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H0396

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Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the...
Hisashi Matsuda et al.
Bioorganic & medicinal chemistry, 17(20), 7313-7323 (2009-09-25)
The 80% aqueous acetone extract from the fruit of Piper chaba (Piperaceae) was found to have hepatoprotective effects on D-galactosamine (D-GalN)/lipopolysaccharide-induced liver injury in mice. From the ethyl acetate-soluble fraction, three new amides, piperchabamides E, G, and H, 33 amides...
Giorgio Ottaviani et al.
Journal of medicinal chemistry, 49(13), 3948-3954 (2006-06-23)
This work was devoted to the search for new artificial membranes allowing a rapid evaluation of passive human skin permeation of compounds with a parallel artificial membrane permeability assay (PAMPA). Effective permeability coefficients (Pe) determined for a set of compounds...
Pil H Lee et al.
Bioorganic & medicinal chemistry letters, 20(1), 69-73 (2009-12-08)
A multiple linear regression QSAR model was developed based on a set of 61 compounds with internally consistent permeability data measured across Franz cell. The data was normalized using a mean permeability value of a reference compound, 3-isobutyl-1-methylxanthine (IBMX). The...
Gianpaolo Chiriano et al.
European journal of medicinal chemistry, 48, 206-213 (2012-01-03)
In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as β-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising...
Mariana P Arce et al.
Journal of medicinal chemistry, 52(22), 7249-7257 (2009-10-28)
Novel multifunctional compounds have been designed, synthesized, and evaluated as potential drugs for the treatment of Alzheimer's disease (AD). With an L-glutamic moiety as a suitable biocompatible linker, three pharmacophoric groups were joined: (1) an N-benzylpiperidine fragment selected to inhibit...
Yohan Choi et al.
Biology of reproduction, 81(6), 1122-1130 (2009-07-31)
Calcium ions have been implicated in the establishment and maintenance of pregnancy, but the regulatory mechanisms of calcium ions in the uterine endometrium and conceptus are not well understood in pigs. Recently, we showed that TRPV6, a calcium ion channel...
Daniel R Goulet et al.
Molecular cancer research : MCR, 18(11), 1685-1698 (2020-08-06)
Triple-negative breast cancers contain a spectrum of epithelial and mesenchymal phenotypes. SUM-229PE cells represent a model for this heterogeneity, maintaining both epithelial and mesenchymal subpopulations that are genomically similar but distinct in gene expression profiles. We identified differential regions of...
Felipe Perozzo Daltoe et al.
Brazilian oral research, 34, e033-e033 (2020-04-09)
The aim of our study was to isolate populations of keratinocyte stem cells based on the expression of cell surface markers and to investigate whether the culture could affect their phenotype. keratinocytes from human oral mucosa were sorted based on...
Irene Zorzan et al.
Nature communications, 11(1), 2364-2364 (2020-05-14)
Human pluripotent stem cells (hPSCs) have the capacity to give rise to all differentiated cells of the adult. TGF-beta is used routinely for expansion of conventional hPSCs as flat epithelial colonies expressing the transcription factors POU5F1/OCT4, NANOG, SOX2. Here we...
Hisashi Matsuda et al.
Bioorganic & medicinal chemistry letters, 18(6), 2038-2042 (2008-02-22)
The methanolic extract from the fruit of Piper chaba (Piperaceae) was found to have a hepatoprotective effect on D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. From the ethyl acetate-soluble fraction, a new amide constituent named piperchabamide E together with twenty...
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds...
Yohan Choi et al.
Asian-Australasian journal of animal sciences, 25(1), 44-51 (2012-01-01)
Calcium ions play an important role in the establishment and maintenance of pregnancy, but molecular and cellular regulatory mechanisms of calcium ion action in the uterine endometrium are not fully understood in pigs. Previously, we have shown that calcium regulatory...
Markus A Lill et al.
Journal of medicinal chemistry, 48(18), 5666-5674 (2005-09-02)
We investigated the influence of induced fit of the androgen receptor binding pocket on free energies of ligand binding. On the basis of a novel alignment procedure using flexible docking, molecular dynamics simulations, and linear-interaction energy analysis, we simulated the...
Muhammad Alimuddin et al.
Journal of medicinal chemistry, 51(16), 5140-5142 (2008-08-01)
A method for log D (pH 7.4) measurement was developed using microfluidic liquid-liquid extraction. Values were determined for 26 compounds and compared to results obtained via shake-flask methods. Excellent correlation between the values obtained via both methods was achieved (R(2)...
Gema C González-Muñoz et al.
European journal of medicinal chemistry, 46(6), 2224-2235 (2011-03-23)
We have previously reported the multifunctional profile of N-(3-chloro-10H-phenothiazin-10-yl)-3-(dimethylamino)propanamide (1) as an effective neuroprotectant and selective butyrylcholinesterase inhibitor. In this paper, we have developed a series of N-acylaminophenothiazines obtained from our compound library or newly synthesised. At micro- and sub-micromolar...
