Validation of chemokine receptors as drug targets

Current Opinion in Drug Discovery and Development

Volumn 3, Issue 5, 2000, Pages 610-623

  Luttichau, H R ^a   Schwartz, T W ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Chemokine receptor; Drug target; Ligand; Phenotype; T helper cell

Indexed keywords

1,1' [1,4 PHENYLENEBIS(METHYLENE)]BIS(1,4,8,11 TETRAAZACYCLOTETRADECANE); 2,2' [4,4' [(AMINOCARBONYL)AMINO]BIS[N 4' DI(PYRROLE 2 CARBOXAMIDE 1,1' DIMETHYL)] 6,8 NAPHTHALENEDISULFONIC ACID]HEXASODIUM; 4 HYDROXYPIPERIDINE DERIVATIVE; ACYCLIC I; ALX 404C; BX 471; CGP 6422; CGP 64222; CHEMOKINE; CHEMOKINE RECEPTOR; G PROTEIN COUPLED RECEPTOR; MACROPHAGE INFLAMMATORY PROTEIN 1ALPHA; PEPTIDE; RS 136270; RS 504393; RS 511336 000; SB 225002; SB 328437; T 22; TAK 779; UCB 35625; UNCLASSIFIED DRUG;

ADVERSE DRUG REACTION; CLINICAL TRIAL; DRUG TARGETING; GENE; HELPER CELL; HUMAN; INFLAMMATION; NONHUMAN; PHENOTYPE; REVIEW;

EID: 0033770435     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (131)

