CCR5 receptor antagonist (English Wikipedia)

Lederman MM, Penn-Nicholson A, Cho M, Mosier D (August 2006). "Biology of CCR5 and its role in HIV infection and treatment". JAMA. 296 (7): 815–26. doi:10.1001/jama.296.7.815. PMID 16905787.
De Clercq E (December 2007). "The design of drugs for HIV and HCV". Nature Reviews Drug Discovery. 6 (12): 1001–18. doi:10.1038/nrd2424. PMID 18049474. S2CID 37859193.
Pulley, Shon (2007). "CCR5 antagonists: from discovery to clinical efficacy". In Neote, Kuldeep; Letts, Gordon L.; Moser, Bernhard (eds.). Chemokine Biology — Basic Research and Clinical Application. Progress in Inflammation Research. Vol. 2. Birkhauser Basel. pp. 145–163. doi:10.1007/978-3-7643-7437-2_11. ISBN 978-3-7643-7195-1.
Samson M, Libert F, Doranz BJ, et al. (August 1996). "Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene". Nature. 382 (6593): 722–5. Bibcode:1996Natur.382..722S. doi:10.1038/382722a0. PMID 8751444. S2CID 4370818.
Dragic T, Litwin V, Allaway GP, et al. (June 1996). "HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5". Nature. 381 (6584): 667–73. Bibcode:1996Natur.381..667D. doi:10.1038/381667a0. PMID 8649512. S2CID 4301976.
Flexner C (December 2007). "HIV drug development: the next 25 years". Nature Reviews Drug Discovery. 6 (12): 959–66. doi:10.1038/nrd2336. PMID 17932493. S2CID 31261997.
Ray N, Doms RW (2006). "HIV-1 Coreceptors and Their Inhibitors". Chemokines and Viral Infection. Current Topics in Microbiology and Immunology. Vol. 303. pp. 97–120. doi:10.1007/978-3-540-33397-5_5. ISBN 978-3-540-29207-4. PMID 16570858.
Westby M, van der Ryst E (2005). "CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection". Antiviral Chemistry & Chemotherapy. 16 (6): 339–54. doi:10.1177/095632020501600601. PMID 16329283. S2CID 24994759.
Briz V, Poveda E, Soriano V (April 2006). "HIV entry inhibitors: mechanisms of action and resistance pathways". The Journal of Antimicrobial Chemotherapy. 57 (4): 619–27. doi:10.1093/jac/dkl027. PMID 16464888.
Murga JD, Franti M, Pevear DC, Maddon PJ, Olson WC (October 2006). "Potent Antiviral Synergy between Monoclonal Antibody and Small-Molecule CCR5 Inhibitors of Human Immunodeficiency Virus Type 1". Antimicrobial Agents and Chemotherapy. 50 (10): 3289–96. doi:10.1128/AAC.00699-06. PMC 1610098. PMID 17005807.
Watson C, Jenkinson S, Kazmierski W, Kenakin T (April 2005). "The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor". Molecular Pharmacology. 67 (4): 1268–82. doi:10.1124/mol.104.008565. PMID 15644495. S2CID 2587200.
Fermini B, Fossa AA (June 2003). "The impact of drug-induced QT interval prolongation on drug discovery and development". Nature Reviews Drug Discovery. 2 (6): 439–47. doi:10.1038/nrd1108. PMID 12776219. S2CID 27492332.
Cumming JG, Cooper AE, Grime K, et al. (November 2005). "Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides". Bioorganic & Medicinal Chemistry Letters. 15 (22): 5012–5. doi:10.1016/j.bmcl.2005.08.014. PMID 16154744.
Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG (April 2004). "Orally bioavailable competitive CCR5 antagonists". Journal of Medicinal Chemistry. 47 (8): 1939–55. doi:10.1021/jm031046g. PMID 15055994.
Bryan Oates; Richard J. Budhu; Sander G. Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S. Springer; Bruce L. Daugherty; Sandra L. Gould; Julie A. DeMartino; Salvatore J. Siciliano; Anthony Carella; Gwen Carver; Karen Holmes; Renee Danzeisen; Daria Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; William A. Schleif; Emilio A. Emini (January 2001). "Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes". Bioorganic & Medicinal Chemistry Letters. 11 (2): 259–64. doi:10.1016/S0960-894X(00)00637-5. PMID 11206473.
Tremblay CL, Giguel F, Guan Y, Chou TC, Takashima K, Hirsch MS (August 2005). "TAK-220, a Novel Small-Molecule CCR5 Antagonist, Has Favorable Anti-Human Immunodeficiency Virus Interactions with Other Antiretrovirals In Vitro". Antimicrobial Agents and Chemotherapy. 49 (8): 3483–5. doi:10.1128/AAC.49.8.3483-3485.2005. PMC 1196290. PMID 16048964.
"Phase 2 clinical trials started on PRO 140". AIDS Patient Care and STDs. 22 (2): 159–60. February 2008. doi:10.1089/apc.2008.9960. PMID 18273941. ^{[verification needed]}
Biswas P, Tambussi G, Lazzarin A (2007). "Access denied? The status of co-receptor inhibition to counter HIV entry". Expert Opin Pharmacother. 8 (7): 923–33. doi:10.1517/14656566.8.7.923. PMID 17472538. S2CID 32675897. ^{[verification needed]}
