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1

Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor

Bert Brône, Pieter J. Peeters, Roger Marrannes, Marc Mercken, Ronny Nuydens, Theo Meert, Harrie J.M. Gijsen

Journal:

Toxicology and Applied Pharmacology

Year:

2008

Language:

english

File:

PDF, 566 KB

english, 2008

2

Analogues of Morphanthridine and the Tear Gas Dibenz[b,f][1,4]oxazepine (CR) as Extremely Potent Activators of the Human Transient Receptor Potential Ankyrin 1 (TRPA1) Channel

Gijsen, Harrie J. M., Berthelot, Didier, Zaja, Mirko, Brône, Bert, Geuens, Ivo, Mercken, Marc

Journal:

Journal of Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 986 KB

english, 2010

3

Recent Advances in the Chemoenzymatic Synthesis of Carbohydrates and Carbohydrate Mimetics

Gijsen, Harrie J. M., Qiao, Lei, Fitz, Wolfgang, Wong, Chi-Huey

Journal:

Chemical Reviews

Year:

1996

Language:

english

File:

PDF, 1.75 MB

english, 1996

4

Unprecedented Asymmetric Aldol Reactions with Three Aldehyde Substrates Catalyzed by 2-Deoxyribose-5-phosphate Aldolase

Gijsen, Harrie J. M., Wong, Chi-Huey

Journal:

Journal of the American Chemical Society

Year:

1994

Language:

english

File:

PDF, 169 KB

english, 1994

5

The evolution of amidine-based brain penetrant BACE1 inhibitors

Oehlrich, Daniel, Prokopcova, Hana, Gijsen, Harrie J.M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 2.91 MB

english, 2014

6

REALISIS: A Medicinal Chemistry-Oriented Reagent Selection, Library Design, and Profiling Platform.

Aziz Yasri, Didier Berthelot, Harry Gijsen, Theo Thielemans, Patrick Marichal, Michael Engels, Jan Hoflack

Journal:

Year:

2005

File:

PDF, 8 KB

2005

7

Synthesis of a cyclitol via a tandem enzymatic aldol — intramolecular Horner-Wadsworth-Emmons reaction

Harrie J.M. Gijsen, Chi-Huey Wong

Journal:

Tetrahedron Letters

Year:

1995

Language:

english

File:

PDF, 222 KB

english, 1995

8

5-Sulfonyl-benzimidazoles as selective CB2 agonists

Bie M.P. Verbist, Michel A.J. De Cleyn, Michel Surkyn, Erwin Fraiponts, Jeroen Aerssens, Marjoleen J.M.A. Nijsen, Harrie J.M. Gijsen

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 217 KB

english, 2008

9

Development of two diastereoselective routes towards trans-4-aminomethyl-piperidin-3-ol building blocks

Harrie J.M. Gijsen, Michel J.A. De Cleyn, Christopher J. Love, Michel Surkyn, Sven F.A. Van Brandt, Marc G.C. Verdonck, Luc Moens, Jef Cuypers, Jean-Paul R.M.A. Bosmans

Journal:

Year:

2008

Language:

english

File:

PDF, 347 KB

english, 2008

10

Rearrangement reactions of aromadendrane derivatives. The synthesis of (+)-maaliol, starting from natural (+)-aromadendrene-IV

Harrie J.M. Gijsen, Joannes B.P.A. Wijnberg, Connie van Ravenswaay, Aede de Groot

Journal:

Year:

1994

Language:

english

File:

PDF, 991 KB

english, 1994

11

Thermal rearrangement of bicyclogermacrane-1,8-dione. Synthesis of humulenedione and (−)-cubenol, starting from natural (+)-Aromadendrene-V

Harrie J.M. Gijsen, Joannes B.P.A. Wijnberg, Aede de Groot

Journal:

Year:

1994

Language:

english

File:

PDF, 800 KB

english, 1994

12

The synthesis of mono- and dihydroxy aromadendrane sesquiterpenes, starting from natural (+)-aromadendrene-III

Harrie J.M. Gijsen, Joannes B.P.A. Wijnberg, Gerrit A. Stork, Aede de Groot, Maarten A. de Waard, Johannes G.M. van Nistelrooy

Journal:

Year:

1992

Language:

english

File:

PDF, 1009 KB

english, 1992

13

Presenilin-1 but not amyloid precursor protein mutations present in mouse models of Alzheimer’s disease attenuate the response of cultured cells to γ-secretase modulators regardless of their potency and structure

Stefanie Hahn, Tanja Brüning, Julia Ness, Eva Czirr, Sandra Baches, Harrie Gijsen, Carsten Korth, Claus U. Pietrzik, Bruno Bulic, Sascha Weggen

Journal:

Journal of Neurochemistry

Year:

2011

Language:

english

File:

PDF, 441 KB

english, 2011

14

5-Sulfonyl-benzimidazoles as selective CB2 agonists-Part 2

Harrie J.M. Gijsen, Michel A.J. De Cleyn, Michel Surkyn, Guy R.E. Van Lommen, Bie M.P. Verbist, Marjoleen J.M.A. Nijsen, Theo Meert, Jean Van Wauwe, Jeroen Aerssens

