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Geoffrey Henson

Research Profile

Chemicals & Drugs

Physiology

Virus Replication

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Publications

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Claire Bourdin; Andrea Brancale; K Dawn Bryant; Stanley Chamberlain; Babita Ganguly; Elena Gorovits; Geoffrey Henson; Damound Hunley; Jeff Hutchins; Alexander Kolykhalov; Christopher McGuigan; Jerry Muhammad; Aleksandr Obikhod; Joseph Patti; Changalvala V S Ramamurty; Srinivas K Battina; Blair Bleiman; John Vernachio; C Robin Walters; Jin Wang; C Srivinas Rao
Synthesis and evaluation against hepatitis C virus of 7-deaza analogues of 2'-C-methyl-6-O-methyl guanosine nucleoside and L-Alanine ester phosphoramidates.
Christopher McGuigan; Changalvala V S Ramamurty; C Srinivas Rao; John Vernachio; Arnaud Gilles; Andrea Hall; Geoffrey Henson; Jeff Hutchins; Alexander Kolykhalov; Karolina Madela; Mohamed Aljarah; Srinivas K Battina; Stanley Chamberlain
Dual pro-drugs of 2'-C-methyl guanosine monophosphate as potent and selective inhibitors of hepatitis C virus.
Helen S Pentikis; Mark Matson; George Atiee; Brian Boehlecke; Jeff T Hutchins; Joseph M Patti; Geoffrey Henson; Amy Morris
Pharmacokinetics and safety of FV-100, a novel oral anti-herpes zoster nucleoside analogue, administered in single and multiple doses to healthy young adult and elderly adult volunteers.