Pugach P, Ketas TJ, Michael E, Moore JP (August 2008). "Neutralizing antibody and anti-retroviral drug sensitivities of HIV-1 isolates resistant to small molecule CCR5 inhibitors". Virology. 377 (2): 401–7. doi:10.1016/j.virol.2008.04.032. PMC 2528836. PMID 18519143. ^{[verification needed]}
Jiao X, Wang M, Zhang Z, Li Z, Ni D, Ashton AW, Tang HY, Speicher DW, Pestell RG, et al. (January 2021). "Leronlimab, a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy". Breast Cancer Research. 23 (1): 11. doi:10.1186/s13058-021-01391-1. PMC 7825185. PMID 33485378.
Maeda K, Nakata H, Koh Y, et al. (August 2004). "Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro". Journal of Virology. 78 (16): 8654–62. doi:10.1128/JVI.78.16.8654-8662.2004. PMC 479103. PMID 15280474.
Tagat JR, McCombie SW, Steensma RW, et al. (August 2001). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element". Bioorganic & Medicinal Chemistry Letters. 11 (16): 2143–6. doi:10.1016/S0960-894X(01)00381-X. PMID 11514156.
Tagat JR, Steensma RW, McCombie SW, et al. (October 2001). "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". Journal of Medicinal Chemistry. 44 (21): 3343–6. doi:10.1021/jm0155401. PMID 11585438.
McCombie SW, Tagat JR, Vice SF, et al. (February 2003). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides". Bioorganic & Medicinal Chemistry Letters. 13 (3): 567–71. doi:10.1016/S0960-894X(02)00918-6. PMID 12565973.
Tagat JR, McCombie SW, Nazareno D, et al. (May 2004). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist". Journal of Medicinal Chemistry. 47 (10): 2405–8. doi:10.1021/jm0304515. PMID 15115380.
Dorr, P; Westby, M; Dobbs, S; Griffin, P; Irvine, B; Macartney, M; Mori, J; Rickett, G; Smith-Burchnell, C; Napier, C; Webster, R; Armour, D; Price, D; Stammen, B; Wood, A; Perros, M (November 2005). "Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity". Antimicrobial Agents and Chemotherapy. 49 (11): 4721–32. doi:10.1128/AAC.49.11.4721-4732.2005. PMC 1280117. PMID 16251317.
Wood A, Armour D (2005). The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS. Progress in Medicinal Chemistry. Vol. 43. pp. 239–71. doi:10.1016/S0079-6468(05)43007-6. ISBN 978-0-444-51572-8. PMID 15850827.
Price DA, Armour D, de Groot M, et al. (September 2006). "Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc". Bioorganic & Medicinal Chemistry Letters. 16 (17): 4633–7. doi:10.1016/j.bmcl.2006.06.012. PMID 16782336.
Debnath AK (October 2003). "Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors". Journal of Medicinal Chemistry. 46 (21): 4501–15. doi:10.1021/jm030265z. PMID 14521412.
Maeda K, Das D, Ogata-Aoki H, et al. (May 2006). "Structural and molecular interactions of CCR5 inhibitors with CCR5". The Journal of Biological Chemistry. 281 (18): 12688–98. doi:10.1074/jbc.M512688200. PMID 16476734.
Kondru R, Zhang J, Ji C, et al. (March 2008). "Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists". Molecular Pharmacology. 73 (3): 789–800. doi:10.1124/mol.107.042101. PMID 18096812. S2CID 16267853.
Wang T, Duan Y (June 2008). "Binding Modes of CCR5-targetting HIV Entry Inhibitors: Partial and Full Antagonists". Journal of Molecular Graphics & Modelling. 26 (8): 1287–95. doi:10.1016/j.jmgm.2007.12.003. PMC 2701198. PMID 18249144.
Arimont A, Sun S, Smit MJ, Leurs R, de Esch IJ, de Graaf C (2017). "Structural Analysis of Chemokine Receptor-Ligand Interactions". J Med Chem. 60 (12): 4735–4779. doi:10.1021/acs.jmedchem.6b01309. PMC 5483895. PMID 28165741.
Rotstein DM, Gabriel SD, Makra F, et al. (September 2009). "Spiropiperidine CCR5 antagonists". Bioorganic & Medicinal Chemistry Letters. 19 (18): 5401–6. doi:10.1016/j.bmcl.2009.07.122. PMID 19674898.
Kuritzkes DR (March 2009). "HIV-1 Entry Inhbitors: An Overview". Current Opinion in HIV and AIDS. 4 (2): 82–7. doi:10.1097/COH.0b013e328322402e. PMC 2753507. PMID 19339945.
Swan CH, Bühler B, Steinberger P, Tschan MP, Barbas CF 3rd, Torbett BE, et al. (June 2006). "T-cell protection and enrichment through lentiviral CCR5 intrabody gene delivery". Gene Ther. 13 (20): 1480–92. doi:10.1038/sj.gt.3302801. PMID 16738691.
Zhang C, Ötjengerdes RM, Roewe J, Mejias R, Marschall AL, et al. (April 2020). "Applying Antibodies Inside Cells: Principles and Recent Advances in Neurobiology, Virology and Oncology". BioDrugs. 34 (4): 435–462. doi:10.1007/s40259-020-00419-w. PMC 7391400. PMID 32301049.

