Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation

K Neukirch; K Alsabil; CP Dinh; R Bilancia; M Raasch; A Ville; I Cerqua; G Viault; D Breard; S Pace; Veronika Temml; E Brunner; PM Jordan; MC Marques; K Loeser; A Gollowitzer; S Permann; J Gerstmeier; S Lorkowski; H Stuppner; U Garscha; T Rodrigues; GJL Bernardes; Daniela Brigitte Schuster; D Seraphin; P Richomme; A Rossi; AS Mosig; F Roviezzo; O Werz; JJ Helesbeux; A Koeberle

doi:10.1021/acs.jmedchem.1c00806

Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation

K Neukirch, K Alsabil, CP Dinh, R Bilancia, M Raasch, A Ville, I Cerqua, G Viault, D Breard, S Pace, Veronika Temml (Co-author), E Brunner, PM Jordan, MC Marques, K Loeser, A Gollowitzer, S Permann, J Gerstmeier, S Lorkowski, H StuppnerU Garscha, T Rodrigues, GJL Bernardes, Daniela Brigitte Schuster (Co-author), D Seraphin, P Richomme, A Rossi, AS Mosig, F Roviezzo, O Werz, JJ Helesbeux, A Koeberle

Insitute of Pharmacy

Research output: Contribution to journal › Original Article › peer-review

11 Citations (Web of Science)

Original language	English
Pages (from-to)	11496-11526
Journal	JOURNAL OF MEDICINAL CHEMISTRY
Volume	64
Issue number	15
DOIs	https://doi.org/10.1021/acs.jmedchem.1c00806
Publication status	Published - 2021

Keywords

PROSTAGLANDIN E-2 SYNTHASE-1
GARCINOIC ACID
ANTIINFLAMMATORY ACTIVITY
5-LIPOXYGENASE ACTIVITY
ORTHO-FORMYLATION
LIPID MEDIATORS
HUMAN SERUM
E SERIES
DERIVATIVES
DISEASE

Access to Document

10.1021/acs.jmedchem.1c00806

Cite this

Neukirch, K., Alsabil, K., Dinh, CP., Bilancia, R., Raasch, M., Ville, A., Cerqua, I., Viault, G., Breard, D., Pace, S., Temml, V., Brunner, E., Jordan, PM., Marques, MC., Loeser, K., Gollowitzer, A., Permann, S., Gerstmeier, J., Lorkowski, S., ... Koeberle, A. (2021). Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation. JOURNAL OF MEDICINAL CHEMISTRY , 64(15), 11496-11526. https://doi.org/10.1021/acs.jmedchem.1c00806

Neukirch, K ; Alsabil, K ; Dinh, CP et al. / Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation. In: JOURNAL OF MEDICINAL CHEMISTRY 2021 ; Vol. 64, No. 15. pp. 11496-11526.

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title = "Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation",

keywords = "PROSTAGLANDIN E-2 SYNTHASE-1, GARCINOIC ACID, ANTIINFLAMMATORY ACTIVITY, 5-LIPOXYGENASE ACTIVITY, ORTHO-FORMYLATION, LIPID MEDIATORS, HUMAN SERUM, E SERIES, DERIVATIVES, DISEASE",

author = "K Neukirch and K Alsabil and CP Dinh and R Bilancia and M Raasch and A Ville and I Cerqua and G Viault and D Breard and S Pace and Veronika Temml and E Brunner and PM Jordan and MC Marques and K Loeser and A Gollowitzer and S Permann and J Gerstmeier and S Lorkowski and H Stuppner and U Garscha and T Rodrigues and GJL Bernardes and Schuster, {Daniela Brigitte} and D Seraphin and P Richomme and A Rossi and AS Mosig and F Roviezzo and O Werz and JJ Helesbeux and A Koeberle",

note = "Schuster; Temml: Department of Pharmaceutical and Medicinal Chemistry, Paracelsus Medical University Salzburg, 5020 Salzburg, Austria",

year = "2021",

doi = "10.1021/acs.jmedchem.1c00806",

language = "English",

volume = "64",

pages = "11496--11526",

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Neukirch, K, Alsabil, K, Dinh, CP, Bilancia, R, Raasch, M, Ville, A, Cerqua, I, Viault, G, Breard, D, Pace, S, Temml, V, Brunner, E, Jordan, PM, Marques, MC, Loeser, K, Gollowitzer, A, Permann, S, Gerstmeier, J, Lorkowski, S, Stuppner, H, Garscha, U, Rodrigues, T, Bernardes, GJL, Schuster, DB, Seraphin, D, Richomme, P, Rossi, A, Mosig, AS, Roviezzo, F, Werz, O, Helesbeux, JJ & Koeberle, A 2021, 'Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation', JOURNAL OF MEDICINAL CHEMISTRY , vol. 64, no. 15, pp. 11496-11526. https://doi.org/10.1021/acs.jmedchem.1c00806

Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation. / Neukirch, K; Alsabil, K; Dinh, CP et al.
In: JOURNAL OF MEDICINAL CHEMISTRY , Vol. 64, No. 15, 2021, p. 11496-11526.

Research output: Contribution to journal › Original Article › peer-review

TY - JOUR

T1 - Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation

AU - Neukirch, K

AU - Alsabil, K

AU - Dinh, CP

AU - Bilancia, R

AU - Raasch, M

AU - Ville, A

AU - Cerqua, I

AU - Viault, G

AU - Breard, D

AU - Pace, S

AU - Temml, Veronika

AU - Brunner, E

AU - Jordan, PM

AU - Marques, MC

AU - Loeser, K

AU - Gollowitzer, A

AU - Permann, S

AU - Gerstmeier, J

AU - Lorkowski, S

AU - Stuppner, H

AU - Garscha, U

AU - Rodrigues, T

AU - Bernardes, GJL

AU - Schuster, Daniela Brigitte

AU - Seraphin, D

AU - Richomme, P

AU - Rossi, A

AU - Mosig, AS

AU - Roviezzo, F

AU - Werz, O

AU - Helesbeux, JJ

AU - Koeberle, A

N1 - Schuster; Temml: Department of Pharmaceutical and Medicinal Chemistry, Paracelsus Medical University Salzburg, 5020 Salzburg, Austria

PY - 2021

Y1 - 2021

KW - PROSTAGLANDIN E-2 SYNTHASE-1

KW - GARCINOIC ACID

KW - ANTIINFLAMMATORY ACTIVITY

KW - 5-LIPOXYGENASE ACTIVITY

KW - ORTHO-FORMYLATION

KW - LIPID MEDIATORS

KW - HUMAN SERUM

KW - E SERIES

KW - DERIVATIVES

KW - DISEASE

U2 - 10.1021/acs.jmedchem.1c00806

DO - 10.1021/acs.jmedchem.1c00806

M3 - Original Article

C2 - 34279935

SN - 0022-2623

VL - 64

SP - 11496

EP - 11526

JO - JOURNAL OF MEDICINAL CHEMISTRY

JF - JOURNAL OF MEDICINAL CHEMISTRY

IS - 15

ER -

Neukirch K, Alsabil K, Dinh CP, Bilancia R, Raasch M, Ville A et al. Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation. JOURNAL OF MEDICINAL CHEMISTRY . 2021;64(15):11496-11526. doi: 10.1021/acs.jmedchem.1c00806