Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Renato, Skerlj"'
Autor:
Katarina, Zmajkovicova, Sumit, Pawar, Sabine, Maier-Munsa, Barbara, Maierhofer, Ivana, Wiest, Renato, Skerlj, Arthur G, Taveras, Adriana, Badarau
Publikováno v:
Genes and immunity. 23(6)
Warts, hypogammaglobulinemia, infections, myelokathexis (WHIM) syndrome is a rare primary immunodeficiency predominantly caused by heterozygous gain-of-function mutations in CXCR4 C-terminus. We assessed genotype-phenotype correlations for known path
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::fc4d613faaa8dc45da0660bdbc6df0c6
https://pubmed.ncbi.nlm.nih.gov/36089616
https://pubmed.ncbi.nlm.nih.gov/36089616
Autor:
Frank C Firkin, David C. Dale, Weihua Tang, Sarah L. Cohen, Audrey Anna Bolyard, Varun Garg, Kenneth J. Gorelick, Vahagn Makaryan, Honghua Jiang, Merideth L. Kelley, Tarek M Ebrahim, Renato Skerlj
Publikováno v:
Blood. 136(26)
Warts, hypogammaglobulinemia, infections, and myelokathexis (WHIM) syndrome is a rare primary immunodeficiency caused by gain-of-function mutations in the CXCR4 gene. We report the safety, tolerability, pharmacokinetics, pharmacodynamics, and prelimi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ddc7fa05a51a626a3064127bd0ece88a
https://pubmed.ncbi.nlm.nih.gov/33367549
https://pubmed.ncbi.nlm.nih.gov/33367549
Publikováno v:
ACS Medicinal Chemistry Letters. 8:22-26
Protein-protein interactions mediate most physiological and disease processes. Helix-constrained peptides potently mimic or inhibit these interactions by making multiple contacts over large surface areas. However, despite high affinities, they typica
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f77a4f522a7ffb0c1911fc91f9b39a5
https://doi.org/10.1021/acsmedchemlett.6b00395
https://doi.org/10.1021/acsmedchemlett.6b00395
Publikováno v:
Tetrahedron Letters. 60:151179
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1d2a6e62178d8f99e911a879dade0696
https://doi.org/10.1016/j.tetlet.2019.151179
https://doi.org/10.1016/j.tetlet.2019.151179
The homochiral complex (RR)-(−)-[(η 5 -C 5 H 5 )Fe(CO)(PPh 3 )]-1-methyl-5-(N-α-methylbenzylcarbamoyl)-1,4-dihydronicotinoyl reduces ethyl benzoylformate to (R)-(−)-ethyl mandelate in 89% enantiomeric excess.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87f2c8d91149063d7c6285fb98bf85fb
https://ora.ox.ac.uk/objects/uuid:af0a2547-e691-480e-916a-c354e84fc536
https://ora.ox.ac.uk/objects/uuid:af0a2547-e691-480e-916a-c354e84fc536
Autor:
Dana Huskens, Marilyn C. Darkes, Gary Bridger, Jennifer H. Cox, Simon P. Fricker, Zefferino Santucci, Renee Mosi, Jean Labrecque, Kim L. Nelson, Renato Skerlj, Stefan R. Idzan, Virginia Anastassova, Dominique Schols, Ketan Patel, Rebecca S.Y. Wong, Gloria Lau
Publikováno v:
Biochemical Pharmacology. 83:472-479
In order to enter and infect human cells HIV must bind to CD4 in addition to either the CXCR4 or the CCR5 chemokine receptor. AMD11070 was the first orally available small molecule antagonist of CXCR4 to enter the clinic. Herein we report the molecul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e84cfd78fc63d6410dc6820fa5f20b2e
https://doi.org/10.1016/j.bcp.2011.11.020
https://doi.org/10.1016/j.bcp.2011.11.020
Autor:
Renato Skerlj, Tuya Ba, Ernest J. McEachern, Elyse Bourque, Ian Baird, Dominique Schols, Wilson Trevor R, Renee Mosi, Jonathan Langille, Yuanxi Zhou, Bryon Carpenter, Michael Bey, Simon P. Fricker, Dana Huskens, Duane Veale, Rebecca S.Y. Wong, Gary Bridger, Curtis Harwig, Veronique Bodart, Ron MacFarland, Markus Metz, Sanjay Danthi
Publikováno v:
ACS Medicinal Chemistry Letters. 3:216-221
A series of CCR5 antagonists representing the thiophene-3-yl-methyl ureas were designed that met the pharmacological criteria for HIV-1 inhibition and mitigated a human ether-a-go-go related gene (hERG) inhibition liability. Reducing lipophilicity wa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9674269a09a599b87e9e9ed8edb34dc
https://doi.org/10.1021/ml2002604
https://doi.org/10.1021/ml2002604
Autor:
Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Ernest McEachern, Jonathan Langille, Curtis Harwig, Duane Veale, Wen Yang, Tongshong Li, Yongbao Zhu, Michael Bey, Ian Baird, Michael Sartori, Markus Metz, Renee Mosi, Kim Nelson, Veronique Bodart, Rebecca Wong, Simon Fricker, Ron Mac Farland, Dana Huskens, Dominique Schols
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6950-6954
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe8c7c65ea6806cdd761d65d01e7a8e4
https://doi.org/10.1016/j.bmcl.2011.09.133
https://doi.org/10.1016/j.bmcl.2011.09.133
Autor:
Ling Qin, Renato Skerlj, Yongbao Zhu, Zefferino Santucci, Renee Mosi, Jennifer H. Cox, Simon P. Fricker, Virginia Anastassov, Beth R. Cameron, Markus Metz
Publikováno v:
Journal of Inorganic Biochemistry. 105:754-762
Gold(III) compounds have been examined for potential anti-cancer activity. It is proposed that the molecular targets of these compounds are thiol-containing biological molecules such as the cathepsin cysteine proteases. These enzymes have been implic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8994eb644197fee91831afe72ccfcb4f
https://doi.org/10.1016/j.jinorgbio.2011.01.012
https://doi.org/10.1016/j.jinorgbio.2011.01.012
Autor:
Tong-Shuang Li, Simon P. Fricker, Gang Chen, Renato Skerlj, David Bogucki, Markus Metz, Gary Bridger, Susan Nan, Rebecca S.Y. Wong, Dominique Schols, Jean Labrecque, Gloria Lau, Marilyn C. Darkes, Bryon Carpenter
Publikováno v:
Virology. 413(2):231-243
Based on the attrition rate of CCR5 small molecule antagonists in the clinic the discovery and development of next generation antagonists with an improved pharmacology and safety profile is necessary. Herein, we describe a combined molecular modeling
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1b73eb6084c8734ad98a5cb07350dbd