fool.com

Brian Lawler. Progenics' Intriguing Study Results. The Motley Fool. 2 May 2007. ^{[verification needed]}

harvard.edu

ui.adsabs.harvard.edu

Samson M, Libert F, Doranz BJ, et al. (August 1996). "Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene". Nature. 382 (6593): 722–5. Bibcode:1996Natur.382..722S. doi:10.1038/382722a0. PMID 8751444. S2CID 4370818.
Dragic T, Litwin V, Allaway GP, et al. (June 1996). "HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5". Nature. 381 (6584): 667–73. Bibcode:1996Natur.381..667D. doi:10.1038/381667a0. PMID 8649512. S2CID 4301976.

hivandhepatitis.com

Liz Highleyman. Monoclonal Antibody CCR5 Inhibitor PRO 140 Produces Long-lasting HIV Suppression in Single-dose Study. 28 Sept 2007. HIVandHepatitis.com ^{[verification needed]}

natap.org

"Schering-Plough Reports Long-Term Vicriviroc Data From Phase II Open-Label Extension Study in Treatment-Experienced HIV-Infected Patients" (Press release). Schering-Plough. 14 September 2009. Retrieved 8 November 2009.

nih.gov

pubmed.ncbi.nlm.nih.gov

Lederman MM, Penn-Nicholson A, Cho M, Mosier D (August 2006). "Biology of CCR5 and its role in HIV infection and treatment". JAMA. 296 (7): 815–26. doi:10.1001/jama.296.7.815. PMID 16905787.
De Clercq E (December 2007). "The design of drugs for HIV and HCV". Nature Reviews Drug Discovery. 6 (12): 1001–18. doi:10.1038/nrd2424. PMID 18049474. S2CID 37859193.
Samson M, Libert F, Doranz BJ, et al. (August 1996). "Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene". Nature. 382 (6593): 722–5. Bibcode:1996Natur.382..722S. doi:10.1038/382722a0. PMID 8751444. S2CID 4370818.
Dragic T, Litwin V, Allaway GP, et al. (June 1996). "HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5". Nature. 381 (6584): 667–73. Bibcode:1996Natur.381..667D. doi:10.1038/381667a0. PMID 8649512. S2CID 4301976.
Flexner C (December 2007). "HIV drug development: the next 25 years". Nature Reviews Drug Discovery. 6 (12): 959–66. doi:10.1038/nrd2336. PMID 17932493. S2CID 31261997.
Ray N, Doms RW (2006). "HIV-1 Coreceptors and Their Inhibitors". Chemokines and Viral Infection. Current Topics in Microbiology and Immunology. Vol. 303. pp. 97–120. doi:10.1007/978-3-540-33397-5_5. ISBN 978-3-540-29207-4. PMID 16570858.
Westby M, van der Ryst E (2005). "CCR5 antagonists: host-targeted antivirals for the treatment of HIV infection". Antiviral Chemistry & Chemotherapy. 16 (6): 339–54. doi:10.1177/095632020501600601. PMID 16329283. S2CID 24994759.
Briz V, Poveda E, Soriano V (April 2006). "HIV entry inhibitors: mechanisms of action and resistance pathways". The Journal of Antimicrobial Chemotherapy. 57 (4): 619–27. doi:10.1093/jac/dkl027. PMID 16464888.
Murga JD, Franti M, Pevear DC, Maddon PJ, Olson WC (October 2006). "Potent Antiviral Synergy between Monoclonal Antibody and Small-Molecule CCR5 Inhibitors of Human Immunodeficiency Virus Type 1". Antimicrobial Agents and Chemotherapy. 50 (10): 3289–96. doi:10.1128/AAC.00699-06. PMC 1610098. PMID 17005807.
Watson C, Jenkinson S, Kazmierski W, Kenakin T (April 2005). "The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor". Molecular Pharmacology. 67 (4): 1268–82. doi:10.1124/mol.104.008565. PMID 15644495. S2CID 2587200.
