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New Scaffold (new + scaffold)
Selected AbstractsA New Scaffold for the Stereoselective Synthesis of ,-O-Linked Glycopeptide Mimetics.CHEMINFORM, Issue 1 2005Francesca Venturi Abstract For Abstract see ChemInform Abstract in Full Text. [source] Tetrazolo[1,5-a]quinoline as a Potential Promising New Scaffold for the Synthesis of Novel Antiinflammatory and Antibacterial Agents.CHEMINFORM, Issue 34 2004Adnan A. Bekhit Abstract For Abstract see ChemInform Abstract in Full Text. [source] New Scaffolds for Combinatorial Synthesis.CHEMINFORM, Issue 5 2003Part 1. Abstract For Abstract see ChemInform Abstract in Full Text. [source] Novel Pirinixic Acids as PPAR, Preferential Dual PPAR,/, AgonistsMOLECULAR INFORMATICS, Issue 5 2009Heiko Zettl Abstract Pirinixic acid is a moderate agonist of both the alpha and the gamma subtype of the peroxisome proliferator activated receptor (PPAR). Previously, we have shown that ,-alkyl substitution leads to balanced low micromolar-active dual agonists of PPAR, and PPAR,. Taking ,-hexyl pirinixic acid as a new scaffold, we further optimized PPAR activity by enlargement of the lipophilic backbone by substituting the 2,3-dimethylphenyl with biphenylic moieties. Such a substitution pattern had only minor impact on PPAR, activity but further increased PPAR, activity leading to nanomolar activities. Supporting docking studies proposed that the (R)-enantiomer should fit the PPAR, ligand-binding pocket better and thus be more active than the (S)-enantiomer. Single enantiomers of selected active analogues were then prepared by enantio-selective synthesis and enantio-selective preparative HPLC, respectively. Biological data for the distinct enantiomers fully corroborated the docking experiments and substantiate a stereochemical impact on PPAR activation. [source] Designing a Three-dimensional Expanded Polytetrafluoroethylene,Poly(lactic-co-glycolic acid) Scaffold for Tissue EngineeringARTIFICIAL ORGANS, Issue 4 2009Hung-Jen Shao Abstract:, The purpose of this study was to design a three-dimensional expanded polytetrafluoroethylene (ePTFE),poly(lactic-co-glycolic acid) (PLGA) scaffold for tissue engineering. To test the feasibility of this composite scaffold, a series of two-dimensional culture experiments were performed to investigate the behavior of anterior cruciate ligament (ACL) cells on the ePTFE and PLGA membranes. It was found PLGA provided a cell-favorable substrate for cell adhesion, migration, and growth, indicating PLGA is an ACL cell-conductive material. Conversely, poor adhesion and proliferation of ACL cells were observed on the ePTFE, even on the collagen-coated ePTFE. Therefore, the scaffold was not fabricated by coating PLGA on the ePTFE surface because it is difficult to coat anything on the extremely hydrophobic ePTFE surface. Instead, the ePTFE embedded in the PLGA matrix was prepared by immersing ePTFE scrim yarns into the PLGA solution, and then precipitating PLGA to form a three-dimensional construction with porous morphology. The role of ePTFE is regarded as a reinforcing constituent to improve the mechanical strength of porous PLGA matrix to provide early repair strength for tissue healing. However, porous PLGA matrix acts as a supportive environment for allowing cell adhesion, migration, and growth to guide the repair and regeneration of ligament tissue. To test this assumption, a preliminary animal experiment of rabbit ACL wound healing with this three-dimensional ePTFE,PLGA scaffold was performed. These results are very encouraging because such a new scaffold made of ePTFE scrim yarns embedded in PLGA may serve as ACL prostheses in the ligament tissue engineering. [source] Extensive structure,activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5CHEMICAL BIOLOGY & DRUG DESIGN, Issue 5 2003P. Grieco Abstract: The melanocortin system is involved in the regulation of several diverse physiologic pathways. Recently we have demonstrated that replacing His6 by Pro6 in the well-known antagonist SHU-9119 resulted in a potent agonist at the hMC5R (EC50 = 0.072 nm) with full antagonist activity at the hMC3R and the hMC4R. We have designed, synthesized, and pharmacologically characterized a series of peptide analogs of MT-II and SHU-9119 at the human melanocortin receptors MC3R, MC4R and MC5R. All these peptides were modified at position 6 with a Pro instead of a His residue. In this study, we have identified new scaffolds which are antagonists at the hMC4R and hMC3R. Additionally, we have discovered a new selective agonist at the hMC4R, Ac-Nle-c[Asp-Pro-D-Phe-Arg-Trp-Lys]-Pro-Val-NH2 (6, PG-931) which will be useful in further biologic investigations of the hMC4R. PG-931 was about 100-fold more selective for the hMC4R vs. the hMC3R (IC50 = 0.58 and 55 nm, respectively). Some of these new analogs have exceptional biologic potencies at the hMC5R and will be useful in further efforts to differentiate the substructural features responsible for selectivity at the hMC3R, hMC4R, and hMC5R. [source] | ||||||||||