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.01 MB

english, 2012

15

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors

Gary Tresadern, Francisca Delgado, Oscar Delgado, Harrie Gijsen, Gregor J. Macdonald, Dieder Moechars, Frederik Rombouts, Richard Alexander, John Spurlino, Michiel Van Gool, Juan Antonio Vega, Andrés

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 716 KB

english, 2011

16

Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists

Harrie J.M. Gijsen, Didier Berthelot, Michel A.J. De Cleyn, Ivo Geuens, Bert Brône, Marc Mercken

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 597 KB

english, 2012

17

γ-Secretase Modulators as Potential Disease Modifying Anti-Alzheimer’s Drugs

Oehlrich, Daniel, Berthelot, Didier J.-C., Gijsen, Harrie J. M.

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 3.85 MB

english, 2011

18

[Annual Reports in Medicinal Chemistry] Annual Reports in Medicinal Chemistry Volume 47 Volume 47 || Secretase Inhibitors and Modulators as a Disease-Modifying Approach Against Alzheimer's Disease

Gijsen, Harrie J.M.

Year:

2012

Language:

english

File:

PDF, 514 KB

english, 2012

19

Sequential One-Pot Aldol Reactions Catalyzed by 2-Deoxyribose-5-phosphate Aldolase and Fructose-1,6-diphosphate Aldolase

Gijsen, Harrie J. M., Wong, Chi-Huey

Journal:

Journal of the American Chemical Society

Year:

1995

Language:

english

File:

PDF, 270 KB

english, 1995

20

Recombinant 2-Deoxyribose-5-phosphate Aldolase in Organic Synthesis: Use of Sequential Two-Substrate and Three-Substrate Aldol Reactions

Wong, Chi-Huey, Garcia-Junceda, Eduardo, Chen, Lihren, Blanco, Olga, Gijsen, Harrie J. M., Steensma, Darryl H.

Journal:

Journal of the American Chemical Society

Year:

1995

Language:

english

File:

PDF, 1.41 MB

english, 1995

21

Sequential Three- and Four-Substrate Aldol Reactions Catalyzed by Aldolases

Gijsen, Harrie J. M., Wong, Chi-Huey

Journal:

Journal of the American Chemical Society

Year:

1995

Language:

english

File:

PDF, 875 KB

english, 1995

22

Upregulation of ADAM proteases and HER ligands through a feedback loop mediates acquired resistance to trastuzumab in HER2-amplified breast cancer

M Gijsen, P King, T Perera, P Parker, B Larijani, A Harris…

Journal:

Breast Cancer Research

Year:

2010

Language:

english

File:

PDF, 390 KB

english, 2010

23

Bexarotene treatment does not clear β-Amyloid in an AD mouse model and Beagle dogs

Tesseur, Ina, Lo, Adrian, Roberfroid, Anouk, Dietvorst, Sofie, Van Broeck, Bianca, Borgers, Marianne, Gijsen, Harrie, Moechars, Diederik, Mercken, Marc, Kemp, John, D’Hooge, Rudi, De Strooper, Bart

Journal:

Molecular Neurodegeneration

Year:

2013

Language:

english

File:

PDF, 72 KB

english, 2013

24

Evidence that gamma-secretase inhibitors induce an incomplete processing phenotype in preclinical models

Mercken, Marc, Hermans, Bart, Van Broeck, Bianca, Gijsen, Harry, Karran, Eric

Journal:

Alzheimer's & Dementia

Year:

2011

Language:

english

File:

PDF, 77 KB

english, 2011

25

Life-span of Tau.P301L mice: Modulation by GSK3b and O-GlcNAcylation

Van Leuven, Fred, Borghgraef, Peter, Menuet, Clement, Devijver, Herman, Gielis, Lies, Lechat, Benoit, Gijsen, Harry, Moechars, Dieder, Hilaire, Gerard

Journal:

Alzheimer's & Dementia

Year:

2011

Language:

english

File:

PDF, 56 KB

english, 2011

26

O-GlcNAc-ase inhibitor improves the clinical conditions of Alzheimer's disease mice

Borghgraef, Peter, Menuet, Clément, Theunis, Clara, Maurin, Hervé, Devijver, Herman, Lechat, Benoit, Gijsen, Harry, Moechars, Dieder, Hilaire, Gérard, Van Leuven, Fred

Journal:

Alzheimer's & Dementia

Year:

2013

Language:

english

File:

PDF, 164 KB

english, 2013

27

Life-span of Tau.P301L mice: Modulation by GSK3b and O-GlcNAc-ylation

Borghgraef, Peter, Menuet, Clément, Devijver, Herman, Gielis, Lies, Lechat, Benoit, Gijsen, Harry, Moechars, Dieder, Hilaire, Gérard, Van Leuven, Fred

Journal:

Alzheimer's & Dementia

Year:

2011

Language:

english

File:

PDF, 75 KB

english, 2011

28

Optimisation of the Preparation and Isolation of 5-Amino-2,4,6-triiodoisophthalic Acid Dichloride

Gijsen, Harrie J. M., Bakel, Herman C. C. K. van, Zwaan, Wim, Hulshof, Lumbertus A.

