Zobrazeno 1 - 8 of 8 pro vyhledávání: '"Charles J. Nichols"'
1
Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein–Protein Inhibitors: Two Test Cases Illustrated by IL1β-IL1R and p38α–TAB1 Complexes
Autor: Joseph Chi Fung Ng, Michael S. Marber, Geoff Kelly, Franca Fraternali, Gian Felice De Nicola, Charles J. Nichols, Annika Keshu, Maria R. Conte
Publikováno v: Journal of Medicinal Chemistry. 63:7559-7568
Nowadays, it is possible to combine X-ray crystallography and fragment screening in a medium throughput fashion to chemically probe the surfaces used by proteins to interact and use the outcome of the screens to systematically design protein-protein
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9f7ef4874f6daf8e2b145be3fe02d44
https://doi.org/10.1021/acs.jmedchem.0c00403
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3
Nonpeptide Luteinizing Hormone-Releasing Hormone Antagonists Derived from Erythromycin A: Design, Synthesis, and Biological Activity of Cladinose Replacement Analogues
Autor: Daryl R. Sauer, Jonathan Greer, Charles J. Nichols, Craig D. Wegner, Jason A. Segreti, Kurt M. Mohning, Fortuna Haviv, John T. Randolph, E N Bush, Philip L. Waid, Gilbert Diaz, Leslie M. Besecke, Gary Bammert
Publikováno v: Journal of Medicinal Chemistry. 47:1085-1097
The design and synthesis of a series of 11,12-cyclic carbamate derivatives of 6-O-methylerythromycin A that are novel, nonpeptide LHRH antagonists, is described. The macrolide antagonist 1, discovered during a screen of our chemical repository, was c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fabef2f09ac213c5e8373f774e466e4
https://doi.org/10.1021/jm030418i
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4
In vitro and in vivo activities of reduced-size antagonists of luteinizing hormone-releasing hormone
Autor: Gilbert Diaz, Gary Bammert, Judith Knittle, Jonathan Greer, Charles J. Nichols, Edwin S. Johnson, Eugene N. Bush, Fortuna Haviv, Timothy D. Fitzpatrick, A. T. Nguyen
Publikováno v: Journal of medicinal chemistry. 37(5)
A novel series of octapeptide LHRH antagonists was designed on the basis of the structure of the (2-9) fragment of a LHRH agonist. By adopting a systematic SAR study, we were able to improve first the in vitro activity and then the in vivo LH suppres
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c162d80694001661dca74664a3820a3
https://pubmed.ncbi.nlm.nih.gov/7510341
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6
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists
Autor: Rolf E. Swenson, A. T. Nguyen, George A. Diaz, Charles J. Nichols, Timothy D. Fitzpatrick, Fortuna Haviv, E N Bush, Mort Nicholas A, Gary Bammert, N. S. Rhutasel
Publikováno v: Journal of medicinal chemistry. 36(3)
Each peptide bond in leuprolide (1), deslorelin (13), and nafarelin (24) was separately substituted with N-methyl. The synthesized compounds were tested for in vitro receptor binding, LH release, and stability against chymotrypsin and intestinal degr
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ea76c5aa0f04c3993bf67eb9877f6ff
https://pubmed.ncbi.nlm.nih.gov/8381183
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7
Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics
Autor: D J Hoffman, H Ghanbari, F Haviy, E N Bush, Charles J. Nichols, Timothy D. Fitzpatrick, H N Nellans, Rolf E. Swenson, A. T. Nguyen, Gilbert Diaz
Publikováno v: Journal of medicinal chemistry. 35(21)
To stabilize leuprolide (1) against chymotrypsin and intestinal degradation several agonists of LHRH (2-12), modified at position 1, 2, or 3 and/or containing N-alpha-methyl at positions 1, 2, or 4, were synthesized by SPPS. These agonists were teste
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd76fb6bee57f6006423c3a30f43a3e2
https://pubmed.ncbi.nlm.nih.gov/1433199
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