The Hydrolysis of Bimatoprost in Corneal Tissue Generates a Potent Prostanoid FP Receptor Agonist

2002 ◽  
Vol 47 ◽  
pp. S34-S40 ◽  
Author(s):  
Kirk M Maxey ◽  
Jennifer L Johnson ◽  
Jennifer LaBrecque
Keyword(s):  
Receptor Agonist ◽  
Corneal Tissue ◽  
Fp Receptor ◽  
Hydrolysis Of

Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug

2004 ◽  
Vol 78 (4) ◽  
pp. 767-776 ◽  
Author(s):  
Yasutaka Takagi ◽  
Tadashi Nakajima ◽  
Atsushi Shimazaki ◽  
Masaaki Kageyama ◽  
Takeshi Matsugi ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Hypotensive Drug ◽  
Fp Receptor

Synthesis of the Highly Potent Prostanoid FP Receptor Agonist, AFP-168: A Novel 15-Deoxy-15,15-difluoroprostaglandin F2α Derivative.

ChemInform ◽  
2004 ◽  
Vol 35 (21) ◽  
Author(s):  
Yasushi Matsumura ◽  
Nobuaki Mori ◽  
Takashi Nakano ◽  
Hideshi Sasakura ◽  
Takeshi Matsugi ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Fp Receptor

S1′ and S2′ subsite specificities of human plasma kallikrein and tissue kallikrein 1 for the hydrolysis of peptides derived from the bradykinin domain of human kininogen

2008 ◽  
Vol 389 (12) ◽  
Author(s):  
Aurelio Resende Lima ◽  
Fabiana M. Alves ◽  
Pedro Francisco Ângelo ◽  
Douglas Andrade ◽  
Sachiko I. Blaber ◽  
...  
Keyword(s):  
Amino Acids ◽  
Human Plasma ◽  
Receptor Agonist ◽  
Plasma Kallikrein ◽  
Tissue Kallikrein ◽  
Charged Amino Acids ◽  
B1 Receptor ◽  
Lower Specificity ◽  
Natural Amino Acids ◽  
Hydrolysis Of

AbstractThe S1′ and S2′ subsite specificities of human tissue kallikrein 1 (KLK1) and human plasma kallikrein (HPK) were examined with the peptide series Abz-GFSPFRXSRIQ-EDDnp and Abz-GFSPFRSXRIQ-EDDnp [X=natural amino acids or S(PO3H2)]. KLK1 efficiently hydrolyzed most of the peptides except those containing negatively charged amino acids at P1′ and P2′ positions. Abz-GFSPFRSSRIQ-EDDnp, as in human kininogen, is the best substrate for KLK1 and exclusively cleaved the R-S bond. All other peptides were cleaved also at the F-R bond. The synthetic human kininogen segment Abz-MISLMKRPPGFSPFRS390S391RI-NH2was hydrolyzed by KLK1 first at R-S and then at M-K bonds, releasing Lys-bradykinin. In the S390and S391phosphorylated analogs, this order of hydrolysis was inverted due to the higher resistance of the R-S bond. Abz-MISLMKRPPG-FSPFRSS(PO3H2)391RI-NH2was hydrolyzed by KLK1 at M-K and mainly at the F-R bond, releasing des-(Arg9)-Lys-Bk which is a B1 receptor agonist. HPK cleaved all the peptides at R and showed restricted specificity for S in the S1′ subsite, with lower specificity for the S2′ subsite. Abz-MISLMKRPPGFSPFRSSRI-NH2was efficiently hydrolyzed by HPK under bradykinin release, while the analogs containing S(PO3H2) were poorly hydrolyzed. In conclusion, S1′ and S2′ subsite specificities of KLK1 and HPK showed peculiarities that were observed with substrates containing the amino acid sequence of human kininogen.

