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Sigrid Hatse

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Chemicals & Drugs

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Sigrid Hatse; Carsten Kriebitzsch; Annouschka Laenen; Diether Lambrechts; Patrick Neven; Robert Paridaens; Gilian Peuteman; Ann Smeets; Thijs Vandorpe; Lieve Verlinden; Annemieke Verstuyf; Roger Bouillon; Olivier Brouckaert; Barbara Brouwers; Marie-Rose Christiaens; Anne-Sophie Dieudonné; Hans Wildiers
Vitamin D status at breast cancer diagnosis: correlation with tumor characteristics, disease outcome, and genetic determinants of vitamin D insufficiency.
Renato T Skerlj; Gary J Bridger; Al Kaller; Ernest J McEachern; Jason B Crawford; Yuanxi Zhou; Bem Atsma; Jonathon Langille; Susan Nan; Duane Veale; Trevor Wilson; Curtis Harwig; Sigrid Hatse; Katrien Princen; Erik De Clercq; Dominique Schols
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Gary J Bridger; Renato T Skerlj; Pedro E Hernandez-Abad; David E Bogucki; Zhongren Wang; Yuanxi Zhou; Susan Nan; Eva M Boehringer; Trevor Wilson; Jason Crawford; Markus Metz; Sigrid Hatse; Katrien Princen; Erik De Clercq; Dominique Schols
Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication.

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All Publications

2012: Sigrid Hatse; Carsten Kriebitzsch; Annouschka Laenen; Diether Lambrechts; Patrick Neven; Robert Paridaens; Gilian Peuteman; Ann Smeets; Thijs Vandorpe; Lieve Verlinden; Annemieke Verstuyf; Roger Bouillon; Olivier Brouckaert; Barbara Brouwers; Marie-Rose Christiaens; Anne-Sophie Dieudonné; Hans Wildiers
Vitamin D status at breast cancer diagnosis: correlation with tumor characteristics, disease outcome, and genetic determinants of vitamin D insufficiency.
Carcinogenesis 2012;33(7):1319-26.
2010: Renato T Skerlj; Gary J Bridger; Al Kaller; Ernest J McEachern; Jason B Crawford; Yuanxi Zhou; Bem Atsma; Jonathon Langille; Susan Nan; Duane Veale; Trevor Wilson; Curtis Harwig; Sigrid Hatse; Katrien Princen; Erik De Clercq; Dominique Schols
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Journal of medicinal chemistry 2010;53(8):3376-88.
2010: Gary J Bridger; Renato T Skerlj; Pedro E Hernandez-Abad; David E Bogucki; Zhongren Wang; Yuanxi Zhou; Susan Nan; Eva M Boehringer; Trevor Wilson; Jason Crawford; Markus Metz; Sigrid Hatse; Katrien Princen; Erik De Clercq; Dominique Schols
Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication.
Journal of medicinal chemistry 2010;53(3):1250-60.
2010: Sandra Liekens; Dominique Schols; Sigrid Hatse
CXCL12-CXCR4 axis in angiogenesis, metastasis and stem cell mobilization.
Current pharmaceutical design 2010;16(35):3903-20.
2007: Mette M Rosenkilde; Lars-Ole Gerlach; Sigrid Hatse; Renato T Skerlj; Dominique Schols; Gary J Bridger; Thue W Schwartz
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.
The Journal of biological chemistry 2007;282(37):27354-65.
2007: Sigrid Hatse; Dana Huskens; Katrien Princen; Kurt Vermeire; Gary J Bridger; Erik De Clercq; Mette M Rosenkilde; Thue W Schwartz; Dominique Schols
Modest human immunodeficiency virus coreceptor function of CXCR3 is strongly enhanced by mimicking the CXCR4 ligand binding pocket in the CXCR3 receptor.
Journal of virology 2007;81(7):3632-9.
2007: Sandra Liekens; Sofie Gijsbers; Els Vanstreels; Dirk Daelemans; Erik De Clercq; Sigrid Hatse
The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells.
