|DALE J. KEMPF
SCIENTIFIC AWARDS AND ACTIVITIES
1978-1982 University of Illinois Graduate Fellowship
1982 Fuson Graduate Award, Division of Organic Chemistry, University of Illinois
1982 National Institutes of Health Postdoctoral Research Grant
1992 Chairman's Award, Abbott Laboratories
1994 Chairman's Award, Abbott Laboratories
1994 Co-Chair, 1994 Bioorganic Chemistry Gordon Research Conference, Plymouth State College, Plymouth, NH, June 27 - July 1, 1994
1994 Associate Editor, Protein and Peptide Letters
1995 Outstanding Researcher Award, Abbott Laboratories
1996 Chairman's Award, Abbott Laboratories
1996 Co-organizer, Symposium on New Antiviral Clinical Agents, 211th American Chemical Society Meeting, New Orleans, LA, March 28, 1996
1996 Member of Scientific Advisory Committee, II International Consensus Symposium on Combined Antiviral Therapy and Implications for Future Therapies, Barcelona, Spain, Sept. 8 - 11, 1996
1997 National Inventor of the Year, Intellectual Property Owners Association
1997 Inventor of the Year, Intellectual Property Law Association of Chicago
1999 Pharmaceutical Research and Manufacturers of America Discoverers Award
1999 Vice-chair, Chemotherapy of AIDS Gordon Research Conference, Ventura, CA, March 14-19, 1999
1999 Scientific Committee, 3rd International Workshop on HIV Drug Resistance & Treatment Strategies, San Diego, June 23-26, 1999
2000 Outstanding Research Team, Abbott Laboratories
2000 Scientific Committee, 4th International Workshop on HIV Drug Resistance & Treatment Strategies, Sitges, Spain, June 12-16, 1999
2000 Abbott Laboratories Pharmaceutical Products Division Growing Together Team Award
2000 Chairman's Award, Abbott Laboratories
88 Scientific Publications
52 U.S. Patents
J. Erickson, et al. Science, 1990, 249, 527; Design, Activity and 2.8 Ĺ Crystal Structure of a C2 Symmetric Inhibitor Complexed to HIV-1 Protease.
D. J. Kempf, et al. J. Med. Chem. 1990, 33, 2687; Structure-Based, C2 Symmetric Inhibitors of HIV Protease.
D. J. Kempf, et al. Antimicrobial Agents and Chemotherapy, 1991, 35, 2209-2214; Antiviral and Pharmacokinetic Properties of C2 Symmetric Inhibitors of HIV-1 Protease.
D. J. Kempf, et al. J. Med. Chem. 1993, 36, 320-330; Symmetry-Based Inhibitors of HIV Protease. Structure-Activity Studies of Acylated 2,4-Diamino-1,5-diphenyl-3-hydroxypentane and 2,5-Diamino-1,6-diphenylhexan-3,4-diol.
A. H. Kaplan, et al. J. Virology, 1993, 67, 4050-4055; Partial Inhibition of the Human Immunodeficiency Virus Type 1 Protease Results in Aberrant Virus Assembly and the Formation of Noninfectious Particles.
M. V. Hosur, et al. J. Am. Chem. Soc., 1994, 116, 847-855; Influence of Stereochemistry on Activity and Binding Modes for C2 Symmetry-Based Inhibitors of HIV-1 Protease.
A. Kaplan, et al. Proc. Natl. Acad. Sci., 1994, 91, 5597-5601; Selection of HIV-1 Variants Which Encode Viral Proteases with Decreased Sensitivity to an Inhibitor of the Viral Protease. [Full-Text PDF]
D. D. Ho, et al. J. Virology, 1994, 68, 2016-2020; Characterization of HIV-1 Variants with Increased Resistance to a C2-Symmetric Protease Inhibitor.
S. Kageyama, et al. AIDS Res. Human Retroviruses, 1994, 10, 735-743; A C2 Symmetry-Based HIV Protease Inhibitor, A77003, Irreversibly Inhibits Infectivity of HIV-1 In Vitro.
D. J. Kempf, et al. Bioorg. Med. Chem., 1994, 847-858; Design of Orally Bioavailable, Symmetry-Based Inhibitors of HIV Protease.
