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The following term was not found in PubMed: 11Z-6s-trans-fixed
Page 1
Treatment of geographic atrophy: an update on data related to pegcetacoplan.
Patel SB, Heier JS, Chaudhary V, Wykoff CC. Patel SB, et al. Curr Opin Ophthalmol. 2024 Jan 1;35(1):64-72. doi: 10.1097/ICU.0000000000000845. Epub 2023 Oct 10. Curr Opin Ophthalmol. 2024. PMID: 37815317 Review.
Dysregulation of the complement cascade has been directly implicated in AMD pathogenesis. Pegcetacoplan is a pegylated highly selective bicyclic peptide that inhibits the cleavage of complement component 3 (C3), which represents a key step in propagation of the complement …
Dysregulation of the complement cascade has been directly implicated in AMD pathogenesis. Pegcetacoplan is a pegylated highly selective b …
Synthesis, Characterization, and in vivo Evaluation of a Novel Potent Autotaxin-Inhibitor.
Hunziker D, Reinehr S, Palmhof M, Wagner N, Biniasch T, Stute G, Mattei P, Schmitz P, DiGiorgio P, Hert J, Rudolph MG, Benz J, Stihle M, Gsell B, Müller S, Gasser R, Schonhoven N, Ullmer C, Joachim SC. Hunziker D, et al. Front Pharmacol. 2022 Jan 18;12:699535. doi: 10.3389/fphar.2021.699535. eCollection 2021. Front Pharmacol. 2022. PMID: 35126098 Free PMC article.
In order to inhibit or modulate this pathway, we developed a new series of ATX-inhibitors containing novel bicyclic and spirocyclic structural motifs. A potent lead compound (IC(50) against ATX: 6 nM) with good in vivo PK, favorable in vitro property, and safety profile wa …
In order to inhibit or modulate this pathway, we developed a new series of ATX-inhibitors containing novel bicyclic and spirocyclic s …
Structural basis for carotenoid cleavage by an archaeal carotenoid dioxygenase.
Daruwalla A, Zhang J, Lee HJ, Khadka N, Farquhar ER, Shi W, von Lintig J, Kiser PD. Daruwalla A, et al. Proc Natl Acad Sci U S A. 2020 Aug 18;117(33):19914-19925. doi: 10.1073/pnas.2004116117. Epub 2020 Aug 3. Proc Natl Acad Sci U S A. 2020. PMID: 32747548 Free PMC article.
NdCCD was active toward beta-apocarotenoids but did not cleave bicyclic carotenoids. It exhibited an unusual regiospecificity, cleaving apocarotenoids solely at the C14'-C13' alkene bond to produce beta-apo-14'-carotenals. The structure of NdCCD revealed a tapered active s …
NdCCD was active toward beta-apocarotenoids but did not cleave bicyclic carotenoids. It exhibited an unusual regiospecificity, cleavi …
Targeting Plasma Kallikrein With a Novel Bicyclic Peptide Inhibitor (THR-149) Reduces Retinal Thickening in a Diabetic Rat Model.
Van Bergen T, Hu TT, Little K, De Groef L, Moons L, Stitt AW, Vermassen E, Feyen JHM. Van Bergen T, et al. Invest Ophthalmol Vis Sci. 2021 Oct 4;62(13):18. doi: 10.1167/iovs.62.13.18. Invest Ophthalmol Vis Sci. 2021. PMID: 34677569 Free PMC article.
RESULTS: Single or repeated THR-149 injections resulted in reduced inflammation, as depicted by decreasing numbers and activation state of immune cells and IL-6 cytokine levels in the diabetic retina. The processes of reactive gliosis, vessel leakage, and retinal th …
RESULTS: Single or repeated THR-149 injections resulted in reduced inflammation, as depicted by decreasing numbers and activation state of i …
Structure around C6-C7 bond of the chromophore in bathorhodopsin: low-temperature spectroscopy of 6s-cis-locked bicyclic rhodopsin analogs.