Molecular pharmacology 2007;71(3):695-703.
2007: Jan Balzarini; Kristel Van Laethem; Dirk Daelemans; Sigrid Hatse; Antonella Bugatti; MARCO RUSNATI; Yasuhiro Igarashi; Toshikazu Oki; Dominique Schols
Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus.
Journal of virology 2007;81(1):362-73.
2006: Sigrid Hatse; Jan Balzarini; Sandra Liekens
Stromal cell-derived factor 1 (CXCL12) binds to endothelial cells and signals through a receptor different from CXCR4.
Biochemical and biophysical research communications 2006;348(1):192-9.
2005: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Matheus Froeyen; Willy J Peumans; Els J M Van Damme; Dominique Schols
Carbohydrate-binding agents cause deletions of highly conserved glycosylation sites in HIV GP120: a new therapeutic concept to hit the achilles heel of HIV.
The Journal of biological chemistry 2005;280(49):41005-14.
2005: Sigrid Hatse; Katrien Princen; Erik De Clercq; Mette M Rosenkilde; Thue W Schwartz; Pedro E Hernandez-Abad; Renato T Skerlj; Gary J Bridger; Dominique Schols
AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor.
Biochemical pharmacology 2005;70(5):752-61.
2005: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Matheus Froeyen; Els J M Van Damme; Anders Bolmstedt; Willy J Peumans; Erik De Clercq; Dominique Schols
Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis.
Molecular pharmacology 2005;67(5):1556-65.
2005: Bert De Klerck; Lies Geboes; Sigrid Hatse; Hilde Kelchtermans; Yves Meyvis; Kurt Vermeire; Gary J Bridger; An D Billiau; Dominique Schols; Patrick Matthys
Pro-inflammatory properties of stromal cell-derived factor-1 (CXCL12) in collagen-induced arthritis.
Arthritis research & therapy 2005;7(6):R1208-20.
2004: Katrien Princen; Sigrid Hatse; Kurt Vermeire; Stefano Aquaro; Erik De Clercq; Lars-Ole Gerlach; Mette M Rosenkilde; Thue W Schwartz; Renato T Skerlj; Gary J Bridger; Dominique Schols
Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist.
Journal of virology 2004;78(23):12996-3006.
2004: Kurt Vermeire; Katrien Princen; Sigrid Hatse; Erik De Clercq; Kaka Dey; Thomas W Bell; Dominique Schols
CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro.
AIDS (London, England) 2004;18(16):2115-25.
2004: Jan Balzarini; Sigrid Hatse; Kurt Vermeire; Katrien Princen; Stefano Aquaro; Carlo Federico Perno; Erik De Clercq; Herman Egberink; Guy Vanden Mooter; Willy J Peumans; Els J M Van Damme; Dominique Schols
Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection.
Antimicrobial agents and chemotherapy 2004;48(10):3858-70.
2004: Sigrid Hatse; Katrien Princen; Sandra Liekens; Kurt Vermeire; Erik De Clercq; Dominique Schols
Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 2004;61(2):178-88.
2004: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Kurt Vermeire; Erik De Clercq; Willy J Peumans; Els Van Damme; Anne-Mieke Vandamme; Anders Bölmstedt; Dominique Schols; Anders Böhlmstedt
Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins.
Journal of virology 2004;78(19):10617-27.
2004: Leen De Bolle; Sigrid Hatse; Erik Verbeken; Erik De Clercq; Lieve Naesens
Human herpesvirus 6 infection arrests cord blood mononuclear cells in G(2) phase of the cell cycle.
FEBS letters 2004;560(1-3):25-9.
2004: Katrien Princen; Sigrid Hatse; Kurt Vermeire; Erik De Clercq; Dominique Schols
Establishment of a novel CCR5 and CXCR4 expressing CD4+ cell line which is highly sensitive to HIV and suitable for high-throughput evaluation of CCR5 and CXCR4 antagonists.
Retrovirology 2004;1():2.