1. Chemokines
2. Recent advances in chemokines and chemokine receptors
3. International union of pharmacology. XXII. Nomenclature for chemokine receptors
4. Chemokines and leukocyte traffic
5. The concept of type-1 and type-2 helper T-cells and their cytokines in humans
6. Selective expression of the eotaxin receptor CCR3 by human T-helper 2 cells
7. Flexible programs of chemokine receptor expression on human polarized T-helper 1 and 2 lymphocytes
8. Differential expression of chemokine receptors and chemotactic responsiveness of type 1 T-helper cells (TH1s) and Th2s
9. The chemokine receptor CCR8 is preferentially expressed in Th2 but not Th1 cells
10. Selective up-regulation of chemokine receptors CCR4 and CCR8 upon activation of polarized human type 2 Th cells
11. The role of CCR7 in Th1 and Th2 cell localization and delivery of B-cell help in vivo
12. CCR7 coordinates the primary immune response by establishing functional microenvironments in secondary lymphoid organs
13. Mice lacking expression of secondary lymphoid organ chemokine have defects in lymphocyte homing and dendritic cell localization
14. Secondary lymphoid tissue chemokine mediates T-cell-dependent antitumor responses in vivo
15. Defects of B-cell lymphopeiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1
16. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development
17. The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract
18. Marked increase in anti-HIV activity, as well as inhibitory activity against HIV entry mediated by CXCR4, linked to enhancement of the binding ability of tachyplesin analogs to CXCR4
19. A second target for the peptoid tat/trensactivation response element inhibitor CGP64222: Inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry
20. A small-molecule inhibitor directed against the chamokine receptor CXCR4 prevents its use as an HIV-1 coreceptor
21. Small molecule inhibitor of HIV-1 cell fusion blocks chemokine receptor-mediated function
22. A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus
23. A highly selective CC chemokine receptor (CCR)8 antagonist encoded by the poxvirus molluscum contagiosum
24. Fusion-competent vaccines: Broad neutraiization of primary isolates of HIV
25. Inactivation of HIV-1 chemokine co-receptor CXCR-4 by a novel intrakine strategy
26. AMD-3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor
27. Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers
28. Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists
29. A putative chemokine receptor, BLR1, directs B-cell migration to defined lymphoid organs and specific anatomic compartments of the spleen
30. Lack of chemokine receptor CCR1 enhances Th1 responses and glomerular injury during nephrotoxic nephritis
31. Targeted disruption of the β-chemokine receptor CCR1 protects against pancreatitis-associated lung injury
32. Targeting of the chemokine receptor CCR1 suppresses development of acute and chronic cardiac allograft rejection
33. Impaired host defense, hematopoiesis, granulomatous inflammation and type 1-type 2 cytokine balance in mice lacking CC chemokine receptor 1
34. Dominant myelopoietic effector functions medlated by chemokine receptor CCR1
35. Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor
36. Discovery of novel non-peptide CCR1 receptor antagonists
37. Identification and characterization of a potent, selective and orally active antagonist of the CC chemokine receptor-1
38. Requirement of MIP-1α for an inflammatory response to viral infection
39. Early murine cytomegalovirus (MCMW) infection induces liver natural killer (NK) cell inflammation and protection through Macrophage inflammatory protein 1α (MIP-1α)-dependent pathways
40. An important role for the chemokine macrophage inflammatory protain-1 α in the pathogenesis of the T-cell-mediated autoimmune disease, experimental autoimmune encephalomyelitis
41. CD8+ T-cells are a biologically relevant source of macrophage inflammatory protein-1 α in vivo
42. A randomized phase-II study of BB-10010 (macrophage inflammatory protein-1α) in patients with advanced breast cancer receiving 5-fluorouracil, adriamycin, and cyclophospharoide chemotherapy
43. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist
44. The chemokine receptor antagonist AOPRANTES reduces monocyte infiltration in experimental glomerulonephritits
45. The coordinated action of CC chemokines in the lung orchestrates allergic inflammation and airway hyperresponsiveness
46. Met-RANTES reduces vascular and tubular damage during acute renal transplant rejection: Blocking monocyte arrest and recruitment
47. Effect of a CC chemokine receptor antagonist on collagen induced arthritis in DBA/1 mice
48. Polyclonal antibody directed against human RANTES ameliorates disease in the Lewis rat adjuvant-induced arthritis model
49. Differential expression and cross-regulatory function of RANTES during mycobacterial (type 1) and schistosomal (type 2) antigen-elicited grenuloroatous inflammation
50. Absence of CC chemokine receptor-2 reduces atherosclerosis in apolipoprotein E-deficient mice
51. MCP-1 deficiency reduces susceptibility to atherosclerosis in mice that overexpress human apolipoprotein B
52. Absence of monocyte chemoattractant protein-1 reduces atherosclerosis in low density lipoprotein receptor-deficient mice
53. Impaired monocyte migration and reduced type 1 (Th1) cytokine responses in C-C chemokine receptor 2 knockout mice
54. CCR2 expression determines T1 versus T2 polarization during pulmonary Cryptococcus neoformans infection
55. Effect of C-C chemokine receptor 2 (CCR2) knockout on type-2 (schistosomal antigen-elicited) pulmonary granuloma formation: Analysis of cellular recruitment and cytokine responses
56. Control of Th2 polarization by the chemokine monocyte chemoattractant protein-1
57. Exaggerated hepatic injury due to acetaminophen challenge in royce lacking C-C chemokine receptor 2
58. Monocyte chemoattractant protein-1 mediates cockroach allergen-induced bronchial hyperreactivity in normal but not CCR2-/- mice: The role of roast cells
59. Defects in macrophage recruitment and host defense in mice lacking the CCR2 chemokine receptor
60. Mice with selective deletion of the CC chemokine receptors 5 and 2 are protected from dextran sodium sulfate-medlated colitis: Lack of the CC chemokine receptor 5 expression results in a NK1.1+ lymphocyte-associated Th2-type immune response in the intestine
61. RANTES and monocyte chemoattractant protein-1 (MCP-1) play an important role in the inflammatory phase of crescentic nephrititis, but only MCP-1 is involved in crescent formation and interstitiel fibrosis
62. Acute and relapsing experimental autoimmune encephalomyelitis are regulated by differential expression of the CC chamokines macrophage inflammatory protein-1α and monocyte chemotactic protein-1
63. Clark-Lewis h An antagonist of monocyte chemoattractant protein 1 (MCP-1) inhibits arthritis in the MRL-Ipr mouse model
64. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: Binding to a common chemokine receptor motif within the helical bundle
