Results of a phase 2 trial of an oral CXCR4 antagonist, mavorixafor, for treatment of WHIM syndrome
Dale, David C., Firkin, Frank, Bolyard, Audrey Anna, Kelley, Merideth, Makaryan, Vahagn, Gorelick, Kenneth J., Ebrahim, Tarek, Garg, Varun, Tang, Weihua, Jiang, Honghua, Skerlj, Renato, Beaussant Cohen, Sarah
Published in Blood (24.12.2020)
Published in Blood (24.12.2020)
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A randomized single and multiple ascending dose study in healthy volunteers of LTI‐291, a centrally penetrant glucocerebrosidase activator
Heijer, Jonas M., Kruithof, Annelieke C., Amerongen, Guido, Kam, Marieke L., Thijssen, Eva, Grievink, Hendrika W., Moerland, Matthijs, Walker, Mike, Been, Kees, Skerlj, Renato, Justman, Craig, Dudgeon, Lindsay, Lansbury, Peter, Cullen, Valerie C., Hilt, Dana C., Groeneveld, Geert Jan
Published in British journal of clinical pharmacology (01.09.2021)
Published in British journal of clinical pharmacology (01.09.2021)
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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
Skerlj, Renato T, Bridger, Gary J, Kaller, Al, McEachern, Ernest J, Crawford, Jason B, Zhou, Yuanxi, Atsma, Bem, Langille, Jonathon, Nan, Susan, Veale, Duane, Wilson, Trevor, Harwig, Curtis, Hatse, Sigrid, Princen, Katrien, De Clercq, Erik, Schols, Dominique
Published in Journal of medicinal chemistry (22.04.2010)
Published in Journal of medicinal chemistry (22.04.2010)
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Molecular Mechanism of Action of Monocyclam Versus Bicyclam Non-peptide Antagonists in the CXCR4 Chemokine Receptor
Rosenkilde, Mette M., Gerlach, Lars-Ole, Hatse, Sigrid, Skerlj, Renato T., Schols, Dominique, Bridger, Gary J., Schwartz, Thue W.
Published in The Journal of biological chemistry (14.09.2007)
Published in The Journal of biological chemistry (14.09.2007)
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Metal compounds for the treatment of parasitic diseases
Fricker, Simon P., Mosi, Renee M., Cameron, Beth R., Baird, Ian, Zhu, Youngbao, Anastassov, Virginia, Cox, Jennifer, Doyle, Patricia S., Hansell, Elizabeth, Lau, Gloria, Langille, Jonathan, Olsen, Micki, Qin, Ling, Skerlj, Renato, Wong, Rebecca S.Y., Santucci, Zefferino, McKerrow, James H.
Published in Journal of inorganic biochemistry (01.10.2008)
Published in Journal of inorganic biochemistry (01.10.2008)
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Inhibition of the cathepsin cysteine proteases B and K by square-planar cycloaurated gold(III) compounds and investigation of their anti-cancer activity
Zhu, Yongbao, Cameron, Beth R., Mosi, Renee, Anastassov, Virginia, Cox, Jennifer, Qin, Ling, Santucci, Zefferino, Metz, Markus, Skerlj, Renato T., Fricker, Simon P.
Published in Journal of inorganic biochemistry (01.05.2011)
Published in Journal of inorganic biochemistry (01.05.2011)
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The molecular pharmacology of AMD11070: An orally bioavailable CXCR4 HIV entry inhibitor
Mosi, Renee M., Anastassova, Virginia, Cox, Jennifer, Darkes, Marilyn C., Idzan, Stefan R., Labrecque, Jean, Lau, Gloria, Nelson, Kim L., Patel, Ketan, Santucci, Zefferino, Wong, Rebecca S.Y., Skerlj, Renato T., Bridger, Gary J., Huskens, Dana, Schols, Dominique, Fricker, Simon P.