2003: Katrien Princen; Sigrid Hatse; Kurt Vermeire; Gary J Bridger; Renato T Skerlj; Erik De Clercq; Dominique Schols
The antiviral activity of the CXCR4 antagonist AMD3100 is independent of the cytokine-induced CXCR4/HIV coreceptor expression level.
AIDS research and human retroviruses 2003;19(12):1135-9.
2003: Sigrid Hatse; Katrien Princen; Kurt Vermeire; Lars-Ole Gerlach; Mette M Rosenkilde; Thue W Schwartz; Gary J Bridger; Erik De Clercq; Dominique Schols
Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entry.
FEBS letters 2003;546(2-3):300-6.
2003: Sigrid Hatse; Gary J Bridger; Erik De Clercq; Dominique Schols
X4 HIV-1 induces neuroblastoma cell death by interference with CXCL12/CXCR4 interaction.
Cellular and molecular biology (Noisy-le-Grand, France) 2003;49 Online Pub():OL443-52.
2003: Katrien Princen; Sigrid Hatse; Kurt Vermeire; Erik De Clercq; Dominique Schols
Evaluation of SDF-1/CXCR4-induced Ca2+ signaling by fluorometric imaging plate reader (FLIPR) and flow cytometry.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 2003;51(1):35-45.
2002: Kurt Vermeire; Ying Zhang; Katrien Princen; Sigrid Hatse; Meinrado F Samala; Kaka Dey; Heung-Jin Choi; Youngmi Ahn; Andrej Sodoma; Robert Snoeck; Graciela Andrei; Erik De Clercq; Thomas W Bell; Dominique Schols
CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor.
Virology 2002;302(2):342-53.
2002: Sigrid Hatse; Katrien Princen; Gary J Bridger; Erik De Clercq; Dominique Schols
Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
FEBS letters 2002;527(1-3):255-62.
2002: Janardhan Sampath; Masashi Adachi; Sigrid Hatse; Lieve Naesens; J Balzarini; Robin M Flatley; Larry H Matherly; John D Schuetz
Role of MRP4 and MRP5 in biology and chemotherapy.
AAPS pharmSci 2002;4(3):E14.
2001: Patrick Matthys; Sigrid Hatse; Kurt Vermeire; Anja Wuyts; Gary J Bridger; Geoffrey Henson; Erik De Clercq; An D Billiau; Dominique Schols
AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine receptor CXCR4, inhibits autoimmune joint inflammation in IFN-gamma receptor-deficient mice.
Journal of immunology (Baltimore, Md. : 1950) 2001;167(8):4686-92.
2001: Sigrid Hatse; Katrien Princen; Lars-Ole Gerlach; Gary J Bridger; Geoffrey Henson; Erik De Clercq; Thue W Schwartz; Dominique Schols
Mutation of Asp(171) and Asp(262) of the chemokine receptor CXCR4 impairs its coreceptor function for human immunodeficiency virus-1 entry and abrogates the antagonistic activity of AMD3100.
Molecular pharmacology 2001;60(1):164-73.
2000: Jan Balzarini; B Degrève; Sigrid Hatse; Erik De Clercq; Michael Breuer; M Johansson; Roger Huybrechts; Anna Karlsson
The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides.
Molecular pharmacology 2000;57(4):811-9.
2000: Ying Zhang; Sigrid Hatse; Erik De Clercq; Dominique Schols
CXC-chemokine receptor 4 is not a coreceptor for human herpesvirus 7 entry into CD4(+) T cells.
Journal of virology 2000;74(4):2011-6.
2000: Dirk Daelemans; Dominique Schols; Myriam Witvrouw; Christophe Pannecouque; Sigrid Hatse; Sonia Van Dooren; François Hamy; Thomas Klimkait; Erik De Clercq; Anne-Mieke Vandamme
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
Molecular pharmacology 2000;57(1):116-24.
1999: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
Biochemical pharmacology 1999;58(4):539-55.
