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K. Aertgeerts · SciRah

Researcher profile · Semantic Scholar

K. Aertgeerts

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K. Aertgeerts — researcher profile on SciRah

h-index: 24
Works: 68
Citations: 2,934

Most-cited papers

Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein
K. Aertgeerts, R. Skene, J. Yano, Bi-Ching Sang +11 more
2011Journal of Biological Chemistry376 citations Open access
Semantic Scholar
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
A. Srivastava, J. Yano, Yoshihiko Hirozane, G. Kefala +8 more
2014Nature346 citations
Semantic Scholar
Plasminogen activator inhibitor-1 detaches cells from extracellular matrices by inactivating integrins
R. Czekay, K. Aertgeerts, S. Curriden, D. Loskutoff
2003Journal of Cell Biology318 citations Open access
Semantic Scholar
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
T. Ishikawa, M. Seto, H. Banno, Y. Kawakita +13 more
2011Journal of Medicinal Chemistry222 citations Open access
Semantic Scholar
Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation
K. Aertgeerts, S. Ye, Mike Tennant, M. Kraus +5 more
2004Protein Science204 citations Open access
Semantic Scholar
The Low Density Lipoprotein Receptor-related Protein Is a Motogenic Receptor for Plasminogen Activator Inhibitor-1*
B. Degryse, Jaap G. Neels, R. Czekay, K. Aertgeerts +2 more
2004Journal of Biological Chemistry202 citations Open access
Semantic Scholar
Structural and Kinetic Analysis of the Substrate Specificity of Human Fibroblast Activation Protein α*
K. Aertgeerts, I. Levin, Lihong Shi, G. Snell +8 more
2005Journal of Biological Chemistry187 citations Open access
Semantic Scholar
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.
Zhiyuan Zhang, M. Wallace, Jun Feng, J. Stafford +11 more
2011Journal of Medicinal Chemistry115 citations Open access
Semantic Scholar
Mechanisms contributing to the conformational and functional flexibility of plasminogen activator inhibitor-1
K. Aertgeerts, H. D. De Bondt, C. D. de Ranter, P. Declerck
1995Nature Structural Biology112 citations
Semantic Scholar
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Masanori Okaniwa, M. Hirose, T. Arita, M. Yabuki +13 more
2013Journal of Medicinal Chemistry103 citations Open access
Semantic Scholar
Conformational Flexibility in Crystal Structures of Human 11β-Hydroxysteroid Dehydrogenase Type I Provide Insights into Glucocorticoid Interconversion and Enzyme Regulation*
D. Hosfield, Yi-Qin Wu, R. Skene, M. Hilgers +3 more
2005Journal of Biological Chemistry98 citations Open access
Semantic Scholar
N‐linked glycosylation of dipeptidyl peptidase IV (CD26): Effects on enzyme activity, homodimer formation, and adenosine deaminase binding
K. Aertgeerts, S. Ye, Lihong Shi, S. Prasad +6 more
2004Protein Science67 citations Open access
Semantic Scholar
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Masanori Okaniwa, M. Hirose, T. Imada, T. Ohashi +18 more
2012Journal of Medicinal Chemistry65 citations
Semantic Scholar
Outcome of the first wwPDB/CCDC/D3R Ligand Validation Workshop
P. Adams, K. Aertgeerts, C. Bauer, J. Bell +53 more
2016Structure60 citations Open access
Semantic Scholar
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.
Yasufumi Miyamoto, Yoshihiro Banno, Tohru Yamashita, Tatsuhiko Fujimoto +18 more
2011Journal of Medicinal Chemistry51 citations Open access
Semantic Scholar
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.
Takuya Fujimoto, Y. Imaeda, Noriko Konishi, K. Hiroe +4 more
2009Journal of Medicinal Chemistry51 citations Open access
Semantic Scholar
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.
Brian P. Dyck, B. Branstetter, T. Gharbaoui, A. Hudson +25 more
2017Journal of Medicinal Chemistry47 citations Open access
Semantic Scholar
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.
Laurent Gomez, M. Massari, Troy D. Vickers, Graeme C. Freestone +22 more
2017Journal of Medicinal Chemistry43 citations Open access
Semantic Scholar
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Yoshihiro Banno, Yasufumi Miyamoto, M. Sasaki, Satoru Oi +14 more
2011Bioorganic & Medicinal Chemistry36 citations Open access
Semantic Scholar
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
A. Gould, Ruth Adams, S. Adhikari, K. Aertgeerts +44 more
2011Journal of Medicinal Chemistry34 citations Open access
Semantic Scholar
A model of the reactive form of plasminogen activator inhibitor-1.
K. Aertgeerts, H. D. De Bondt, C. D. de Ranter, Paul J. Declerck
1994Journal of Structural Biology29 citations
Semantic Scholar
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.
Hironobu Maezaki, Yoshihiro Banno, Yasufumi Miyamoto, Yuusuke Moritou +15 more
2011Bioorganic & Medicinal Chemistry28 citations Open access
Semantic Scholar
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125.
Yasufumi Miyamoto, Yoshihiro Banno, Tohru Yamashita, Tatsuhiko Fujimoto +16 more
2011Bioorganic & Medicinal Chemistry24 citations Open access
Semantic Scholar
Identification of positively charged residues contributing to the stability of plasminogen activator inhibitor 1