A. H. Kaplan, et al. Antimicrobial Agents and Chemotherapy, 1994, 38, 2929-2933; HIV-1 Virions Composed of Unprocessed Gag and Gag-Pol Precursors are Capable of Efficiently Reverse Transcribing the Viral Genomic RNA.
M. Markowitz, et al. J. Virology, 1995, 69, 701-706; Selection and Analysis of Human Immunodeficiency Virus Type 1 Variants with Increased Resistance to ABT-538, a Novel Protease Inhibitor. [Full-Text PDF]
D. Kempf, et al. Proc. Natl. Acad. Sci., 1995, 92, 2484-2488; Abt-538 is a Potent Inhibitor of Human Immunodeficiency Virus Protease With High Oral Bioavailability in Humans . [Full-Text PDF]
J. A. Bilello, et al. Antimicrob. Agents Chemother. 1996, 40, 1491-1497, Human Serum a1-Acid Glycoprotein Reduces the Uptake, Intracellular Concentration and Antiviral Activity of A-80987, an Inhibitor of the Human Immunodeficiency Virus Type I (HIV-1) Protease. [Full-Text PDF]
A. Molla, et al. Nature Medicine, 1996, 2, 760-766, Ordered Accumulation of Mutations in HIV Protease Confers Resistance to Ritonavir.
D. J. Kempf, et al. Antimicrob. Agents Chemother., 1997, 41, 654-660, Pharmacokinetic Enhancement of Inhibitors of the Human Immunodeficiency Virus Protease by Coadministration with Ritonavir. [Full-Text PDF]
D. Kempf, et al. J. Med. Chem., 1998, 41, 602-617; Discovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy.
D. J. Kempf, et al. AIDS, 1998, 12, F9-F14; The Duration of Viral Suppression During Protease Inhibitor Therapy for HIV-1 Infection is Predicted by Plasma HIV-1 RNA at the Nadir .
H. L. Sham, et al. Antimicrob. Agents Chemother., 1998, 42, 3218-3224, ABT-378, a potent second generation inhibitor of the human immunodeficiency virus protease [Full-Text]
A. Molla, et al. Virology, 1998, 250, 255-262, Human Serum Attenuates the Activity of Protease Inhibitors Toward Wild Type and Mutant Human Immunodeficiency Virus.
A. Carrillo, et al. J. Virology, 1998, 72, 7532-7541, In Vitro Selection and Characterization of HIV-1 Variants with Increased Resistance to ABT-378, a Novel Protease Inhibitor. [Full-Text]
D. W. Cameron, et al. AIDS, 1998, 13, 213-224, Ritonavir and Saquinavir Combination Therapy for the Treatment of HIV Infection.
D. J. Kempf, et al. J. Virology, 2001, 75, 7462-7469, Identification of Genotypic Changes in HIV Protease that Correlate with Reduced Susceptibility to the Protease Inhibitor Lopinavir Among Viral Isolates from Protease Inhibitor Experienced Patients. [Full-Text]
C. A. Benson, et al. J. Infect. Diseases, 2002, 185, 599-607, Safety and Antiviral Activity at 48 Weeks of Lopinavir/Ritonavir plus Nevirapine and 2 Nucleoside Reverse-Transcriptase Inhibitors in Human Immunodeficiency Virus Type I-Protease Inhibitor-Experienced Patients.
W. Kati, et al. Antimicrob. Agents Chemother., 2002, 46, 1014-1021, In vitro Characterization of A-315675: a Highly Potent Inhibitor of A and B Strain Influenza Virus Neuraminidases and Influenza Virus Replication.
D. J. Kempf, J. D. Isaacson, M. S. King, S. C. Brun, J. Sylte, B. Richards, B. Bernstein, R. Rode, E. Sun, Antiviral Therapy, 2002, 7, 165-174, Analysis of the Virologic Response With Respect to Baseline Viral Phenotype and Genotype in Protease Inhibitor-Experienced HIV-1-Infected Patients Receiving Lopinavir/Ritonavir Therapy.
Hsu, J. Isaacson, S. Brun, B. Bernstein, W. Lam, R. Bertz, C. Foit, K. Rynkiewicz, B. Richards, M. King, D. J. Kempf, G. R. Granneman, E. Sun, Antimicrob. Agents Chemother., 2003, 47, 350-359 Pharmacokinetic/ Pharmacodynamic Analysis of Lopinavir/ritonavir in Combination with Efavirenz and Two Nucleoside Reverse Transcriptase Inhibitors in Extensively Pretreated HIV-Infected Patients.