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All Publications

2013: Claire Bourdin; Andrea Brancale; K Dawn Bryant; Stanley Chamberlain; Babita Ganguly; Elena Gorovits; Geoffrey Henson; Damound Hunley; Jeff Hutchins; Alexander Kolykhalov; Christopher McGuigan; Jerry Muhammad; Aleksandr Obikhod; Joseph Patti; Changalvala V S Ramamurty; Srinivas K Battina; Blair Bleiman; John Vernachio; C Robin Walters; Jin Wang; C Srivinas Rao
Synthesis and evaluation against hepatitis C virus of 7-deaza analogues of 2'-C-methyl-6-O-methyl guanosine nucleoside and L-Alanine ester phosphoramidates.
Bioorganic & medicinal chemistry letters 2013;23(7):2260-4.
2011: Christopher McGuigan; Changalvala V S Ramamurty; C Srinivas Rao; John Vernachio; Arnaud Gilles; Andrea Hall; Geoffrey Henson; Jeff Hutchins; Alexander Kolykhalov; Karolina Madela; Mohamed Aljarah; Srinivas K Battina; Stanley Chamberlain
Dual pro-drugs of 2'-C-methyl guanosine monophosphate as potent and selective inhibitors of hepatitis C virus.
Bioorganic & medicinal chemistry letters 2011;21(19):6007-12.
2011: Helen S Pentikis; Mark Matson; George Atiee; Brian Boehlecke; Jeff T Hutchins; Joseph M Patti; Geoffrey Henson; Amy Morris
Pharmacokinetics and safety of FV-100, a novel oral anti-herpes zoster nucleoside analogue, administered in single and multiple doses to healthy young adult and elderly adult volunteers.
Antimicrobial agents and chemotherapy 2011;55(6):2847-54.
2011: John H Vernachio; Blair Bleiman; K Dawn Bryant; Stanley Chamberlain; Damound Hunley; Jeff Hutchins; Brenda Ames; Elena L Gorovits; Babita Ganguly; Andrea Hall; Alexander Kolykhalov; Yule Liu; Jerry Muhammad; Nicholas Raja; C Robin Walters; Jin Wang; Karen Williams; Joseph M Patti; Geoffrey Henson; Karolina Madela; Mohamed Aljarah; Arnaud Gilles; Christopher McGuigan
INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties.
Antimicrobial agents and chemotherapy 2011;55(5):1843-51.
2010: Christopher McGuigan; Karolina Madela; Mohamed Aljarah; Arnaud Gilles; Andrea Brancale; Nicola Zonta; Stanley Chamberlain; John Vernachio; Jeff Hutchins; Andrea Hall; Brenda Ames; Elena Gorovits; Babita Ganguly; Alexander Kolykhalov; Jin Wang; Jerry Muhammad; Joseph M Patti; Geoffrey Henson
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.
Bioorganic & medicinal chemistry letters 2010;20(16):4850-4.
2010: Christopher McGuigan; Arnaud Gilles; Karolina Madela; Mohamed Aljarah; Sabrina Holl; Sarah Jones; John Vernachio; Jeff Hutchins; Brenda Ames; K Dawn Bryant; Elena Gorovits; Babita Ganguly; Damound Hunley; Andrea Hall; Alexander Kolykhalov; Yule Liu; Jerry Muhammad; Nicholas Raja; Robin Walters; Jin Wang; Stanley Chamberlain; Geoffrey Henson
Phosphoramidate ProTides of 2'-C-methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties.
Journal of medicinal chemistry 2010;53(13):4949-57.
2009: Christopher McGuigan; Marco Derudas; Maurizio Quintiliani; Graciela Andrei; Robert Snoeck; Geoffrey Henson; Jan Balzarini
2'-Fluorosugar analogues of the highly potent anti-varicella-zoster virus bicyclic nucleoside analogue (BCNA) Cf 1743.
Bioorganic & medicinal chemistry letters 2009;19(22):6264-7.
2007: Marco D Migliore; Nicola Zonta; Christopher McGuigan; Geoffrey Henson; Graciela Andrei; Robert Snoeck; Jan Balzarini
Synthesis and antiviral activity of the carbocyclic analogue of the highly potent and selective anti-VZV bicyclo furano pyrimidines.
Journal of medicinal chemistry 2007;50(26):6485-92.
2007: Christopher McGuigan; Ranjith N Pathirana; Marco Migliore; Rina Adak; Giovanna M Luoni; Arwyn T Jones; Alberto Díez-Torrubia; Maria-Jose Camarasa; Sonsoles Velázquez; Geoffrey Henson; Erik Verbeken; Rebecca Sienaert; Lieve Naesens; Robert Snoeck; Graciela Andrei; Jan Balzarini
Preclinical development of bicyclic nucleoside analogues as potent and selective inhibitors of varicella zoster virus.
The Journal of antimicrobial chemotherapy 2007;60(6):1316-30.
2004: Craig W Hendrix; Ann C Collier; Michael M Lederman; Dominique Schols; Richard B Pollard; Stephen Brown; J Brooks Jackson; Robert W Coombs; Marshall J Glesby; Charles Flexner; Gary J Bridger; Karin Badel; Ronald T MacFarland; Geoffrey Henson; Gary Calandra
Safety, pharmacokinetics, and antiviral activity of AMD3100, a selective CXCR4 receptor inhibitor, in HIV-1 infection.
Journal of acquired immune deficiency syndromes (1999) 2004;37(2):1253-62.
2004: Kai Hübel; W Conrad Liles; Hal E Broxmeyer; Elin Rodger; Brent Wood; Scott Cooper; Giao Hangoc; Ronald T MacFarland; Gary J Bridger; Geoffrey Henson; Gary Calandra; David C Dale
Leukocytosis and Mobilization of CD34+ Hematopoietic Progenitor Cells by AMD3100, a CXCR4 Antagonist.
Supportive cancer therapy 2004;1(3):165-72.
2003: W Conrad Liles; Hal E Broxmeyer; Elin Rodger; Brent Wood; Kai Hübel; Scott Cooper; Giao Hangoc; Gary J Bridger; Geoffrey Henson; Gary Calandra; David C Dale
Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist.
Blood 2003;102(8):2728-30.
2003: Geoffrey Henson
Inhibition of HIV by chemokine receptor antagonists: exciting new targets, complex development.
Expert review of anti-infective therapy 2003;1(3):347-9.
