Small molecule antagonists of chemokine receptors as emerging anti-HIV agents

Expert Opinion on Therapeutic Patents

Volumn 11, Issue 8, 2001, Pages 1245-1252

  Mastrolorenzo, A ^a   Scozzafava, A ^a   Supuran, C T ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

Author keywords

Antiviral agent; Bicyclam; Chemokine receptor (CCR5, CXCR4); HIV entry

Indexed keywords

1,1' [1,4 PHENYLENEBIS(METHYLENE)]BIS(1,4,8,11 TETRAAZACYCLOTETRADECANE); AMD 3465; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CXCR4; N [4 [[[6,7 DIHYDRO 2 (4 METHYLPHENYL) 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL] N,N DIMETHYL 2H TETRAHYDROPYRAN 4 AMINIUM CHLORIDE; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; PROTEINASE INHIBITOR; RANTES; RNA DIRECTED DNA POLYMERASE INHIBITOR; SULFONAMIDE; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG POTENTIATION; DRUG STRUCTURE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; PATENT; REVIEW; STRUCTURE ACTIVITY RELATION;

EID: 0034899714     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.11.8.1245     Document Type: Review

References (32)

1. Mechanisms for HIV-1 entry: Current strategies to interfere with this step
2. Mechanisms of viral membrane fusion and its inhibition
3. HIV-1 entry - An expanding portal for drug discovery
4. Inhibitors of HIV cellular fusion
5. Current evidence and future directions for targeting HIV-1 entry
6. Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody
7. Human immunodeficiency virus type-1 and chemokines: Beyond competition for common cellular receptors
8. Design of an HIV-1 entry inhibitor
9. From receptor recognition mechanisms to bioinspired mimetic antagonists in HIV-1/cell docking
10. N- and C-domains of HIV-1 gp41: Mutation, structure and functions
11. HIV type 1 entry inhibitors PRO542 and T-20 are potently synergistic in blocking virus-cell and cell-cell fusion
12. Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV-1 agents with very high selectivity indexes
13. Antagonists of the human CCR5 receptor as anti-HIV-1. Part 1: Discovery and initial structure - Activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes
14. Antagonists of the human CCR5 receptor as anti-HIV-1. Part 2: Structure - Activity relationships for substituted 2-aryl-1-[N-(methyl)-N-phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes
15. Convenient efficient synthesis of TAK-779, a nonpeptide CCR5 antagonist: Development of preparation of various ammonium salts using trialkylphosphite and N-halogeno-succinimide
16. The CXCR4 antagonist AMD3100 effeciently inhibits cell-surface-expressed HIV type 1 envelope-induced apoptosis
17. Molecular targets for antiviral agents
18. Cyanovirin-N, a potent HIV-inactivating protein, blocks both CD4-dependent and CD4-independent binding of soluble gp120 to target cells, inhibits sCD4-induced binding of sgp120 to cell-associated CXCR4, from target cells
19. Pharmacokinetics and safety of AMD3100, a novel antagonist of the CXCR4 chemokine receptor in human volunteers
20. Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists
21. Safe use of the CXCR4 inhibitor ALX40-4c in humans
22. Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: Synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety
23. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5
24. Carbonic anhydrase inhibitors: Synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus the cytosolic isozymes
25. Carbonic anhydrase inhibitors: Synthesis of sulfonamides incorporating 2,4,6-trisubstituted-pyridinium-ethylcarboxamido moieties possessing membrane-impermeability and in vivo selectivity for the membrane-bound cytosolic (CA I and CA II) isozymes
26. The chemokine/chemokine receptor family: Potential progress for therapeutic intervention
27. Protease inhibitors in the treatment of AIDS
28. HIV chemotherapy
29. Gulliver's travels in HIV land
30. Challenges and opportunities for development of an AIDS vaccine
31. Agents that target cysteine residues of biomolecules and their therapeutic potential