N. Shulman, A. Zolopa, D. Havlir, A. Hsu, C. Renz, S. Boller, P. Jiang, R. Rode, J. Gallant, E. Race, D. Kempf, E. Sun, Antimicrob. Agents Chemother. 2002, 46, 3907-3916, Virtual Inhibitory Quotient Predicts Response to Ritonavir Boosting of Indinavir-Based Therapy in Human Immunodeficiency Virus-Infected Patients with Ongoing Viremia.
INVITED REVIEW ARTICLES
D. W. Norbeck, D. J. Kempf; Ann. Rep. Med. Chem., 1991, 26, 141-150, HIV Protease Inhibitors.
D. Kempf; PAACNOTES, 1993, 5, 143-145; HIV Protease as a Therapeutic Target.
D. J. Kempf; in Meth. Enzymology; 1994, 241, 334-354; Design of Symmetry-Based, Peptidomimetic Inhibitors of HIV Protease.
D. J. Kempf, Perspect. Drug Discovery Design, 1995, 2, 427-436; Progress in the Discovery of Orally Bioavailable Inhibitors of HIV Protease.
D. J. Kempf, H. L. Sham, Curr. Pharm. Design, 1996, 2, 225-246; HIV Protease Inhibitors.
A. Molla, et al., Antiviral Research, 1998, 39, 1-23; Recent Developments in HIV Protease Inhibitor Therapy.
D. Kempf, A. Hsu, The AIDS Reader, 1998, 8 (Supplement B), 4-7; Pharmacology of Dual Protease Inhibitor Therapy: Ritonavir/Saquinavir and Ritonavir/Indinavir.
D. J. Kempf, in Protease Inhibitors in AIDS Therapy, R. C. Ogden, C. W. Flexner, Eds. New York: Marcel Dekker, 2000, p. 49-64, Discovery and Early Development of Ritonavir and ABT-378.
D. J. Kempf, A. Hsu, A. Molla, in Antiretroviral Therapy, E. DeClerq, ed., Washington, D.C.: ASM Press, 2001, p. 147-173, Protease Inhibitors as Anti-Hyman Immunodeficiency Virus Agents.
SELECTED INVITED LECTURES
Plenary Session, National Institute of Allergy and Infectious Diseases/AIDS Clinical Trials Groups Meeting, Bethesda, Maryland, July 13, 1990; Inhibitors of HIV Protease.
Gordon Research Conference on Medicinal Chemistry, New London, New Hampshire, August 6-10, 1990; Novel Inhibitors of HIV-1 Protease.
Symposium on the Design of Anti-Viral Agents, 32nd Annual Medicinal Chemistry Symposium, State University of New York at Buffalo, June 3-5, 1991; Structure-Based, Symmetric Inhibitors of HIV Protease
Workshop on Structure-Based Drug Design, Fourth Conference of the NIH National Cooperative Drug Discovery Groups for the Treatment of HIV Infection, San Diego, CA, Nov. 3-7, 1991; Rational Design of Inhibitors of the Human Immunodeficiency Virus Type 1 Protease.
Symposium: HIV-Infektion, Chemotherapeutische Entwicklungen, Frankfurt am Main, February 28, 1992, Inhibition of HIV Protease as a Therapeutic Approach.
Plenary speaker, First Gordon Research Conference on Bioorganic Chemistry, New London, New Hampshire, June 23-27, 1992, Symmetry-Based Inhibitors of HIV Protease.
Plenary Session, 1st Royal Society of Chemistry International Symposium: Recent Advances in the Chemistry of Anti-Infective Agents, Churchill College, Cambridge, England, July 5-8, 1992, Structure-Based, Symmetric Inhibitors of HIV Protease.
Seventh Annual Colloquium on Human Diseases: Molecular Medicine of AIDS and Prospects of Control, State University of New York at Stony Brook, October 5, 1992; Design of Inhibitors of HIV Protease.
Gordon Research Conference on the Chemotherapy of AIDS, Oxnard, CA, March 21-26, 1993; Inhibitors of HIV Protease.
