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Items: 1 to 50 of 51

1.

Identifying the molecular target sites for CFTR potentiators GLPG1837 and VX-770.

Yeh HI, Qiu L, Sohma Y, Conrath K, Zou X, Hwang TC.

J Gen Physiol. 2019 Jul 1;151(7):912-928. doi: 10.1085/jgp.201912360. Epub 2019 Jun 4.

PMID:
31164398
2.

GLPG1837, a CFTR potentiator, in p.Gly551Asp (G551D)-CF patients: An open-label, single-arm, phase 2a study (SAPHIRA1).

Davies JC, Van de Steen O, van Koningsbruggen-Rietschel S, Drevinek P, Derichs N, McKone EF, Kanters D, Allamassey L, Namour F, de Kock H, Conrath K.

J Cyst Fibros. 2019 May 27. pii: S1569-1993(19)30111-0. doi: 10.1016/j.jcf.2019.05.006. [Epub ahead of print]

3.

Identification of GLPG/ABBV-2737, a Novel Class of Corrector, Which Exerts Functional Synergy With Other CFTR Modulators.

de Wilde G, Gees M, Musch S, Verdonck K, Jans M, Wesse AS, Singh AK, Hwang TC, Christophe T, Pizzonero M, Van der Plas S, Desroy N, Cowart M, Stouten P, Nelles L, Conrath K.

Front Pharmacol. 2019 May 9;10:514. doi: 10.3389/fphar.2019.00514. eCollection 2019.

4.

CFTR activity is enhanced by the novel corrector GLPG2222, given with and without ivacaftor in two randomized trials.

Bell SC, Barry PJ, De Boeck K, Drevinek P, Elborn JS, Plant BJ, Minić P, Van Braeckel E, Verhulst S, Muller K, Kanters D, Bellaire S, de Kock H, Geller DE, Conrath K, Van de Steen O, van der Ent K.

J Cyst Fibros. 2019 May 2. pii: S1569-1993(19)30073-6. doi: 10.1016/j.jcf.2019.04.014. [Epub ahead of print]

5.

Identification and Characterization of Novel CFTR Potentiators.

Gees M, Musch S, Van der Plas S, Wesse AS, Vandevelde A, Verdonck K, Mammoliti O, Hwang TC, Sonck K, Stouten P, Swensen AM, Jans M, Van der Schueren J, Nelles L, Andrews M, Conrath K.

Front Pharmacol. 2018 Oct 26;9:1221. doi: 10.3389/fphar.2018.01221. eCollection 2018.

6.

Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors.

Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.

J Med Chem. 2018 May 10;61(9):4270. doi: 10.1021/acs.jmedchem.8b00579. Epub 2018 Apr 19. No abstract available.

PMID:
29672037
7.

Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.

Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M.

J Med Chem. 2018 Feb 22;61(4):1425-1435. doi: 10.1021/acs.jmedchem.7b01288. Epub 2018 Jan 10.

PMID:
29148763
8.

A common mechanism for CFTR potentiators.

Yeh HI, Sohma Y, Conrath K, Hwang TC.

J Gen Physiol. 2017 Dec 4;149(12):1105-1118. doi: 10.1085/jgp.201711886. Epub 2017 Oct 27.

9.

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.

Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.

J Med Chem. 2017 Sep 14;60(17):7371-7392. doi: 10.1021/acs.jmedchem.7b00647. Epub 2017 Aug 18. Erratum in: J Med Chem. 2018 May 10;61(9):4270.

PMID:
28731719
10.

Solution conformation and flexibility of capsular polysaccharides from Neisseria meningitidis and glycoconjugates with the tetanus toxoid protein.

Abdelhameed AS, Morris GA, Almutairi F, Adams GG, Duvivier P, Conrath K, Harding SE.

Sci Rep. 2016 Oct 26;6:35588. doi: 10.1038/srep35588.

11.

A glycoconjugate of Haemophilus influenzae Type b capsular polysaccharide with tetanus toxoid protein: hydrodynamic properties mainly influenced by the carbohydrate.

Abdelhameed AS, Adams GG, Morris GA, Almutairi FM, Duvivier P, Conrath K, Harding SE.

Sci Rep. 2016 Feb 26;6:22208. doi: 10.1038/srep22208.

12.

Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.

MacLeod AM, Mitchell DR, Palmer NJ, Van de Poël H, Conrath K, Andrews M, Leyssen P, Neyts J.