Synthesis of the highly potent prostanoid FP receptor agonist, AFP-168: a novel 15-deoxy-15,15-difluoroprostaglandin F 2α derivative

2004 ◽  
Vol 45 (7) ◽  
pp. 1527-1529 ◽  
Author(s):  
Yasushi Matsumura ◽  
Nobuaki Mori ◽  
Takashi Nakano ◽  
Hideshi Sasakura ◽  
Takeshi Matsugi ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Fp Receptor

Synthesis of [phenyl-2-3H]-travoprost: isopropyl ester prodrug of a selective prostaglandin FP receptor agonist

2001 ◽  
Vol 44 (3) ◽  
pp. 173-183 ◽  
Author(s):  
Robert Selliah ◽  
Anura Dantanarayana ◽  
Karen Haggard ◽  
Judith Egan ◽  
Ernest U. Do ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Isopropyl Ester ◽  
Fp Receptor ◽  
Ester Prodrug

scholarly journals Ocular Hypotensive Effect of ONO-9054, an EP3/FP Receptor Agonist

2016 ◽  
Vol 25 (10) ◽  
pp. e826-e833 ◽  
Author(s):  
Alon Harris ◽  
Caroline L. Ward ◽  
Cheryl L. Rowe-Rendleman ◽  
Takafumi Ouchi ◽  
Andrew Wood ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Hypotensive Effect ◽  
Fp Receptor

Fine Structural Localization of Acyltransferases Involved in Lipid Synthesis in Intestinal Mucosa.

1970 ◽  
Vol 28 ◽  
pp. 54-55
Author(s):  
R. J. Barrnett ◽  
J. A. Higgins
Keyword(s):  
Smooth Endoplasmic Reticulum ◽  
Lipid Synthesis ◽  
Mucosal Cell ◽  
Structural Localization ◽  
Morphological Studies ◽  
Mucosal Cells ◽  
Initial Appearance ◽  
Sh Group ◽  
Hydrolysis Of ◽  
Intestinal Mucosal Cells

The main products of intestinal hydrolysis of dietary triglycerides are free fatty acids and monoglycerides. These form micelles from which the lipids are absorbed across the mucosal cell brush border. Biochemical studies have indicated that intestinal mucosal cells possess a triglyceride synthesising system, which uses monoglyceride directly as an acylacceptor as well as the system found in other tissues in which alphaglycerophosphate is the acylacceptor. The former pathway is used preferentially for the resynthesis of triglyceride from absorbed lipid, while the latter is used mainly for phospholipid synthesis. Both lipids are incorporated into chylomicrons. Morphological studies have shown that during fat absorption there is an initial appearance of fat droplets within the cisternae of the smooth endoplasmic reticulum and that these subsequently accumulate in the golgi elements from which they are released at the lateral borders of the cell as chylomicrons.We have recently developed several methods for the fine structural localization of acyltransferases dependent on the precipitation, in an electron dense form, of CoA released during the transfer of the acyl group to an acceptor, and have now applied these methods to a study of the fine structural localization of the enzymes involved in chylomicron lipid biosynthesis. These methods are based on the reduction of ferricyanide ions by the free SH group of CoA.

Lattice imaging and pore structure of β ferric oxyhydroxide

1978 ◽  
Vol 36 (1) ◽  
pp. 264-265
Author(s):  
T. Baird ◽  
J.R. Fryer ◽  
S.T. Galbraith
Keyword(s):  
Electron Microscopy ◽  
Room Temperature ◽  
Bulk Material ◽  
Model Structure ◽  
Bulk Crystals ◽  
Lattice Imaging ◽  
Thin Sections ◽  
Ferric Oxyhydroxide ◽  
Resolution Electron ◽  
Hydrolysis Of

Introduction Previously we had suggested (l) that the striations observed in the pod shaped crystals of β FeOOH were an artefact of imaging in the electron microscope. Contrary to this adsorption measurements on bulk material had indicated the presence of some porosity and Gallagher (2) had proposed a model structure - based on the hollandite structure - showing the hollandite rods forming the sides of 30Å pores running the length of the crystal. Low resolution electron microscopy by Watson (3) on sectioned crystals embedded in methylmethacrylate had tended to support the existence of such pores.We have applied modern high resolution techniques to the bulk crystals and thin sections of them without confirming these earlier postulatesExperimental β FeOOH was prepared by room temperature hydrolysis of 0.01M solutions of FeCl3.6H2O, The precipitate was washed, dried in air, and embedded in Scandiplast resin. The sections were out on an LKB III Ultramicrotome to a thickness of about 500Å.

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