Fermini B, Fossa AA (June 2003). "The impact of drug-induced QT interval prolongation on drug discovery and development". Nature Reviews Drug Discovery. 2 (6): 439–47. doi:10.1038/nrd1108. PMID 12776219. S2CID 27492332.
Cumming JG, Cooper AE, Grime K, et al. (November 2005). "Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides". Bioorganic & Medicinal Chemistry Letters. 15 (22): 5012–5. doi:10.1016/j.bmcl.2005.08.014. PMID 16154744.
Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG (April 2004). "Orally bioavailable competitive CCR5 antagonists". Journal of Medicinal Chemistry. 47 (8): 1939–55. doi:10.1021/jm031046g. PMID 15055994.
Bryan Oates; Richard J. Budhu; Sander G. Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S. Springer; Bruce L. Daugherty; Sandra L. Gould; Julie A. DeMartino; Salvatore J. Siciliano; Anthony Carella; Gwen Carver; Karen Holmes; Renee Danzeisen; Daria Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; William A. Schleif; Emilio A. Emini (January 2001). "Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes". Bioorganic & Medicinal Chemistry Letters. 11 (2): 259–64. doi:10.1016/S0960-894X(00)00637-5. PMID 11206473.
Tremblay CL, Giguel F, Guan Y, Chou TC, Takashima K, Hirsch MS (August 2005). "TAK-220, a Novel Small-Molecule CCR5 Antagonist, Has Favorable Anti-Human Immunodeficiency Virus Interactions with Other Antiretrovirals In Vitro". Antimicrobial Agents and Chemotherapy. 49 (8): 3483–5. doi:10.1128/AAC.49.8.3483-3485.2005. PMC 1196290. PMID 16048964.
"Phase 2 clinical trials started on PRO 140". AIDS Patient Care and STDs. 22 (2): 159–60. February 2008. doi:10.1089/apc.2008.9960. PMID 18273941. ^{[verification needed]}
Biswas P, Tambussi G, Lazzarin A (2007). "Access denied? The status of co-receptor inhibition to counter HIV entry". Expert Opin Pharmacother. 8 (7): 923–33. doi:10.1517/14656566.8.7.923. PMID 17472538. S2CID 32675897. ^{[verification needed]}
Pugach P, Ketas TJ, Michael E, Moore JP (August 2008). "Neutralizing antibody and anti-retroviral drug sensitivities of HIV-1 isolates resistant to small molecule CCR5 inhibitors". Virology. 377 (2): 401–7. doi:10.1016/j.virol.2008.04.032. PMC 2528836. PMID 18519143. ^{[verification needed]}
Jiao X, Wang M, Zhang Z, Li Z, Ni D, Ashton AW, Tang HY, Speicher DW, Pestell RG, et al. (January 2021). "Leronlimab, a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy". Breast Cancer Research. 23 (1): 11. doi:10.1186/s13058-021-01391-1. PMC 7825185. PMID 33485378.
Maeda K, Nakata H, Koh Y, et al. (August 2004). "Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro". Journal of Virology. 78 (16): 8654–62. doi:10.1128/JVI.78.16.8654-8662.2004. PMC 479103. PMID 15280474.
Tagat JR, McCombie SW, Steensma RW, et al. (August 2001). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element". Bioorganic & Medicinal Chemistry Letters. 11 (16): 2143–6. doi:10.1016/S0960-894X(01)00381-X. PMID 11514156.
Tagat JR, Steensma RW, McCombie SW, et al. (October 2001). "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". Journal of Medicinal Chemistry. 44 (21): 3343–6. doi:10.1021/jm0155401. PMID 11585438.