65. Depletion of eosinophils in mice through the use of antibodies specific for C-C chemokine receptor 3 (CCR3)
66. C-C chemokine receptor 3 antagonism by the β-chemokine macrophage inflammatory protein 4, a property strongly enhanced by an amino-terminal alanine-methionine swap
67. A small molecule antagonist of the chemokine receptors CCR1 and CCR3: Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry
68. Identification of a potent, selective non-pepfide CCR3 antagonist that inhibits eotaxin-2 and MCP-4 induced eosinophil migration
69. Targeted disruption of the chemokine eotaxin partially reduces antigen-induced tissue eosinophilla
70. Antigen-induced eosinophilic lung inflammation develops in mice deficient in chemokine eotaxin
71. Chamokine-induced eosinophil recruitment. Evidence of a role for endogenous eotaxin in an in vivo allergy model in mouse skin
72. A key rote for CC chemokine receptor 4 in lipopolysaccharide-induced endotoxic shock
73. Pivotal role of TARC, a CC chemokine, in bacteria-induced fulminant hepatic failure in mice
74. Mouse monocyte-derived chemokine is involved in airway hyperreactivity and lung inflammation
75. Genetic restriction of HIV-1 infection and progression to AIDS by a deletion allele of the CKR5 structural gene
76. The role of a mutant CCR5 allele in HIV-1 transmission and disease progression
77. CC chemokine receptor 5 polymorphism in rheumatoid arthritis
78. Association of rheumatoid arthritis with a functional chemokine receptor, CCR5
79. CC-chemokine receptor 5 polymorphism and age of onset In familial multiple sclerosis. Multiple Sclerosis Genetics Group
80. Impaired macrophage function and enhanced T-cell-dependent immune response in mice lacking CCR5, the mouse homologue of the major HIV-1 coreceptor
81. Cutting edge: Role of C-C chemokine receptor 5 in organ-specific and innate immunity to Cryptococcus neoformans
82. Induction of experimental autoimmune encephalomyelitis in C57BL/6 mice deficient in either the chemokine macrophage inflammatory protein-1α or its CCR5 receptor
83. A small-molecule, non-peptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
84. CCR6 mediates dendritic cell localization, lymphocyte homeostasis, and immune responses in mucosal tissue
85. Macrophage inflammatory protein 3α is involved in the constitutive trafficking of epidermal Langerhans cells
86. Up-regulation of macrophage inflammatory protein-3α/CCL20 and CC chemokine receptor 6 in psoriasis
87. The CC chemokine I-309 inhibits CCR8-dependent infection by diverse HIV-1 strains
88. Human NK cells express CC chemokine receptors 4 and 8 and respond to thymus and activation-regulated chemokine, macrophage-derived chemokine, and I-309
89. Lack of host cellular Immune response in eruptive molluscum contagiosum
90. Immunocompetent cells and epithelial cell modifications in molluscum contagiosum
91. Langerhans cells in molluscum contagiosum, verruca vulgaris, plantar wart, and condyloma acuminatum
92. Human G protein-coupled receptor GPR-9-6/CC chemokine receptor 9 is selectively expressed on intestinal homing T-lymphocytes, mucosal lymphocytes, and thymocytes and is required for thymus-expressed chemokine-mediated chemotaxis
93. CTACK, a skin-associated chemokine that preferentially attracts skin-homing memory T-cells
94. Identification of a novel chemokine (CCL28), which binds CCR10
95. Neutrophil and B-cell expansion In mice that lack the murine IL-8 receptor homomog
96. Involvement of interleukin (IL) 8 receptor in negative regulation of myeloid progenitor cells in vivo: Evidence from mice lacking the murine IL-8 receptor homologue
97. The murine homolog of the interluekin-8 receptor CXCR-2 is essential for the occurrence of neutrophilic inflammation in the air pouch model of acute urate crystal-Induced gouty synovitls
98. Transfection of interleukin-8 increases angiogenesis and tumorigenesis of human gastric carcinoma cells in nude mice
99. Inhibition of interleukin-8 reduces tumorigenesis of human non-small cell lung cancer in SCID mice
100. Prevention of lung reperfusion injury in rabbits by a monoclonal antibody against Interleukin-8
101. The delayed-type hypersensitivity reaction is dependent on IL-8. Inhibition of a tuberculin skin reaction by an anti-IL-8 monoclonal antibody
102. Fully human anti-interleukin-8 monoclonal antibodies: Potential therapeutics for the treatment of inflammatory disease states
103. Neutralization of IL-8 inhibits neutrophil influx in a rabbit model of endotoxin-induced pleurisy
104. Interleukin-8 antagonists generated by N-terminal modification
105. Chemokine antagonists that discriminate between interleukin-8 receptors. Selective blockers of CXCR2
106. Clark-Lewis h inhibition of murine neutrophil recruitment in vivo by CXC chemokine receptor antagonists
107. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration
108. The chemokine receptors CXCR3 and CCR5 mark subsets of T-cells associated with certain inflammatory reactions
109. Involvement of the IP-10 chemokine in sarcoid granulomatous reactions
110. + T-cells ere increased in multiple sclerosis and their ligands MIP-1α and IP-10 are expressed in demyelinating brain lesions
111. Identification of viral macrophage inflammatory protein (vMIP)-II as ligand for GPR5/XCR1
112. Analysis of fractalkine receptor CX(3)CR1 function by targeted deletion and green fluorescent protein reporter gene insertion
113. 3 motif
114. The mitotic machinery as a source of genetic instability in cancer
115. In vivo Inhibition of CC and CX3C chemokine-induced leukocyte infiltration and attenuation of glomerulonephritis in Wister-Kyoto (WKY) rats by vMIP-II
116. Prevention of crescentic glomerulonephritis by immunoneutralization of the fractalkine receptor CX3CR1 rapid communication
117. A receptor for the malarial parasite Plasmodium vivax: The erythrocyte chemokine receptor. Science
118. From malaria to chemokine receptor: The emerging physiologic role of the Duffy blood group antigen
119. Deletion of the routine Duffy gene (Dfy) reveals that the Duffy receptor is functionally redundant
120. Angiogenic and HIV-inhibitory functions of KSHV-encoded chemokines
121. Coreceptor ligand inhibition of fetal brain cell infection by HIV type 1
122. Chemokine antagonist infusion attenuates cellular infiltration following spinal cord injury in rat
123. Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation
124. G-protein-coupled receptor of Keposi's sarcoma-associated herpesvirus is a viral oncogene and angiogenesis activator
125. Agonist and inverse agonist for the herpesvirus 8-encoded constitutively active seven-transmembrane oncogene product, ORF-74
126. The human cytomegslovirus chemokine receptor US28 mediates vascular smooth muscle cell migration
127. Selective recognition of the membrane-bound CX3C chemokine, fractalkine, by the human cytomegalovirus-encoded broad-spectrum receptor US28
128. Transgenic expression of the chemokine receptor encoded by human harpesvirus 8 induces an angioproliferative disease resembling Kaposi's sarcoma
129. Selective elimination of constitutive activity or chemokine binding in the human herpesvirus 8 encoded oncogene ORF74