Journal:

Organic Process Research & Development

Year:

1999

Language:

english

File:

PDF, 212 KB

english, 1999

29

Evaluation of Furan Photooxygenation as a Device for Construction of the Zaragozic Acid (Squalestatin) Core

Maezaki, Naoyoshi, Gijsen, Harrie J. M., Sun, Li-Qiang, Paquette, Leo A.

Journal:

Journal of Organic Chemistry

Year:

1996

Language:

english

File:

PDF, 345 KB

english, 1996

30

Simple approach to the synthesis of novel tricyclic BACE1 inhibitor warhead through β-lactam opening

Bel Abed, Hassen, Van Brandt, Sven F.A., Vega, Juan Antonio, Gijsen, Harrie J.M.

Journal:

Tetrahedron Letters

Year:

2015

Language:

english

File:

PDF, 421 KB

english, 2015

31

HER2 Phosphorylation Is Maintained by a PKB Negative Feedback Loop in Response to Anti-HER2 Herceptin in Breast Cancer

Gijsen, Merel, King, Peter, Perera, Tim, Parker, Peter J., Harris, Adrian L., Larijani, Banafshé, Kong, Anthony, Kemp, Christopher

Journal:

Year:

2010

Language:

english

File:

PDF, 979 KB

english, 2010

32

Nieuwe orale anticoagulantia

Gyselaers, Jan, Gijsen, Gunther, Gijsen, Sofie, Smeets, Miek, Dewitte, Harrie, Vaes, Bert

Journal:

Year:

2015

Language:

dutch

File:

PDF, 184 KB

dutch, 2015

33

ChemInform Abstract: The Evolution of Amidine-Based Brain Penetrant BACE1 Inhibitors

Oehlrich, Daniel, Prokopcova, Hana, Gijsen, Harrie J. M.

Journal:

Year:

2014

File:

PDF, 12 KB

2014

34

Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Gijsen, Harrie J. M., Alonso de Diego, Sergio A., De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J., Martínez-Lamenca, Carolina, Oehlrich, Daniel, Prokopcova, Hana, Rombouts, Frederik J.

Journal:

Journal of Medicinal Chemistry

Year:

2018

Language:

english

File:

PDF, 665 KB

english, 2018

35

-Secretase Modulators: Can We Combine Potency with Safety?

Gijsen, Harrie J. M., Mercken, Marc

Journal:

International Journal of Alzheimer's Disease

Year:

2012

Language:

english

File:

PDF, 2.29 MB

english, 2012

36

Comparison of Two Different Methods for Measurement of Amyloid-β Peptides in Cerebrospinal Fluid after BACE1 Inhibition in a Dog Model

Borghys, Herman, Jacobs, Tom, Van Broeck, Bianca, Dillen, Lieve, Dhuyvetter, Deborah, Gijsen, Harrie, Mercken, Marc

Journal:

Journal of Alzheimer's Disease

Year:

2013

Language:

english

File:

PDF, 857 KB

english, 2013

37

Correction to Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate

Gijsen, Harrie J. M., Alonso de Diego, Sergio A., De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J., Martinez-Lamenca, Carolina, Oehlrich, Daniel, Prokopcova, Hana, Rombouts, Frederik J.

Journal:

Journal of Medicinal Chemistry

Year:

2018

Language:

english

File:

PDF, 243 KB

english, 2018

38

New Evolutions in the BACE1 Inhibitor Field from 2014 to 2018

Hsiao, Chien-Chi, Rombouts, Frederik, Gijsen, Harrie J.M.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2019

Language:

english

File:

PDF, 2.75 MB

english, 2019

39

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators

Bischoff, François P., Velter, Adriana Ingrid, Minne, Garrett, Pieters, Serge, Berthelot, Didier, De Cleyn, Michel, Gijsen, Harrie J.M., Macdonald, Gregor, Surkyn, Michel, Van Brandt, Sven, Van Roosbr

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2019

Language:

english

File:

PDF, 872 KB

english, 2019

40

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators

Bischoff, François P., Velter, Adriana Ingrid, Minne, Garrett, Pieters, Serge, Berthelot, Didier, De Cleyn, Michel, Gijsen, Harrie J.M., Macdonald, Gregor, Surkyn, Michel, Van Brandt, Sven, Van Roosbr

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2019

File:

PDF, 872 KB

2019

41

3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: potent and permeable BACE-1 inhibitors

Peschiulli, Aldo, Oehlrich, Daniel, Rombouts, Frederik, Vos, Ann, Gijsen, Harrie JM

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2020

Language:

english

File:

PDF, 701 KB

english, 2020

42

Small-molecule BACE1 inhibitors: a patent literature review (2011 to 2020)

Rombouts, Frederik, Kusakabe, Ken-ichi, Hsiao, Chien-Chi, Gijsen, Harrie J. M.

Journal:

Expert Opinion on Therapeutic Patents

Year:

2020

File:

PDF, 1.33 MB

2020