McCombie SW, Tagat JR, Vice SF, et al. (February 2003). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides". Bioorganic & Medicinal Chemistry Letters. 13 (3): 567–71. doi:10.1016/S0960-894X(02)00918-6. PMID 12565973.
Tagat JR, McCombie SW, Nazareno D, et al. (May 2004). "Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist". Journal of Medicinal Chemistry. 47 (10): 2405–8. doi:10.1021/jm0304515. PMID 15115380.
Dorr, P; Westby, M; Dobbs, S; Griffin, P; Irvine, B; Macartney, M; Mori, J; Rickett, G; Smith-Burchnell, C; Napier, C; Webster, R; Armour, D; Price, D; Stammen, B; Wood, A; Perros, M (November 2005). "Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity". Antimicrobial Agents and Chemotherapy. 49 (11): 4721–32. doi:10.1128/AAC.49.11.4721-4732.2005. PMC 1280117. PMID 16251317.
Wood A, Armour D (2005). The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS. Progress in Medicinal Chemistry. Vol. 43. pp. 239–71. doi:10.1016/S0079-6468(05)43007-6. ISBN 978-0-444-51572-8. PMID 15850827.
Price DA, Armour D, de Groot M, et al. (September 2006). "Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc". Bioorganic & Medicinal Chemistry Letters. 16 (17): 4633–7. doi:10.1016/j.bmcl.2006.06.012. PMID 16782336.
Debnath AK (October 2003). "Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors". Journal of Medicinal Chemistry. 46 (21): 4501–15. doi:10.1021/jm030265z. PMID 14521412.
Maeda K, Das D, Ogata-Aoki H, et al. (May 2006). "Structural and molecular interactions of CCR5 inhibitors with CCR5". The Journal of Biological Chemistry. 281 (18): 12688–98. doi:10.1074/jbc.M512688200. PMID 16476734.
Kondru R, Zhang J, Ji C, et al. (March 2008). "Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists". Molecular Pharmacology. 73 (3): 789–800. doi:10.1124/mol.107.042101. PMID 18096812. S2CID 16267853.
Wang T, Duan Y (June 2008). "Binding Modes of CCR5-targetting HIV Entry Inhibitors: Partial and Full Antagonists". Journal of Molecular Graphics & Modelling. 26 (8): 1287–95. doi:10.1016/j.jmgm.2007.12.003. PMC 2701198. PMID 18249144.
Arimont A, Sun S, Smit MJ, Leurs R, de Esch IJ, de Graaf C (2017). "Structural Analysis of Chemokine Receptor-Ligand Interactions". J Med Chem. 60 (12): 4735–4779. doi:10.1021/acs.jmedchem.6b01309. PMC 5483895. PMID 28165741.
Rotstein DM, Gabriel SD, Makra F, et al. (September 2009). "Spiropiperidine CCR5 antagonists". Bioorganic & Medicinal Chemistry Letters. 19 (18): 5401–6. doi:10.1016/j.bmcl.2009.07.122. PMID 19674898.
Kuritzkes DR (March 2009). "HIV-1 Entry Inhbitors: An Overview". Current Opinion in HIV and AIDS. 4 (2): 82–7. doi:10.1097/COH.0b013e328322402e. PMC 2753507. PMID 19339945.
Swan CH, Bühler B, Steinberger P, Tschan MP, Barbas CF 3rd, Torbett BE, et al. (June 2006). "T-cell protection and enrichment through lentiviral CCR5 intrabody gene delivery". Gene Ther. 13 (20): 1480–92. doi:10.1038/sj.gt.3302801. PMID 16738691.
Zhang C, Ötjengerdes RM, Roewe J, Mejias R, Marschall AL, et al. (April 2020). "Applying Antibodies Inside Cells: Principles and Recent Advances in Neurobiology, Virology and Oncology". BioDrugs. 34 (4): 435–462. doi:10.1007/s40259-020-00419-w. PMC 7391400. PMID 32301049.

