Analysis of the Mechanism by Which the Small-Molecule CCR5 Antagonists SCH-351125 and SCH-350581 Inhibit Human Immunodeficiency Virus Type 1 Entry
暂无分享,去创建一个
Thomas P. Sakmar | Christoph Seibert | A. Trkola | John P. Moore | T. Ketas | J. Clader | T. Sakmar | S. Gavrilov | Christoph Seibert | Alexandra Trkola | Tatjana Dragic | T. Dragic | Francis Kajumo | John W. Clader | J. Tagat | F. Kajumo | Svetlana Gavrilov | Fotini Tsamis | Jayaram R. Tagat | Stuart McCombie | Bahige Baroudy | Shawn Kuhmann | Tom Ketas | Anadan Palani | S. Kuhmann | B. Baroudy | S. McCombie | Fotini Tsamis | A. Palani
[1] William C. Olson,et al. Differential Inhibition of Human Immunodeficiency Virus Type 1 Fusion, gp120 Binding, and CC-Chemokine Activity by Monoclonal Antibodies to CCR5 , 1999, Journal of Virology.
[2] M. Parmentier,et al. Synthetic full‐length and truncated RANTES inhibit HIV‐1 infection of primary macrophages , 1998, AIDS (London).
[3] C. Mackay,et al. Reduced HIV-1 infectability of CD4+ lymphocytes from exposed-uninfected individuals: association with low expression of CCR5 and high production of beta-chemokines. , 1998, Virology.
[4] M. Hammer,et al. Global survey of genetic variation in CCR5, RANTES, and MIP-1α: Impact on the epidemiology of the HIV-1 pandemic , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[5] S. Arya,et al. Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIV-suppressive factors produced by CD8+ T cells. , 1995, Science.
[6] Marc Parmentier,et al. Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene , 1996, Nature.
[7] John P. Moore,et al. Will Multiple Coreceptors Need To Be Targeted by Inhibitors of Human Immunodeficiency Virus Type 1 Entry? , 1999, Journal of Virology.
[8] W. Greenlee,et al. Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection. , 2001, Journal of medicinal chemistry.
[9] R. Doms. Chemokine receptors and HIV entry. , 2001, AIDS.
[10] E. Clercq,et al. Inhibition of T-tropic HIV Strains by Selective Antagonization of the Chemokine Receptor CXCR4 , 1997, The Journal of experimental medicine.
[11] B. Dewald,et al. N-terminal Peptides of Stromal Cell-derived Factor-1 with CXC Chemokine Receptor 4 Agonist and Antagonist Activities* , 1998, Journal of Biological Chemistry.
[12] J. Farber,et al. Chemokine receptors as HIV-1 coreceptors: roles in viral entry, tropism, and disease. , 1999, Annual review of immunology.
[13] O. Nishimura,et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[14] John P. Moore,et al. Alanine Substitutions of Polar and Nonpolar Residues in the Amino-Terminal Domain of CCR5 Differently Impair Entry of Macrophage- and Dualtropic Isolates of Human Immunodeficiency Virus Type 1 , 1998, Journal of Virology.
[15] Serena Xu,et al. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[16] Edward J. Fuchs,et al. Pharmacokinetics and Safety of AMD-3100, a Novel Antagonist of the CXCR-4 Chemokine Receptor, in Human Volunteers , 2000, Antimicrobial Agents and Chemotherapy.
[17] S. O’Brien,et al. The effect of genetic variation in chemokines and their receptorson HIV transmission and progression to AIDS , 2000, Immunological reviews.
[18] Douglas D. Richman,et al. HIV chemotherapy : AIDS , 2001 .
[19] S. Arya,et al. Identification of RANTES, MIP-1α, and MIP-1β as the Major HIV-Suppressive Factors Produced by CD8+ T Cells , 1995, Science.
[20] A. Trkola,et al. HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use , 2002, Proceedings of the National Academy of Sciences of the United States of America.
[21] J J Goedert,et al. Genetic Restriction of HIV-1 Infection and Progression to AIDS by a Deletion Allele of the CKR5 Structural Gene , 1996, Science.