Yong-Hua Wang et al.
Bioorganic & medicinal chemistry letters, 15(18), 4076-4084 (2005-07-02)
In order to determine K(m) values of substrates for CYP3A4-mediated metabolism, an in silico model has been developed in the present work. Using electrotopological state (E-state) indices, together with Bayesian-regularized neural network (BRNN), we have described an in silico method...
Alfonso Pérez-Garrido et al.
Bioorganic & medicinal chemistry, 17(2), 896-904 (2008-12-06)
This paper reports a QSAR study for predicting the complexation of a large and heterogeneous variety of substances (233 organic compounds) with beta-cyclodextrins (beta-CDs). Several different theoretical molecular descriptors, calculated solely from the molecular structure of the compounds under investigation...
Artem Cherkasov et al.
Journal of medicinal chemistry, 51(7), 2047-2056 (2008-03-12)
A benchmark data set of steroids with known affinity for sex hormone-binding globulin (SHBG) has been widely used to validate popular molecular field-based QSAR techniques. We have expanded the data set by adding a number of nonsteroidal SHBG ligands identified...
Tadashi Honda et al.
Journal of medicinal chemistry, 54(6), 1762-1778 (2011-03-03)
Forty-four novel tricycles containing nonenolizable cyano enones (TCEs) were designed and synthesized on the basis of a semisynthetic pentacyclic triterpenoid, bardoxolone methyl, which is currently being developed in phase II clinical trials for the treatment of severe chronic kidney disease...
Christopher A Elkins et al.
Antimicrobial agents and chemotherapy, 51(3), 923-929 (2007-01-11)
AcrAB-TolC is the major, constitutively expressed tripartite multidrug efflux system in Escherichia coli that recognizes various structurally unrelated molecules, including many antibiotics, dyes, and steroids. The AcrB inner membrane pump portion of the efflux system has been shown in recent...
Kamel A Metwally et al.
European journal of medicinal chemistry, 42(2), 152-160 (2006-10-21)
Two series of 1,2,4-triazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles derived from three selected arylpropionic acids namely, ibuprofen, flurbiprofen and naproxen, were synthesized and evaluated for anti-inflammatory activity and ulcerogenic potential. All the tested compounds exhibited anti-inflammatory activity comparable to that of hydrocortisone. Compared...
Marjan Van Cleemput et al.
Journal of natural products, 72(6), 1220-1230 (2009-05-30)
Hop acids, a family of bitter compounds derived from the hop plant (Humulus lupulus), have been reported to exert a wide range of effects, both in vitro and in vivo. They exhibit potential anticancer activity by inhibiting cell proliferation and...
Veena Padmanaban et al.
Nature protocols, 15(8), 2413-2442 (2020-07-22)
Cancer invasion and metastasis are challenging to study in vivo since they occur deep inside the body over extended time periods. Organotypic 3D culture of fresh tumor tissue enables convenient real-time imaging, genetic and microenvironmental manipulation and molecular analysis. Here...
Nimrod Elazar et al.
Neuron, 101(2), 224-231 (2018-12-16)
The initiation of axoglial contact is considered a prerequisite for myelination, yet the role cell adhesion molecules (CAMs) play in mediating such interactions remains unclear. To examine the function of axoglial CAMs, we tested whether enhanced CAM-mediated adhesion between OLs...
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this...
Stine M Andersen et al.
Carcinogenesis, 31(8), 1483-1490 (2010-06-18)
Valrubicin is a second generation anthracycline characterized by an excellent safety profile presenting no skin toxicity or necrosis upon contact. In its current liquid formulation (Valstar; Indevus Pharmaceuticals, Lexington, MA), it is approved solely for the treatment of bladder cancer....
Pelayo Camps et al.
Journal of medicinal chemistry, 52(17), 5365-5379 (2009-08-12)
Two isomeric series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase, AChE-induced and self-induced beta-amyloid (Abeta) aggregation, and beta-secretase (BACE-1) and to cross blood-brain barrier. The new hybrids...
Alexander Kanitz et al.
PloS one, 7(11), e49568-e49568 (2012-11-21)
Vascular endothelial growth factor A (VEGFA) plays a key role in the angiogenesis of human skin. Elevated levels of VEGFA are associated with several pathological conditions, including chronic inflammatory skin diseases and several types of skin cancer. In particular, squamous...
Heewon Seo et al.
Biology of reproduction, 84(2), 279-287 (2010-10-01)
Uterine secretions are essential for the development of the conceptus during pregnancy. In pigs, various molecules, including transport proteins, growth factors, enzymes, and extracellular matrix proteins, are secreted into the uterine lumen. Our previous work identified salivary lipocalin (SAL1), a...
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