ncbi.nlm.nih.gov

Murga JD, Franti M, Pevear DC, Maddon PJ, Olson WC (October 2006). "Potent Antiviral Synergy between Monoclonal Antibody and Small-Molecule CCR5 Inhibitors of Human Immunodeficiency Virus Type 1". Antimicrobial Agents and Chemotherapy. 50 (10): 3289–96. doi:10.1128/AAC.00699-06. PMC 1610098. PMID 17005807.
Tremblay CL, Giguel F, Guan Y, Chou TC, Takashima K, Hirsch MS (August 2005). "TAK-220, a Novel Small-Molecule CCR5 Antagonist, Has Favorable Anti-Human Immunodeficiency Virus Interactions with Other Antiretrovirals In Vitro". Antimicrobial Agents and Chemotherapy. 49 (8): 3483–5. doi:10.1128/AAC.49.8.3483-3485.2005. PMC 1196290. PMID 16048964.
Pugach P, Ketas TJ, Michael E, Moore JP (August 2008). "Neutralizing antibody and anti-retroviral drug sensitivities of HIV-1 isolates resistant to small molecule CCR5 inhibitors". Virology. 377 (2): 401–7. doi:10.1016/j.virol.2008.04.032. PMC 2528836. PMID 18519143. ^{[verification needed]}
Jiao X, Wang M, Zhang Z, Li Z, Ni D, Ashton AW, Tang HY, Speicher DW, Pestell RG, et al. (January 2021). "Leronlimab, a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy". Breast Cancer Research. 23 (1): 11. doi:10.1186/s13058-021-01391-1. PMC 7825185. PMID 33485378.
Maeda K, Nakata H, Koh Y, et al. (August 2004). "Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro". Journal of Virology. 78 (16): 8654–62. doi:10.1128/JVI.78.16.8654-8662.2004. PMC 479103. PMID 15280474.
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Lalezari, J.; Goodrich, J.; DeJesus, E.; Lampiris, H.; Gulick, R.; Saag, M.; Ridgway, C.; McHale, M.; Van Der Ryst, E. "Efficacy and Safety of Maraviroc plus Optimized Background Therapy In Viremic, ART-Experienced Patients Infected With CCR5-Tropic HIV‑1, 24-week results of a Phase 2b/3 study in the U. S. & Canada. Abstract 104bLB". 14th Conference on Retroviruses and Opportunistic Infections. Archived from the original on 2009-03-18. Retrieved 2009-11-03.

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web.archive.org

Lalezari, J.; Goodrich, J.; DeJesus, E.; Lampiris, H.; Gulick, R.; Saag, M.; Ridgway, C.; McHale, M.; Van Der Ryst, E. "Efficacy and Safety of Maraviroc plus Optimized Background Therapy In Viremic, ART-Experienced Patients Infected With CCR5-Tropic HIV‑1, 24-week results of a Phase 2b/3 study in the U. S. & Canada. Abstract 104bLB". 14th Conference on Retroviruses and Opportunistic Infections. Archived from the original on 2009-03-18. Retrieved 2009-11-03.
"CytoDyn Announces Acquisition of PRO 140" (Press release). CytoDyn Inc. October 17, 2012. Archived from the original on September 25, 2013. Retrieved September 3, 2019. ^{[verification needed]}
Derek Thaczuk. ICAAC: Phase 1 study provides 'proof of concept' for PRO 140, a monoclonal CCR5 antibody Archived 2007-10-27 at the Wayback Machine. AIDSmap.com. 21 Sept 2007. ^{[verification needed]}
"Progenics Pharmaceuticals' HIV Drug, PRO 140, Receives FDA Fast-Track Designation" Archived 2011-10-02 at the Wayback Machine. Press release, 22 February 2006. Progenics Pharmaceuticals. progenics.com. ^{[verification needed]}
"PRO 140" Archived 2012-04-02 at the Wayback Machine. Progenics Pharmaceuticals. progenics.com. ^{[verification needed]}