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: Craig W Hendrix; Charles Flexner; Ronald T MacFarland; C Giandomenico; Edward J Fuchs; E Redpath; Gary J Bridger; Geoffrey Henson
Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers.
Antimicrobial agents and chemotherapy 2000;44(6):1667-73.
2000: Julià Blanco; Jordi Barretina; Geoffrey Henson; Gary J Bridger; Erik De Clercq; Bonaventura Clotet; José A Esté
The CXCR4 antagonist AMD3100 efficiently inhibits cell-surface-expressed human immunodeficiency virus type 1 envelope-induced apoptosis.
Antimicrobial agents and chemotherapy 2000;44(1):51-6.
1999: Gary J Bridger; Renato T Skerlj; S Padmanabhan; S A Martellucci; Geoffrey Henson; Sofie Struyf; Myriam Witvrouw; Dominique Schols; Erik De Clercq
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.
Journal of medicinal chemistry 1999;42(19):3971-81.
1999: Jan Van Gelder; Myriam Witvrouw; Christophe Pannecouque; Geoffrey Henson; Gary J Bridger; Lieve Naesens; Erik De Clercq; Pieter Annaert; Manijeh Shafiee; Guy Van den Mooter; Renaat Kinget; Patrick Augustijns
Evaluation of the potential of ion pair formation to improve the oral absorption of two potent antiviral compounds, AMD3100 and PMPA.
International journal of pharmaceutics 1999;186(2):127-36.
1999: Herman F Egberink; Erik De Clercq; Arno L W van Vliet; J Balzarini; Gary J Bridger; Geoffrey Henson; Marian C Horzinek; Dominique Schols
Bicyclams, selective antagonists of the human chemokine receptor CXCR4, potently inhibit feline immunodeficiency virus replication.
Journal of virology 1999;73(8):6346-52.
1999: José A Esté; C Cabrera; Julià Blanco; A Gutierrez; Gary J Bridger; Geoffrey Henson; Bonaventura Clotet; Dominique Schols; Erik De Clercq
Shift of clinical human immunodeficiency virus type 1 isolates from X4 to R5 and prevention of emergence of the syncytium-inducing phenotype by blockade of CXCR4.
Journal of virology 1999;73(7):5577-85.
1999: José A Esté; C Cabrera; Erik De Clercq; Sofie Struyf; J Van Damme; Gary J Bridger; Renato T Skerlj; M J Abrams; Geoffrey Henson; A Gutierrez; Bonaventura Clotet; Dominique Schols
Activity of different bicyclam derivatives against human immunodeficiency virus depends on their interaction with the CXCR4 chemokine receptor.
Molecular pharmacology 1999;55(1):67-73.
1998: G A Donzella; Dominique Schols; SW Lin; José A Esté; Kirsten A Nagashima; Paul J Maddon; GP Allaway; Thomas P Sakmar; Geoffrey Henson; Erik De Clercq; John P Moore
AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor.
Nature medicine 1998;4(1):72-7.
1997: Dominique Schols; Sofie Struyf; J Van Damme; José A Esté; Geoffrey Henson; Erik De Clercq
Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4.
The Journal of experimental medicine 1997;186(8):1383-8.
1997: Dominique Schols; José A Esté; Geoffrey Henson; Erik De Clercq
Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4.
Antiviral research 1997;35(3):147-56.
1997: M E Ultee; GJ Bridger; MJ Abrams; C B Longley; C A Burton; S K Larsen; Geoffrey Henson; S Padmanabhan; F E Gaul; D A Schwartz
Tumor imaging with technetium-99m-labeled hydrazinonicotinamide-Fab' conjugates.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine 1997;38(1):133-8.
1996: Gary J Bridger; M J Abrams; S Padmanabhan; F Gaul; S Larsen; Geoffrey Henson; D A Schwartz; C B Longley; C A Burton; M E Ultee
A comparison of cleavable and noncleavable hydrazinopyridine linkers for the 99mTc labeling of Fab' monoclonal antibody fragments.
Bioconjugate chemistry 1996;7(2):255-64.
1996: José A Esté; K De Vreese; Myriam Witvrouw; Jean-Claude Schmit; Anne-Mieke Vandamme; Jozef Anne; Jan Desmyter; Geoffrey Henson; Gary J Bridger; E De Clercq
Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1.
Antiviral research 1996;29(2-3):297-307.
1996: K De Vreese; D Reymen; P Griffin; Alexander Steinkasserer; G Werner; Gary J Bridger; José A Esté; W James; Geoffrey Henson; Jan Desmyter; Jozef Anne; I De Clercq
The bicyclams, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding.
Antiviral research 1996;29(2-3):209-19.
1996: Gary J Bridger; Renato T Skerlj; S Padmanabhan; S A Martellucci; Geoffrey Henson; M J Abrams; H C Joao; Myriam Witvrouw; K De Vreese; Rudi Pauwels; E De Clercq
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit human immunodeficiency virus replication. 2. Effect of heteroaromatic linkers on the activity of bicyclams.
Journal of medicinal chemistry 1996;39(1):109-19.
1995: H C Joao; K De Vreese; Rudi Pauwels; E De Clercq; Geoffrey Henson; Gary J Bridger
Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors.
Journal of medicinal chemistry 1995;38(19):3865-73.
1995: Gary J Bridger; Renato T Skerlj; D Thornton; S Padmanabhan; S A Martellucci; Geoffrey Henson; M J Abrams; N Yamamoto; K De Vreese; Rudi Pauwels
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker.
Journal of medicinal chemistry 1995;38(2):366-78.
1994: L Ni; F Douglas Boudinot; S G Boudinot; Geoffrey Henson; G E Bossard; S A Martellucci; P W Ash; Simon P Fricker; M C Darkes; B R Theobald
Pharmacokinetics of antiviral polyoxometalates in rats.
Antimicrobial agents and chemotherapy 1994;38(3):504-10.