A. Gils, Jie Lu, K. Aertgeerts, I. Knockaert +1 more
1997FEBS Letters24 citations
Semantic Scholar
Crystallization and X‐ray diffraction data of the cleaved form of plasminogen activator inhibitor‐1
K. Aertgeerts, H. D. De Bondt, C. D. de Ranter, Paul J. Declerck
1995Proteins: Structure, Function, and Bioinformatics19 citations
Semantic Scholar
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
M. Hirose, Masanori Okaniwa, T. Miyazaki, T. Imada +13 more
2012Bioorganic & Medicinal Chemistry16 citations Open access
Semantic Scholar
Mathematical and Structural Characterization of Strong Nonadditive Structure-Activity Relationship Caused by Protein Conformational Changes.
Laurent Gomez, Rui-Bo Xu, W. Sinko, Brandon R. Selfridge +11 more
2018Journal of Medicinal Chemistry13 citations
Semantic Scholar
STRUCTURAL ANALYSIS OF THE MECHANISM OF INHIBITION AND ALLOSTERIC ACTIVATION OF THE KINASE DOMAIN OF HER 2
K. Aertgeerts, R. Skene, J. Yano, Bi-Ching Sang +11 more
201111 citations
Semantic Scholar
Method for rapid optimization of recombinant GPCR protein expression and stability using virus-like particles.
Thao T Ho, Jasmine Nguyen, Ju-Ping Liu, P. Stańczak +10 more
2017Protein Expression and Purification10 citations
Semantic Scholar
Target Engagement of a Phosphodiesterase 2A Inhibitor Affecting Long-Term Memory in the Rat
G. Gu, Trevor Scott, Y. Yan, Noelle Warren +11 more
2019Journal of Pharmacology and Experimental Therapeutics9 citations Open access
Semantic Scholar
Plasminogen activator inhibitor 1 (PAI-1) in its active conformation: crystallization and preliminary X-ray diffraction data.
Pieter Willems, A. Rabijns, K. Aertgeerts, N. Vleugels +4 more
1999Acta Crystallographica Section D: Biological Crystallography4 citations
Semantic Scholar
Corrigendum to “Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554” [Bioorg. Med. Chem. 19 (2011) 4482–4498]
Hironobu Maezaki, Yoshihiro Banno, Yasufumi Miyamoto, Yusuke Moritoh +15 more
20112 citations Open access
Semantic Scholar
Crystal Structure of the Kinase domain of Human HER2 (erbB2).
R. Skene, K. Aertgeerts, S. Sogabe
20112 citations
Semantic Scholar
Induction of conformational changes within crystals of plasminogen activator inhibitor-1 (PAI-1)
P. Willems, A. Gils, K. Aertgeerts, C. D. de Ranter +1 more
19992 citations
Semantic Scholar
Crystal-structure of a cleaved variant of human plasminogen-activator inhibitor-1
K. Aertgeerts, H. Debondt, C. Deranter, P. Declerck
19952 citations
Semantic Scholar
Optimization of Recombinant GPCR Proteins for Biophysical and Structural Studies Using Virus-like Particles.
K. Aertgeerts, Thao T Ho, Ying-Zhou G. Yan
2022Methods in molecular biology1 citations
Semantic Scholar
Dataset on Galanin Receptor 3 mutants that improve recombinant receptor expression and stability in an agonist and antagonist bound form
Thao T Ho, Jasmine Nguyen, Ju-Ping Liu, P. Stańczak +10 more
2017Data in Brief1 citations Open access
Semantic Scholar
Crystal structure of Human GPR40 bound to allosteric agonist TAK-875
A. Srivastava, J. Yano, Yoshihiko Hirozane, G. Kefala +8 more
20141 citations
Semantic Scholar
Abstract C255: Discovery of TAK-632: A selective kinase inhibitor of pan-RAF with potent antitumor activity against BRAF and NRAS mutant melanomas.
Masanori Okaniwa, M. Hirose, T. Arita, M. Yabuki +13 more
20131 citations
Semantic Scholar
Crystal Structure of the Kinase domain of Human B-raf with a [1,3]thiazolo[5,4-b]pyridine derivative
J. Yano, K. Aertgeerts
20121 citations
Semantic Scholar
EGFR Kinase domain complexed with tak-285
K. Aertgeerts, R. Skene, S. Sogabe
20111 citations
Semantic Scholar
Crystal structure of dipeptidyl peptidase IV in complex with TAK-322
Zhi-Yuan Zhang, M. Wallace, Jun Feng, J. Stafford +10 more
20101 citations
Semantic Scholar
Crystal Structure Of Human Fibroblast Activation Protein alpha
K. Aertgeerts, I. Levin, Lihong Shi, G. Prasad +7 more
20051 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with N-(1-adamantyl)-1-(2-chloro-5-isobutoxy-phenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with N-(1-adamantyl)-1-(2-chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with 1-(2-chloro-5-methoxy-phenyl)-N-isobutyl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with 1-(5-tert-butoxy-2-chloro-phenyl)-N-isobutyl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with 1-(2-chloro-5-isobutoxy-phenyl)-N,4-dimethyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
Crystal structure of human phosphodiesterase 2A with 1-(2-chlorophenyl)-N,4-dimethyl-[1,2,4]triazolo[4,3-a]quinoxaline-8-carboxamide
R. Xu, K. Aertgeerts
20180 citations
Semantic Scholar
CRYSTAL STRUCTURE OF HUMAN PHOSPHODIESTERASE 2A IN COMPLEX WITH 3,3-difluoro-1-[(4-fluorophenyl)carbonyl]-5-{5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl}piperidine
R. Xu, K. Aertgeerts
20170 citations
Semantic Scholar

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J. Yano×16
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Bi-Ching Sang×8
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