is to develop and to validate the in situ closed loop perfusion method in rat colon and to compare with small intestine and Caco-2 cell models. Correlations with human oral fraction absorbed (Fa) and human colon fraction absorbed
[Organ damage in collagen vascular diseases: toward the understanding of the complicated conditions (discussion)].
Seiji Minota et al.
Nihon Naika Gakkai zasshi. The Journal of the Japanese Society of Internal Medicine, 102(10), 2653-2666 (2014-01-10)
Fatma M Abdel Bar et al.
Bioorganic & medicinal chemistry, 18(2), 496-507 (2009-12-26)
Cell invasion and migration are required for the parent solid tumor cells to metastasize to distant organs. Microtubules form a polarized network, enabling organelle and protein movement throughout the cell. Cytoskeletal elements coordinately regulate cell's motility, adhesion, migration, exocytosis, endocytosis
SangJoon Lee et al.
Nature, 597(7876), 415-419 (2021-09-03)
Inflammasomes are important sentinels of innate immune defence, sensing pathogens and inducing cell death in infected cells1. There are several inflammasome sensors that each detect and respond to a specific pathogen- or damage-associated molecular pattern (PAMP or DAMP, respectively)1. During
S Sahin et al.
European review for medical and pharmacological sciences, 17(7), 958-963 (2013-05-04)
Familial Mediterranean fever is an auto-inflammatory disorder. Long term complications of the disease include decreased quality of life. The measurement of quality of life in the patients with chronic disease has become an important research topic during the last years.
Se-Jin Jeong et al.
Autophagy, 17(11), 3740-3752 (2021-03-13)
The autophagy-lysosome system is an important cellular degradation pathway that recycles dysfunctional organelles and cytotoxic protein aggregates. A decline in this system is pathogenic in many human diseases including neurodegenerative disorders, fatty liver disease, and atherosclerosis. Thus there is intense
Eva Cabet et al.
PloS one, 10(9), e0137009-e0137009 (2015-09-04)
Desminopathies, a subgroup of myofibrillar myopathies (MFMs), the progressive muscular diseases characterized by the accumulation of granulofilamentous desmin-positive aggregates, result from mutations in the desmin gene (DES), encoding a muscle-specific intermediate filament. Desminopathies often lead to severe disability and premature
Wen-Kai Yang et al.
Journal of morphology, 277(8), 1113-1122 (2016-05-31)
The tilapia (Oreochromis mossambicus) is a euryhaline fish exhibiting adaptive changes in cell size, phenotype, and ionoregulatory functions upon salinity challenge. Na(+) /Cl(-) cotransporter (NCC) and Na(+) /K(+) /2Cl(-) cotransporter (NKCC) are localized in the apical and basolateral membranes of
Marek T Konieczny et al.
European journal of medicinal chemistry, 89, 733-742 (2014-12-03)
Synthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol-5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site.
Ruili Huang et al.
Journal of medicinal chemistry, 49(6), 1964-1979 (2006-03-17)
This paper examines two biological models of anticancer activity, cytotoxicity and hollow fiber (HF) activity, for chemotherapeutic agents evaluated as part of the National Cancer Institute's (NCI's) drug screening effort. Our analysis proposes strategies to globally assess compounds tested in
J M Andreu et al.
Biochemistry, 37(23), 8356-8368 (1998-06-19)
The roles of the methoxy substituents on ring A of two ring colchicine (COL) analogues were probed by the synthesis of a number of drugs and the examination of their effect on binding to tubulin, inhibition of microtubule assembly, and
Takeki Uehara et al.
Molecular nutrition & food research, 54(2), 218-227 (2009-12-31)
Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted approach for identifying chemicals with potential safety problems. Gene expression profiling is expected to
J Fediuk et al.
Pulmonary pharmacology & therapeutics, 30, 1-10 (2014-10-15)
Persistent Pulmonary Hypertension of the Newborn (PPHN) is characterized by sustained vasospasm and an increased thromboxane:prostacyclin ratio. Thromboxane (TP) receptors signal via Gαq to mobilize IP3 and Ca(2+), causing pulmonary arterial constriction. We have previously reported increased TP internalization in
Spyridon Deftereos et al.
Journal of the American College of Cardiology, 61(16), 1679-1685 (2013-03-19)
This study sought to test the hypothesis that colchicine treatment after percutaneous coronary intervention (PCI) can lead to a decrease in in-stent restenosis (ISR). ISR rates are particularly high in certain patient subsets, including diabetic patients, especially when a bare-metal
A randomized trial of colchicine for acute pericarditis.