ACS Med Chem Lett. 2013 May 8;4(7):585-9. doi: 10.1021/ml400095m. eCollection 2013 Jul 11.

13.

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C.

J Immunol. 2013 Oct 1;191(7):3568-77. doi: 10.4049/jimmunol.1201348. Epub 2013 Sep 4.

14.

A novel, broad-spectrum inhibitor of enterovirus replication that targets host cell factor phosphatidylinositol 4-kinase IIIβ.

van der Schaar HM, Leyssen P, Thibaut HJ, de Palma A, van der Linden L, Lanke KH, Lacroix C, Verbeken E, Conrath K, Macleod AM, Mitchell DR, Palmer NJ, van de Poël H, Andrews M, Neyts J, van Kuppeveld FJ.

Antimicrob Agents Chemother. 2013 Oct;57(10):4971-81. doi: 10.1128/AAC.01175-13. Epub 2013 Jul 29.

15.

An asymmetric and slightly dimerized structure for the tetanus toxoid protein used in glycoconjugate vaccines.

Abdelhameed AS, Morris GA, Adams GG, Rowe AJ, Laloux O, Cerny L, Bonnier B, Duvivier P, Conrath K, Lenfant C, Harding SE.

Carbohydr Polym. 2012 Nov 6;90(4):1831-5. doi: 10.1016/j.carbpol.2012.07.032. Epub 2012 Jul 16.

PMID:
22944454
16.

Solution properties of capsular polysaccharides from Streptococcus pneumoniae.

Harding SE, Abdelhameed AS, Morris GA, Adams G, Laloux O, Cerny L, Bonnier B, Duvivier P, Conrath K, Lenfant C.

Carbohydr Polym. 2012 Sep 1;90(1):237-42. doi: 10.1016/j.carbpol.2012.05.030. Epub 2012 May 15.

PMID:
24751036
17.

A bacterial-two-hybrid selection system for one-step isolation of intracellularly functional Nanobodies.

Pellis M, Pardon E, Zolghadr K, Rothbauer U, Vincke C, Kinne J, Dierynck I, Hertogs K, Leonhardt H, Messens J, Muyldermans S, Conrath K.

Arch Biochem Biophys. 2012 Oct 15;526(2):114-23. doi: 10.1016/j.abb.2012.04.023. Epub 2012 May 11.

PMID:
22583807
18.

Dual beneficial effect of interloop disulfide bond for single domain antibody fragments.

Govaert J, Pellis M, Deschacht N, Vincke C, Conrath K, Muyldermans S, Saerens D.

J Biol Chem. 2012 Jan 13;287(3):1970-9. doi: 10.1074/jbc.M111.242818. Epub 2011 Nov 29.

19.

High affinity nanobodies against the Trypanosome brucei VSG are potent trypanolytic agents that block endocytosis.

Stijlemans B, Caljon G, Natesan SK, Saerens D, Conrath K, Pérez-Morga D, Skepper JN, Nikolaou A, Brys L, Pays E, Magez S, Field MC, De Baetselier P, Muyldermans S.

PLoS Pathog. 2011 Jun;7(6):e1002072. doi: 10.1371/journal.ppat.1002072. Epub 2011 Jun 16.

20.

Substrate-dependent modulation of enzyme activity by allosteric effector antibodies.

Barlow JN, Conrath K, Steyaert J.

Biochim Biophys Acta. 2009 Aug;1794(8):1259-68. doi: 10.1016/j.bbapap.2009.03.019. Epub 2009 Apr 5.

PMID:
19348968
21.

Camelid nanobodies raised against an integral membrane enzyme, nitric oxide reductase.

Conrath K, Pereira AS, Martins CE, Timóteo CG, Tavares P, Spinelli S, Kinne J, Flaudrops C, Cambillau C, Muyldermans S, Moura I, Moura JJ, Tegoni M, Desmyter A.

Protein Sci. 2009 Mar;18(3):619-28. doi: 10.1002/pro.69.

22.

Nanobodies, a promising tool for species-specific diagnosis of Taenia solium cysticercosis.

Deckers N, Saerens D, Kanobana K, Conrath K, Victor B, Wernery U, Vercruysse J, Muyldermans S, Dorny P.

Int J Parasitol. 2009 Apr;39(5):625-33. doi: 10.1016/j.ijpara.2008.10.012. Epub 2008 Nov 17.

PMID:
19041315
23.

General strategy to humanize a camelid single-domain antibody and identification of a universal humanized nanobody scaffold.