Imamoto Y, Sakai M, Katsuta Y, Wada A, Ito M, Shichida Y. Imamoto Y, et al. Biochemistry. 1996 May 21;35(20):6257-62. doi: 10.1021/bi9519359. Biochemistry. 1996. PMID: 8639566
These results strongly suggest that the structure around the beta-ionone ring region of the bathorhodopsin chromophore resembles 6,5-retinal rather than 6,7-retinal. From the comparison of the structural features among retinal, 6,5-retinal, and 6,7- …
These results strongly suggest that the structure around the beta-ionone ring region of the bathorhodopsin chromophore resembles 6,5-reti …
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.
Cioffi CL, Racz B, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Zhu L, Kitchen DB, Barnes KD, Dobri N, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. J Med Chem. 2015 Aug 13;58(15):5863-88. doi: 10.1021/acs.jmedchem.5b00423. Epub 2015 Aug 4. J Med Chem. 2015. PMID: 26181715 Free PMC article.
Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic bisretinoid formation in the retinal pigment epithelium (RPE), which is associated with the pathogenesis of both dry age-related macu …
Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic …
Generation and Characterization of Anti-Glucosepane Antibodies Enabling Direct Detection of Glucosepane in Retinal Tissue.
Streeter MD, Rowan S, Ray J, McDonald DM, Volkin J, Clark J, Taylor A, Spiegel DA. Streeter MD, et al. ACS Chem Biol. 2020 Oct 16;15(10):2655-2661. doi: 10.1021/acschembio.0c00093. Epub 2020 Oct 7. ACS Chem Biol. 2020. PMID: 32975399 Free PMC article.
Here, we report the development of the first polyclonal anti-glucosepane antibodies using a synthetic immunogen that contains the core bicyclic ring structure of glucosepane. We investigate the recognition properties of these antibodies through ELISAs involving an array of …
Here, we report the development of the first polyclonal anti-glucosepane antibodies using a synthetic immunogen that contains the core bi …
An improved synthesis of benzocycloalkanone derivatives.
Wada A, Sawada K, Ono N, Ito M. Wada A, et al. Chem Pharm Bull (Tokyo). 2004 Jan;52(1):132-5. doi: 10.1248/cpb.52.132. Chem Pharm Bull (Tokyo). 2004. PMID: 14709881 Free article.
A convenient and improved annulation method for the synthesis of bicyclic ketones was developed. A 2,2-dimethyl-6-(2-phenylsulfonyl)ethylcyclohexanone was converted into a sulfonylester by the addition of ethyl acetate and subsequent dehydration. ...
A convenient and improved annulation method for the synthesis of bicyclic ketones was developed. A 2,2-dimethyl-6-(2-phenylsulfonyl)e …
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Teufel DP, Bennett G, Harrison H, van Rietschoten K, Pavan S, Stace C, Le Floch F, Van Bergen T, Vermassen E, Barbeaux P, Hu TT, Feyen JHM, Vanhove M. Teufel DP, et al. J Med Chem. 2018 Apr 12;61(7):2823-2836. doi: 10.1021/acs.jmedchem.7b01625. Epub 2018 Mar 15. J Med Chem. 2018. PMID: 29517911
Employing a technology based on phage-display combined with chemical cyclization, we have identified highly selective bicyclic peptide inhibitors with nano- and picomolar potencies toward plasma kallikrein. ...The peptides prevented bradykinin release in vitro, and in vivo …
Employing a technology based on phage-display combined with chemical cyclization, we have identified highly selective bicyclic peptid …
Discovery of alpha-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of rho(1) gamma-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone.
Krall J, Brygger BM, Sigurðardóttir SB, Ng CK, Bundgaard C, Kehler J, Nielsen B, Bek T, Jensen AA, Frølund B. Krall J, et al. ChemMedChem. 2016 Oct 19;11(20):2299-2310. doi: 10.1002/cmdc.201600356. Epub 2016 Sep 13. ChemMedChem. 2016. PMID: 27620323
In this study, we demonstrate that the partial GABA(A) R agonist imidazole-4-acetic acid (IAA) is able to penetrate the blood-brain barrier in vivo; we prepared a series of alpha- and N-alkylated, as well as bicyclic analogues of IAA to explore the structure-activity relat …
In this study, we demonstrate that the partial GABA(A) R agonist imidazole-4-acetic acid (IAA) is able to penetrate the blood-brain barrier …
14 results