Regulation of integrin and growth factor signaling in biomaterials for osteodifferentiation

• Qiang Wei,
• Theresa L. M. Pohl,
• Anja Seckinger,
• Joachim P. Spatz and
• Elisabetta A. Cavalcanti-Adam

Beilstein J. Org. Chem. 2015, 11, 773–783, doi:10.3762/bjoc.11.87

• ; growth factor; integrin; osteodifferentiation; stem cells; Review Introduction Current bone grafting therapeutics do not provide satisfying solutions to the problems of non-healing bone defects. The gold-standard therapy is the grafting of autologous bone; however, it is limited by low availability as

• stable gradients of growth factors to regulate their bioavailability [11]. This matrix-immobilization of the factors might result in long-term binding to cell surface receptors, since the binding affinity of ECM-factors is relatively weak compared to growth factor receptor interactions [8]. Moreover, the

• factors can be released upon matrix turnover and degradation. It has been proven that a large number of growth factors can induce bone healing [9], for example, bone morphogenetic proteins (BMPs) [12], transforming growth factor beta (TGF-β) [13], fibroblast growth factors (FGFs) [14], vascular

Exploring monovalent and multivalent peptides for the inhibition of FBP21-tWW

• Lisa Maria Henning,
• Sumati Bhatia,
• Miriam Bertazzon,
• Michaela Marczynke,
• Oliver Seitz,
• Rudolf Volkmer,
• Rainer Haag and
• Christian Freund

Beilstein J. Org. Chem. 2015, 11, 701–706, doi:10.3762/bjoc.11.80

• endothelial growth factor (VEGF). In the same study, the natural compound borrelidin was suggested to confer its splicing inhibition function by directly binding to the WW domains of FBP21 [6]. Here, we have taken a different approach to inhibit binding of FBP21-tWW to proline-rich sequences in the

Potential of acylated peptides to target the influenza A virus

• Daniel Lauster,
• Damian Pawolski,
• Julian Storm,
• Kai Ludwig,
• Rudolf Volkmer,
• Henry Memczak,
• Andreas Herrmann and
• Sumati Bhatia

Beilstein J. Org. Chem. 2015, 11, 589–595, doi:10.3762/bjoc.11.65

• has not been explored much in the context of virus inhibition. There are only a few reports on using peptide based self-assembly for influenza virus inhibition [12][13][14]. The entry blocker (EB) which is a peptide fragment derived from the fibroblast growth factor signal sequence 4 (FGF) has a

Natural phenolic metabolites with anti-angiogenic properties – a review from the chemical point of view

• Qiu Sun,
• Jörg Heilmann and
• Burkhard König

Beilstein J. Org. Chem. 2015, 11, 249–264, doi:10.3762/bjoc.11.28

• , the tumor cells express pro-angiogenic factors including growth factors such as the vascular endothelial growth factor (VEGF) and fibroblast growth factor (FGF) and enzymes such as cyclooxygenase 2 (COX-2) and protein kinase A (PKA) as well as signaling molecules such as integrins. The evoked cascade

• expression of vascular endothelial growth factor (VEGF) and matrix metalloproteinase (MMP)-9 decreased compared to the controls. No influence on the normal behavior of the animals was observed. In general, HBA represents an interesting anti-angiogenic agent for the treatment of angiogenic diseases. Curcumin

• plants [92]. In a number of early studies [93][94], quercetin showed a strong ability to inhibit tumor growth in vivo. Quercetin suppresses angiogenesis through multiple mechanisms such as inhibition of COX-2 and lipoxygenase (LOX)-5, interference with the EGF receptor, the human epidermal growth factor

An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles

• Marcus Baumann and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2013, 9, 2265–2319, doi:10.3762/bjoc.9.265

Gold(I)-catalyzed hydroarylation reaction of aryl (3-iodoprop-2-yn-1-yl) ethers: synthesis of 3-iodo-2H-chromene derivatives

• Pablo Morán-Poladura,
• Eduardo Rubio and
• José M. González

Beilstein J. Org. Chem. 2013, 9, 2120–2128, doi:10.3762/bjoc.9.249

• for functional applications. Thus, for instance, this molecular frame has been associated with photochromic crystals [7], photochromic organogelators [8], selective cyclooxygenase-2 inhibitors [9][10], antifungal [11] and antitrypanocidal activity [12], transforming growth factor-β receptors [13] and

Exploration of an epoxidation–ring-opening strategy for the synthesis of lyconadin A and discovery of an unexpected Payne rearrangement

• Brad M. Loertscher,
• Yu Zhang and
• Steven L. Castle

Beilstein J. Org. Chem. 2013, 9, 1179–1184, doi:10.3762/bjoc.9.132

• ][3][4]. Biological assays revealed that 1 exhibits cytotoxicity against murine lymphoma L1210 and human epidermoid carcinoma KB cells (IC50 = 0.46 μg/mL and 1.7 μg/mL, respectively) [1]. Moreover, 1 has been shown to promote nerve growth factor biosynthesis in 1321N1 human astrocytoma cells [2]. In

Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway

• Paul M. Hershberger,
• Satyamaheshwar Peddibhotla,
• E. Hampton Sessions,
• Daniela B. Divlianska,
• Ricardo G. Correa,
• Anthony B. Pinkerton,
• John C. Reed and
• Gregory P. Roth

Beilstein J. Org. Chem. 2013, 9, 900–907, doi:10.3762/bjoc.9.103

• validation using a panel of known receptor and kinase-based counter screens [7]. Because activation of NF-κB is known to be initiated through protein kinase C (PKC), we hypothesized that selectivity could be possible by the fact that PKC activation occurs downstream from cell membrane antigen and growth

• -factor receptors yet is still upstream of IKKγ, potentially by inhibition of a new target protein or novel protein–protein interaction. Using cell-based HTS reporter gene assays, a series of chemical probes were identified that selectively inhibit this unique PKC-induced NF-κB pathway without modulating

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

• Allison S. Limpert,
• Margrith E. Mattmann and
• Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

• the health and stability of motor neurons. Compounds that increase growth factor-induced neuronal support have been tested in both cellular and mouse models of ALS with moderate success. For example, in a study performed by Shimazawa et al. [49] a small molecule (SUN N8075, 22, Figure 11), which is

• currently in clinical trials for the treatment of stroke, protected SH-SY5Y cells against pharmacologically induced ER stress-mediated cell death. Further investigation into the mechanism of action of this compound revealed that 22 potentiated the upregulation of VGF nerve growth factor inducible protein

• G93A mice, as analyzed by a grip-strength meter [77]. Interestingly, treatment with 36 increases the levels of insulin-like growth factor (IGF) 1 and 2, which induces myoblast growth and differentiation, while concomitantly decreasing the expression of muscle RING finger 1 (MuRF-1), a protein that can

Towards a biocompatible artificial lung: Covalent functionalization of poly(4-methylpent-1-ene) (TPX) with cRGD pentapeptide

• Lena Möller,
• Christian Hess,
• Jiří Paleček,
• Yi Su,
• Axel Haverich,
• Andreas Kirschning and
• Gerald Dräger

Beilstein J. Org. Chem. 2013, 9, 270–277, doi:10.3762/bjoc.9.33

• , leads to a highly biocompatible poly(methylpentene) surface. The resulting modified membrane preserves the required excellent gas-flow properties while being densely seeded with lung endothelial cells. Keywords: click chemistry; growth factor; nitrenes; plasma chemistry; poly(4-methylpent-1-ene

Synthesis of 5-(ethylsulfonyl)-2-methoxyaniline: An important pharmacological fragment of VEGFR2 and other inhibitors

• Miroslav Murár,
• Gabriela Addová and
• Andrej Boháč

Beilstein J. Org. Chem. 2013, 9, 173–179, doi:10.3762/bjoc.9.20

• kinase 1, alpha and beta adrenoreceptors, glycogen phosphorylase, IMP dehydrogenase, MMPs 2, 3, 9 and 13, etc. [1]. Vascular endothelial growth factor (VEGF-A) is a homodimeric glycoprotein and thought to be the key signalling molecule of angiogenesis, i.e., the formation of new blood vessels from pre

An easily accessible sulfated saccharide mimetic inhibits in vitro human tumor cell adhesion and angiogenesis of vascular endothelial cells

• Grazia Marano,
• Claas Gronewold,
• Martin Frank,
• Anette Merling,
• Christian Kliem,
• Sandra Sauer,
• Manfred Wiessler,
• Eva Frei and
• Reinhard Schwartz-Albiez

Beilstein J. Org. Chem. 2012, 8, 787–803, doi:10.3762/bjoc.8.89

• stimulated and regulated by a complex network of chemo- and cytokine-signaling. One of the pivotal angiogenic factors is the vascular endothelial growth factor (VEGF); in addition, the initial steps of angiogenesis may also be stimulated by inflammatory growth factors, such as the tumor necrosis factor (TNF

• 20% (v/v) FBS (Biochrom, Berlin, Germany), 1 μg/mL hydrocortisone, 0.1 ng/mL human epidermal growth factor and 1ng/mL human basal fibroblast growth factor, as recommended by the manufacturer. Cells used for the assays described below were mycoplasm free as verified by DAPI-staining of DNA and a PCR

Recent advances in direct C–H arylation: Methodology, selectivity and mechanism in oxazole series

• Cécile Verrier,
• Pierrik Lassalas,
• Laure Théveau,
• Guy Quéguiner,
• François Trécourt,
• Francis Marsais and
• Christophe Hoarau

Beilstein J. Org. Chem. 2011, 7, 1584–1601, doi:10.3762/bjoc.7.187

• to the preparation of two potential inhibitors of vascular endothelial growth factor receptor-2 (Scheme 5) [38][39]. In 1998, Miura reported the first study of Pd(0)-catalyzed direct arylation of imidazoles, oxazoles and thiazoles with iodo- and bromobenzene [40]. It was notably shown that the use of