Coordinated Therapies for HIV Infection, Fifth Conference of the NIH National Cooperative Drug Discovery Groups for the Treatment of HIV Infection (NCDDG-HIV), Washington, D.C., July 12, 1993, In Vitro Resistance Development to Symmetry-Based HIV Protease Inhibitors A-77003 and A-80987.
Symposium on Pharmaceutical Chemistry, 206th American Chemical Society Meeting, Chicago, IL, Aug. 22-26, 1993; Design and Development of Symmetry-Based Inhibitors of HIV Protease
Gordon Research Conference on the Chemistry and Biology of Peptides, Ventura, CA, Feb. 14-18, 1994; Peptidomimetic Inhibitors of HIV Protease: Design and Delivery
Keystone Symposia Conference on Structural and Molecular Biology of Protease Function and Inhibition, Santa Fe, NM, March 5-12, 1994; Symmetry-Based Inhibitors of HIV Protease: Oral Bioavailability and Resistance Emergence.
First Winter Conference on Medicinal and Bioorganic Chemistry, Steamboat Springs, CO, January 29-February 2, 1995; Peptidomimetics in Drug Design: Orally Bioavailable Inhibitors of HIV Protease.
Symposium on Anti-Infective Agents, 1995 International Chemical Congress of Pacific Basin Societies, Honolulu, Hawaii, Dec. 17-22, 1995; Chemotherapy of AIDS with ABT-538, a Symmetry-Based Inhibitor of HIV Protease with High Oral Bioavailability.
Symposium on New Antiviral Clinical Agents, 211th American Chemical Society Meeting, New Orleans, LA, March 24-28, 1996; Therapy of HIV Infection with Ritonavir, a Symmetry-Based HIV Protease Inhibitor
Keystone Symposia Conference on Immunopathogenesis of HIV Infection, Hilton Head, SC, March 26-April 1, 1996; Antiviral Therapy with Ritonavir: Resistance and Pharmacokinetic Issues
Symposium on Inhibitors of HIV-1 Protease: A New Force in HIV-1 Therapeutics, Cornell University Medical College and Rockefeller University Hospital, April 28, 1996; In Vivo Resistance to Protease Inhibitors
Gordon Research Conference on Medicinal Chemistry, New London, New Hampshire, August 4-8, 1996; HIV Protease.Inhibitors: An Overview
Twenty Third Winter Course on Infectious Diseases, Snowmass Village, Colorado, February 25, 1997, In Vivo Resistance to Protease Inhibitors
23rd AIDS Clinical Trials Groups Meeting, Washington, D.C., July 19-22, 1997, The Durability of Response to Protease Inhibitor Therapy is Predicted by Viral Load at the Nadir
Sixth European Conference on Clinical Aspects and Treatment of HIV-Infection, Hamburg, Germany, October 11-15, 1997, Satellite Symposium: Optimising the Use of Protease Inhibitors, Understanding Protease Inhibitor Drug Resistance
Symposium on Peptides and Peptide Mimetics, Fifth Chemical Congress of North America, Cancun, Mexico, November 11-15, 1997, Peptide Mimetics as Dual Inhibitors of HIV Protease and Cytochrome P450
12th World AIDS Conference, Geneva, Switzerland, June 28-July 3, 1998, Satellite Symposium: Evolving Strategies in Protease Inhibitor Therapy, Pharmacology of Dual Protease Inhibitor Therapy: Ritonavir/Saquinavir and Ritonavir/Indinavir
40th Annual Buffalo Medicinal Chemistry Symposium, University at Buffalo, Buffalo, NY, May 16-19, 1999, Understanding Clinical Resistance to HIV Protease Inhibitors
Case Study, Residential School on Medicinal Chemistry, Drew University, June 14, 1996; Toward Second Generation HIV Protease Inhibitors: What Does it Take?
2nd International Conference on Protease Inhibitors, Gainesville, Florida, December 3-6, 1999; The Development of ABT-378 as a Second-Generation HIV Protease Inhibitor.
Fifth International Congress on Drug Therapy in HIV Infection, Glasgow, UK, October 22-26, 2000; HIV resistance: Prevention and management.
First HIV Drug Resistance Program Symposium: Understanding Antiviral Drug Resistance, Chantilly, Virginia, December 3-6, 2000; Pharmacologic Barriers to HIV Resistance Development: The Kaletra™ Case Study.