Vincke C, Loris R, Saerens D, Martinez-Rodriguez S, Muyldermans S, Conrath K.

J Biol Chem. 2009 Jan 30;284(5):3273-84. doi: 10.1074/jbc.M806889200. Epub 2008 Nov 14.

24.

Rapid identification of common hexapyranose monosaccharide units by a simple TOCSY matching approach.

Gheysen K, Mihai C, Conrath K, Martins JC.

Chemistry. 2008;14(29):8869-78. doi: 10.1002/chem.200801081.

PMID:
18729117
25.

VHH, bivalent domains and chimeric Heavy chain-only antibodies with high neutralizing efficacy for scorpion toxin AahI'.

Hmila I, Abdallah R BA, Saerens D, Benlasfar Z, Conrath K, Ayeb ME, Muyldermans S, Bouhaouala-Zahar B.

Mol Immunol. 2008 Aug;45(14):3847-56. doi: 10.1016/j.molimm.2008.04.011. Epub 2008 Jul 9.

PMID:
18614235
26.

Disulfide bond introduction for general stabilization of immunoglobulin heavy-chain variable domains.

Saerens D, Conrath K, Govaert J, Muyldermans S.

J Mol Biol. 2008 Mar 21;377(2):478-88. doi: 10.1016/j.jmb.2008.01.022. Epub 2008 Jan 16.

PMID:
18262543
27.

Parallel selection of multiple anti-infectome Nanobodies without access to purified antigens.

Saerens D, Stijlemans B, Baral TN, Nguyen Thi GT, Wernery U, Magez S, De Baetselier P, Muyldermans S, Conrath K.

J Immunol Methods. 2008 Jan 1;329(1-2):138-50. Epub 2007 Oct 31.

PMID:
17996887
28.

[Experimental therapy of African trypanosomiasis with a nanobody-conjugated human trypanolytic factor].

Baral TN, Magez S, Stijlemans B, Conrath K, Vanhollebeke B, Pays E, Muyldermans S, De Baetselier P.

Med Sci (Paris). 2006 Nov;22(11):914-6. French. No abstract available.

29.

Targeting and tracing antigens in live cells with fluorescent nanobodies.

Rothbauer U, Zolghadr K, Tillib S, Nowak D, Schermelleh L, Gahl A, Backmann N, Conrath K, Muyldermans S, Cardoso MC, Leonhardt H.

Nat Methods. 2006 Nov;3(11):887-9.

PMID:
17060912
30.

Experimental therapy of African trypanosomiasis with a nanobody-conjugated human trypanolytic factor.

Baral TN, Magez S, Stijlemans B, Conrath K, Vanhollebeke B, Pays E, Muyldermans S, De Baetselier P.

Nat Med. 2006 May;12(5):580-4. Epub 2006 Apr 9.

PMID:
16604085
31.

Molecular basis for the preferential cleft recognition by dromedary heavy-chain antibodies.

De Genst E, Silence K, Decanniere K, Conrath K, Loris R, Kinne J, Muyldermans S, Wyns L.

Proc Natl Acad Sci U S A. 2006 Mar 21;103(12):4586-91. Epub 2006 Mar 13.

32.

Neutralisation of venom-induced haemorrhage by IgG from camels and llamas immunised with viper venom and also by endogenous, non-IgG components in camelid sera.

Harrison RA, Hasson SS, Harmsen M, Laing GD, Conrath K, Theakston RD.

Toxicon. 2006 Mar;47(3):364-8. Epub 2005 Dec 15.

PMID:
16359717
33.

Engineering camel single-domain antibodies and immobilization chemistry for human prostate-specific antigen sensing.

Saerens D, Frederix F, Reekmans G, Conrath K, Jans K, Brys L, Huang L, Bosmans E, Maes G, Borghs G, Muyldermans S.

Anal Chem. 2005 Dec 1;77(23):7547-55.

PMID:
16316161
34.

Identification of a universal VHH framework to graft non-canonical antigen-binding loops of camel single-domain antibodies.

Saerens D, Pellis M, Loris R, Pardon E, Dumoulin M, Matagne A, Wyns L, Muyldermans S, Conrath K.

J Mol Biol. 2005 Sep 23;352(3):597-607.

PMID:
16095608
35.

Antibody repertoire development in camelids.

De Genst E, Saerens D, Muyldermans S, Conrath K.

Dev Comp Immunol. 2006;30(1-2):187-98. Review.