Massimo Imazio et al.
The New England journal of medicine, 370(8), 781-781 (2014-02-21)
Jenny M Pedersen et al.
Journal of medicinal chemistry, 51(11), 3275-3287 (2008-05-07)
The chemical space of registered oral drugs was explored for inhibitors of the human multidrug-resistance associated protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and drug-like compounds. The data set included a new reference set
Raisa I Krutilina et al.
Cancers, 14(21) (2022-11-12)
HER2+ breast cancer accounts for 15% of all breast cancer cases. Current frontline therapy for HER2+ metastatic breast cancer relies on targeted antibodies, trastuzumab and pertuzumab, combined with microtubule inhibitors in the taxane class (paclitaxel or docetaxel). It is well
Mallinath B Hadimani et al.
Journal of natural products, 76(9), 1668-1678 (2013-09-11)
The natural products colchicine and combretastatin A-4 are potent inhibitors of tubulin assembly, and they have inspired the design and synthesis of a large number of small-molecule, potential anticancer agents. The indole-based molecular scaffold is prominent among these SAR modifications
Aleem Gangjee et al.
Journal of medicinal chemistry, 50(14), 3290-3301 (2007-06-15)
We have discovered a novel series of 7-benzyl-4-methyl-5-[(2-substituted phenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidin-2-amines, which possess antimitotic and antitumor activities against antimitotic-sensitive as well as resistant tumor cells. These agents bind to a site on tubulin that is distinct from the colchicine, vinca alkaloid, and
Yaqin Zhu et al.
Pharmaceutical research, 31(12), 3289-3303 (2014-05-27)
Using different chain lengths of PEG as linkers to develop a novel folate (FA) and TAT peptide co-modified doxorubicin (DOX)-loaded liposome (FA/TAT-LP-DOX) and evaluate its potential for tumor targeted intracellular drug delivery. FA/TAT-LP-DOX was prepared by pH gradient method and
V Helsen et al.
Acta clinica Belgica, 68(2), 113-115 (2013-08-24)
A 83-year-old woman was admitted to hospital with chest pain, fever, dry cough and palpitations. Chest X-ray revealed a pleural effusion, assumed to be caused by cardiac failure and respiratory infection. Despite treatment with antibiotics and diuretics, the pleural effusion
Timothy J Hibberd et al.
The Journal of comparative neurology, 530(18), 3209-3225 (2022-09-01)
Quantitative data of biological systems provide valuable baseline information for understanding pathology, experimental perturbations, and computational modeling. In mouse colon, calcitonin gene-related peptide (CGRP) is expressed by myenteric neurons with multiaxonal (Dogiel type II) morphology, characteristic of intrinsic primary afferent
R De Vincenzo et al.
Anti-cancer drug design, 13(1), 19-33 (1998-02-25)
In this study the in vitro antitumor activity of a series of 20 colchicine analogues was tested and compared with colchicine and thiocolchicine on three different human cancer cell lines, two of which express the multidrug-resistance (MDR) phenotype. At concentrations
R F Ludueña et al.
Current opinion in cell biology, 4(1), 53-57 (1992-02-01)
In the past year, much has been learned about structure-function correlations in the tubulin molecule, and specifically about the nature and roles of post-translational modifications and tubulin isotypes. The interactions between tubulin and its ligands--both microtubule-associated proteins and anti-mitotic drugs--are
Ryuji Uchida et al.
The Journal of antibiotics, 67(11), 777-781 (2014-06-12)
A small molecule named habiterpenol produced by actinomycete Phytohabitans suffuscus 3787_5 was found to abrogate bleomycin-induced G2 arrest in Jurkat cells. Habiterpenol showed no cytotoxic effect on Jurkat cells even at 273 μM; however, the compound inhibited bleomycin-induced G2 arrest in
Sung Hoon Lee et al.
Cell systems, 13(7), 514-529 (2022-06-10)
Navigation through a dense, physically confining extracellular matrix is common in invasive cell spread and tissue reorganization but is still poorly understood. Here, we show that this migration is mediated by cyclic changes in the activity of a small GTPase
Luca Dainese et al.
Journal of cardiothoracic surgery, 6, 96-96 (2011-08-13)
Pericardial effusion represents a common postoperative complication in cardiac surgery. Nonetheless, it can be resistant to conventional therapy leading to prolonged in-hospital stay and worsening of clinical conditions. Recent literature shows that colchicine therapy should be useful in the treatment
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