Published in Biochemical pharmacology (15.02.2012)
Published in Biochemical pharmacology (15.02.2012)
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Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor
Rosenkilde, Mette M, Gerlach, Lars-Ole, Jakobsen, Janus S, Skerlj, Renato T, Bridger, Gary J, Schwartz, Thue W
Published in The Journal of biological chemistry (23.01.2004)
Published in The Journal of biological chemistry (23.01.2004)
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Journal Article
AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor
Hatse, Sigrid, Princen, Katrien, Clercq, Erik De, Rosenkilde, Mette M., Schwartz, Thue W., Hernandez-Abad, Pedro E., Skerlj, Renato T., Bridger, Gary J., Schols, Dominique
Published in Biochemical pharmacology (01.09.2005)
Published in Biochemical pharmacology (01.09.2005)
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Journal Article
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
Bridger, Gary J, Skerlj, Renato T, Hernandez-Abad, Pedro E, Bogucki, David E, Wang, Zhongren, Zhou, Yuanxi, Nan, Susan, Boehringer, Eva M, Wilson, Trevor, Crawford, Jason, Metz, Markus, Hatse, Sigrid, Princen, Katrien, De Clercq, Erik, Schols, Dominique
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
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Implications of Promiscuous Pim-1 Kinase Fragment Inhibitor Hydrophobic Interactions for Fragment-Based Drug Design
Good, Andrew C, Liu, Jinyu, Hirth, Bradford, Asmussen, Gary, Xiang, Yibin, Biemann, Hans-Peter, Bishop, Kimberly A, Fremgen, Trisha, Fitzgerald, Maria, Gladysheva, Tatiana, Jain, Annuradha, Jancsics, Katherine, Metz, Markus, Papoulis, Andrew, Skerlj, Renato, Stepp, J. David, Wei, Ronnie R
Published in Journal of medicinal chemistry (22.03.2012)
Published in Journal of medicinal chemistry (22.03.2012)
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Spontaneous Enzymatically Mediated Dynamic Kinetic Resolution of 8-Amino-5,6,7,8-tetrahydroquinoline
Crawford, Jason B, Skerlj, Renato T, Bridger, Gary J
Published in Journal of organic chemistry (19.01.2007)
Published in Journal of organic chemistry (19.01.2007)
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Journal Article
HIV - 1 entry inhibition by small - molecule CCR5 antagonists: A combined molecular modeling and mutant study using a high - throughput assay
Labrecque, Jean, Metz, Markus, Lau, Gloria, Darkes, Marilyn C, Wong, Rebecca S.Y, Bogucki, David, Carpenter, Bryon, Chen, Gang, Li, Tongshuang, Nan, Susan, Schols, Dominique, Bridger, Gary J, Fricker, Simon P, Skerlj, Renato T
Published in Virology (New York, N.Y.) (10.05.2011)
Published in Virology (New York, N.Y.) (10.05.2011)
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Rhenium Inhibitors of Cathepsin B (ReO(SYS)X (Where Y = S, py; X = Cl, Br, SPhOMe-p)): Synthesis and Mechanism of Inhibition
Mosi, Renee, Baird, Ian R, Cox, Jennifer, Anastassov, Virginia, Cameron, Beth, Skerlj, Renato T, Fricker, Simon P
Published in Journal of medicinal chemistry (24.08.2006)
Published in Journal of medicinal chemistry (24.08.2006)
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Journal Article
Prospective CCR5 Small Molecule Antagonist Compound Design Using a Combined Mutagenesis/Modeling Approach
Metz, Markus, Bourque, Elyse, Labrecque, Jean, Danthi, Sanjay J, Langille, Jonathan, Harwig, Curtis, Yang, Wen, Darkes, Marilyn C, Lau, Gloria, Santucci, Zefferino, Bridger, Gary J, Schols, Dominique, Fricker, Simon P, Skerlj, Renato T
Published in Journal of the American Chemical Society (19.10.2011)
Published in Journal of the American Chemical Society (19.10.2011)
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Journal Article
Inhibition of Human Immunodeficiency Virus Replication by a Dual CCR5/CXCR4 Antagonist
PRINCEN, Katrien, HATSE, Sigrid, SCHOLS, Dominique, VERMEIRE, Kurt, AQUARO, Stefano, DE CLERCQ, Erik, GERLACH, Lars-Ole, ROSENKILDE, Mette, SCHWARTZ, Thue W, SKERLJ, Renato, BRIDGER, Gary
Published in Journal of Virology (01.12.2004)
Published in Journal of Virology (01.12.2004)
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Journal Article
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria
Skerlj, Renato T, Bastos, Cecilia M, Booker, Michael L, Kramer, Martin L, Barker, Robert H, Celatka, Cassandra A, O’Shea, Thomas J, Munoz, Benito, Sidhu, Amar Bir, Cortese, Joseph F, Wittlin, Sergio, Papastogiannidis, Petros, Angulo-Barturen, Inigo, Jimenez-Diaz, Maria Belen, Sybertz, Edmund
Published in ACS medicinal chemistry letters (08.09.2011)
Published in ACS medicinal chemistry letters (08.09.2011)
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