PMID:
16051357
36.

Antigen binding and solubility effects upon the veneering of a camel VHH in framework-2 to mimic a VH.

Conrath K, Vincke C, Stijlemans B, Schymkowitz J, Decanniere K, Wyns L, Muyldermans S, Loris R.

J Mol Biol. 2005 Jul 1;350(1):112-25.

PMID:
15913651
37.

Single domain antibodies derived from dromedary lymph node and peripheral blood lymphocytes sensing conformational variants of prostate-specific antigen.

Saerens D, Kinne J, Bosmans E, Wernery U, Muyldermans S, Conrath K.

J Biol Chem. 2004 Dec 10;279(50):51965-72. Epub 2004 Sep 30.

38.

Efficient targeting of conserved cryptic epitopes of infectious agents by single domain antibodies. African trypanosomes as paradigm.

Stijlemans B, Conrath K, Cortez-Retamozo V, Van Xong H, Wyns L, Senter P, Revets H, De Baetselier P, Muyldermans S, Magez S.

J Biol Chem. 2004 Jan 9;279(2):1256-61. Epub 2003 Oct 3.

39.

Emergence and evolution of functional heavy-chain antibodies in Camelidae.

Conrath KE, Wernery U, Muyldermans S, Nguyen VK.

Dev Comp Immunol. 2003 Feb;27(2):87-103. Review.

PMID:
12543123
40.

Efficient tumor targeting by single-domain antibody fragments of camels.

Cortez-Retamozo V, Lauwereys M, Hassanzadeh Gh G, Gobert M, Conrath K, Muyldermans S, De Baetselier P, Revets H.

Int J Cancer. 2002 Mar 20;98(3):456-62.

41.

Biophysical properties of camelid V(HH) domains compared to those of human V(H)3 domains.

Ewert S, Cambillau C, Conrath K, Plückthun A.

Biochemistry. 2002 Mar 19;41(11):3628-36.

PMID:
11888279
42.

Single-domain antibody fragments with high conformational stability.

Dumoulin M, Conrath K, Van Meirhaeghe A, Meersman F, Heremans K, Frenken LG, Muyldermans S, Wyns L, Matagne A.

Protein Sci. 2002 Mar;11(3):500-15.

43.

Beta-lactamase inhibitors derived from single-domain antibody fragments elicited in the camelidae.

Conrath KE, Lauwereys M, Galleni M, Matagne A, Frère JM, Kinne J, Wyns L, Muyldermans S.

Antimicrob Agents Chemother. 2001 Oct;45(10):2807-12.

44.

Phosphorylation of bovine leukemia virus Tax protein is required for in vitro transformation but not for transactivation.

Willems L, Grimonpont C, Kerkhofs P, Capiau C, Gheysen D, Conrath K, Roussef R, Mamoun R, Portetelle D, Burny A, Adam E, Lefèbvre L, Twizere JC, Heremans H, Kettmann R.

Oncogene. 1998 Apr 30;16(17):2165-76.

45.

The topology of the S protein in the yeast-derived hepatitis B surface antigen particles.

Sonveaux N, Conrath K, Capiau C, Brasseur R, Goormaghtigh E, Ruysschaert JM.

J Biol Chem. 1994 Oct 14;269(41):25637-45.

46.

Sequence and structure of the membrane-associated peptide of glycophorin A.

Challou N, Goormaghtigh E, Cabiaux V, Conrath K, Ruysschaert JM.

Biochemistry. 1994 Jun 7;33(22):6902-10.

PMID:
8204624
47.

Topology of diphtheria toxin B fragment inserted in lipid vesicles.

Cabiaux V, Quertenmont P, Conrath K, Brasseur R, Capiau C, Ruysschaert JM.

Mol Microbiol. 1994 Jan;11(1):43-50.

PMID:
8145645
48.

Enzymatic hydrolysis of reconstituted dimyristoylphosphatidylcholine-apo A-I complexes.

Lins L, Piron S, Conrath K, Vanloo B, Brasseur R, Rosseneu M, Baert J, Ruysschaert JM.

Biochim Biophys Acta. 1993 Sep 19;1151(2):137-42.

PMID:
8373788
50.

HLA typing and lymphocytotoxic crossmatches using conventional techniques or immunobeads. A comparative study.

Mueller-Eckhardt G, Kölzow S, Conrath K, Hoffmann O.

Vox Sang. 1991;61(2):99-105.

PMID:
1837194

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