1999: Sigrid Hatse; Lieve Naesens; Erik De Clercq; Jan Balzarini
N6-cyclopropyl-PMEDAP: a novel derivative of 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) with distinct metabolic, antiproliferative, and differentiation-inducing properties.
Biochemical pharmacology 1999;58(2):311-23.
1999: Erik De Clercq; Graciela Andrei; Jan Balzarini; Sigrid Hatse; Sandra Liekens; Lieve Naesens; Johan Neyts; Robert Snoeck
Antitumor potential of acyclic nucleoside phosphonates.
Nucleosides & nucleotides 1999;18(4-5):759-71.
1999: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Impact of 9-(2-phosphonylmethoxyethyl)adenine on (deoxy)ribonucleotide metabolism and nucleic acid synthesis in tumor cells.
FEBS letters 1999;445(1):92-7.
1999: Lieve Naesens; Sigrid Hatse; Constant Segers; Erik Verbeken; Erik De Clercq; Mark Waer; Jan Balzarini
9-(2-phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine: a novel prodrug of 9-(2-phosphonylmethoxyethyl)guanine with improved antitumor efficacy and selectivity in choriocarcinoma-bearing rats.
Oncology research 1999;11(4):195-203.
1998: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Enhanced 9-(2-phosphonylmethoxyethyl)adenine secretion by a specific, indomethacin-sensitive efflux pump in a mutant 9-(2-phosphonylmethoxyethyl)adenine-resistant human erythroleukemia K562 cell line.
Molecular pharmacology 1998;54(5):907-17.
1998: Sigrid Hatse; Lieve Naesens; Erik De Clercq; Jan Balzarini
Potent differentiation-inducing properties of the antiretroviral agent 9-(2-phosphonylmethoxyethyl) adenine (PMEA) in the rat choriocarcinoma (RCHO) tumor cell model.
Biochemical pharmacology 1998;56(7):851-9.
1998: Sigrid Hatse; Lieve Naesens; B Degrève; Constant Segers; Michel Vandeputte; Mark Waer; Erik De Clercq; Jan Balzarini
Potent antitumor activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine in choriocarcinoma-bearing rats.
International journal of cancer. Journal international du cancer 1998;76(4):595-600.
1998: Jan Balzarini; Sigrid Hatse; Lieve Naesens; Erik De Clercq
Selection and characterisation of murine leukaemia L1210 cells with high-level resistance to the cytostatic activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl) adenine (PMEA).
Biochimica et biophysica acta 1998;1402(1):29-38.
1998: Pieter Annaert; Gilles Gosselin; A Pompon; S Benzaria; G Valette; Jean-Louis Imbach; Lieve Naesens; Sigrid Hatse; Erik De Clercq; Guy Van den Mooter; Renaat Kinget; Patrick Augustijns
Comparison of the disposition of ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 monolayers.
Pharmaceutical research 1998;15(2):239-45.
1998: Sigrid Hatse; Lieve Naesens; B Degrève; Michel Vandeputte; Mark Waer; Erik De Clercq; Jan Balzarini
In vitro and in vivo inhibitory activity of the differentiation-inducing agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against rat choriocarcinoma.
Advances in experimental medicine and biology 1998;431():605-9.
1996: Sigrid Hatse; E De Clercq; Jan Balzarini
Evidence for distinction of the differentiation-inducing activities and cytostatic properties of 9-(2-phosphonylmethoxyethyl)adenine and a variety of differentiation-inducing agents in human erythroleukemia K562 cells.
Molecular pharmacology 1996;50(5):1231-42.
1995: Jan Balzarini; Annemieke Verstuyf; Sigrid Hatse; Jozef Goebels; H Sobis; Michel Vandeputte; E De Clercq
The human immunodeficiency virus(HIV) inhibitor 9-(2-phosphonylmethoxyethyl)adenine (PMEA) is a strong inducer of differentiation of several tumor cell lines.
International journal of cancer. Journal international du cancer 1995;61(1):130-7.