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Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket. 2010
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
Pharmaceutical Discovery Division, Abbott Laboratories, 100 Abbott Park Rd., R46Y, AP10, Abbott Park, IL 60064-6098, United States. kent.d.stewart@abbott.com
The ectodomain of HIV-1 gp41 mediates the fusion of viral and host cellular membranes. The peptide-based drug Enfuvirtide(1) is precedent that antagonists of this fusion activity may act as anti HIV-agents. Here, NMR screening was used to discover non-peptide leads against this target and resulted in the discovery of a new benzamide 1 series. This series is non-peptide, low molecular weight, and analogs have activity in a cell fusion assay with EC50 values ranging 3-41microM. Structural work on the gp41/benzamide 1 complex was determined by NMR spectroscopy using a designed model peptide system that mimics an open pocket of the fusogenic form of the protein.
Related Publications
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
October 1999,
Cell,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
March 2000,
Biochemical and biophysical research communications,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
March 2002,
Biochemistry,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
January 2013,
Viruses,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
February 2009,
The Journal of biological chemistry,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
November 2010,
ChemMedChem,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
December 1998,
Proceedings of the National Academy of Sciences of the United States of America,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
April 2002,
The Journal of biological chemistry,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
June 2015,
Journal of virology,
Kent D Stewart, and
Jeffrey R Huth, and
Teresa I Ng, and
Keith McDaniel, and
Rebecca Newlin Hutchinson, and
Vincent S Stoll, and
Renaldo R Mendoza, and
Edmund D Matayoshi, and
Robert Carrick, and
Hongmei Mo, and
Jean Severin, and
Karl Walter, and
Paul L Richardson, and
Leo W Barrett, and
Robert Meadows, and
Steve Anderson, and
William Kohlbrenner, and
Clarence Maring, and
Dale J Kempf, and
Akhter Molla, and
Edward T Olejniczak
January 2000,
Journal of biological regulators and homeostatic agents,