[22] T. Schwartz,et al. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. , 1997, Science.
[23] H. Guy,et al. Epitope Mapping of CCR5 Reveals Multiple Conformational States and Distinct but Overlapping Structures Involved in Chemokine and Coreceptor Function* , 1999, The Journal of Biological Chemistry.
[24] S. Mccombie,et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element. , 2001, Bioorganic & medicinal chemistry letters.
[25] S. O. Smith,et al. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. , 2000, Proceedings of the National Academy of Sciences of the United States of America.
[26] J. Moore,et al. AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor , 1998, Nature Medicine.
[27] Timothy N. C. Wells,et al. New therapeutics that modulate chemokine networks , 2002, Nature Reviews Drug Discovery.
[28] T. Dragic. An overview of the determinants of CCR5 and CXCR4 co-receptor function. , 2001, The Journal of general virology.
[29] Douglas D. Richman,et al. HIV chemotherapy , 2001, Nature.
[30] D. Kwon,et al. The amino terminus of human CCR5 is required for its function as a receptor for diverse human and simian immunodeficiency virus envelope glycoproteins. , 1998, Virology.
[31] William C. Olson,et al. Amino-Terminal Substitutions in the CCR5 Coreceptor Impair gp120 Binding and Human Immunodeficiency Virus Type 1 Entry , 1998, Journal of Virology.
[32] Nancy Sullivan,et al. CCR5 Levels and Expression Pattern Correlate with Infectability by Macrophage-tropic HIV-1, In Vitro , 1997, The Journal of experimental medicine.
[33] W. Greenlee,et al. Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity. , 2002, Journal of medicinal chemistry.
[34] William C. Olson,et al. Mapping the Determinants of the CCR5 Amino-Terminal Sulfopeptide Interaction with Soluble Human Immunodeficiency Virus Type 1 gp120-CD4 Complexes , 2001, Journal of Virology.
[35] K. Palczewski,et al. Crystal Structure of Rhodopsin: A G‐Protein‐Coupled Receptor , 2002, Chembiochem : a European journal of chemical biology.
[36] B. Walker,et al. Enhanced Inhibition of Human Immunodeficiency Virus Type 1 by Met-Stromal-Derived Factor 1β Correlates with Down-Modulation of CXCR4 , 1999, Journal of Virology.
[37] E. De Clercq. New developments in anti-HIV chemotherapy , 2001, Current medicinal chemistry.
[38] M. Wainberg,et al. Effect of HIV constructs containing protease‐reverse transcriptase fusion proteins on viral replication , 1998, AIDS.
[39] Yong Guo,et al. CCR5-Mediated Human Immunodeficiency Virus Entry Depends on an Amino-Terminal gp120-Binding Site and on the Conformational Integrity of All Four Extracellular Domains , 1999, Journal of Virology.
[40] C. Mackay,et al. Interaction of Chemokine Receptor CCR5 with its Ligands: Multiple Domains for HIV-1 gp120 Binding and a Single Domain for Chemokine Binding , 1997, The Journal of experimental medicine.
[41] E. Fernandez,et al. Crystal structure of chemically synthesized [N33A] stromal cell-derived factor 1α, a potent ligand for the HIV-1 “fusin” coreceptor , 1998 .
[42] E. Santagostino,et al. Synthetic full-length and truncated RANTES inhibit HIV-1 infection of primary macrophages. , 1998 .
[43] B. Neustadt,et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist. , 2001, Journal of medicinal chemistry.
[44] A. Trkola,et al. Genetic Subtype-Independent Inhibition of Human Immunodeficiency Virus Type 1 Replication by CC and CXC Chemokines , 1998, Journal of Virology.
[45] Richard A Koup,et al. Homozygous Defect in HIV-1 Coreceptor Accounts for Resistance of Some Multiply-Exposed Individuals to HIV-1 Infection , 1996, Cell.
[46] John P. Moore,et al. New targets for inhibitors of HIV-1 replication , 2000, Nature Reviews Molecular Cell Biology.