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Items: 1 to 20 of 122

1.

A conserved hydrogen-bonding network of P2 bis-tetrahydrofuran-containing HIV-1 protease inhibitors (PIs) with a protease active-site amino acid backbone aids in their activity against PI-resistant HIV.

Yedidi RS, Garimella H, Aoki M, Aoki-Ogata H, Desai DV, Chang SB, Davis DA, Fyvie WS, Kaufman JD, Smith DW, Das D, Wingfield PT, Maeda K, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2014 Jul;58(7):3679-88. doi: 10.1128/AAC.00107-14. Epub 2014 Apr 21.

2.

GRL-0519, a novel oxatricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor (PI), potently suppresses replication of a wide spectrum of multi-PI-resistant HIV-1 variants in vitro.

Amano M, Tojo Y, Salcedo-Gómez PM, Campbell JR, Das D, Aoki M, Xu CX, Rao KV, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2013 May;57(5):2036-46. doi: 10.1128/AAC.02189-12. Epub 2013 Feb 12.

3.

C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir.

Aoki M, Hayashi H, Yedidi RS, Martyr CD, Takamatsu Y, Aoki-Ogata H, Nakamura T, Nakata H, Das D, Yamagata Y, Ghosh AK, Mitsuya H.

J Virol. 2015 Nov 18;90(5):2180-94. doi: 10.1128/JVI.01829-15.

4.

P2' benzene carboxylic acid moiety is associated with decrease in cellular uptake: evaluation of novel nonpeptidic HIV-1 protease inhibitors containing P2 bis-tetrahydrofuran moiety.

Yedidi RS, Maeda K, Fyvie WS, Steffey M, Davis DA, Palmer I, Aoki M, Kaufman JD, Stahl SJ, Garimella H, Das D, Wingfield PT, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2013 Oct;57(10):4920-7. doi: 10.1128/AAC.00868-13. Epub 2013 Jul 22.

5.

GRL-04810 and GRL-05010, difluoride-containing nonpeptidic HIV-1 protease inhibitors (PIs) that inhibit the replication of multi-PI-resistant HIV-1 in vitro and possess favorable lipophilicity that may allow blood-brain barrier penetration.

Salcedo Gómez PM, Amano M, Yashchuk S, Mizuno A, Das D, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2013 Dec;57(12):6110-21. doi: 10.1128/AAC.01420-13. Epub 2013 Sep 30.

6.

Design of HIV protease inhibitors targeting protein backbone: an effective strategy for combating drug resistance.

Ghosh AK, Chapsal BD, Weber IT, Mitsuya H.

Acc Chem Res. 2008 Jan;41(1):78-86. Epub 2007 Aug 28. Review.

PMID:
17722874
7.

Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.

Tojo Y, Koh Y, Amano M, Aoki M, Das D, Kulkarni S, Anderson DD, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2010 Aug;54(8):3460-70. doi: 10.1128/AAC.01766-09. Epub 2010 May 3.

8.

Novel HIV-1 protease inhibitors (PIs) containing a bicyclic P2 functional moiety, tetrahydropyrano-tetrahydrofuran, that are potent against multi-PI-resistant HIV-1 variants.

Ide K, Aoki M, Amano M, Koh Y, Yedidi RS, Das D, Leschenko S, Chapsal B, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2011 Apr;55(4):1717-27. doi: 10.1128/AAC.01540-10. Epub 2011 Jan 31.

9.

A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.

Amano M, Koh Y, Das D, Li J, Leschenko S, Wang YF, Boross PI, Weber IT, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2007 Jun;51(6):2143-55. Epub 2007 Mar 19.

10.

In vitro and structural evaluation of PL-100 as a potential second-generation HIV-1 protease inhibitor.

Asahchop EL, Oliveira M, Quashie PK, Moisi D, Martinez-Cajas JL, Brenner BG, Tremblay CL, Wainberg MA.

J Antimicrob Chemother. 2013 Jan;68(1):105-12. doi: 10.1093/jac/dks342. Epub 2012 Sep 3.

PMID:
22945918
11.

Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.

Koh Y, Nakata H, Maeda K, Ogata H, Bilcer G, Devasamudram T, Kincaid JF, Boross P, Wang YF, Tie Y, Volarath P, Gaddis L, Harrison RW, Weber IT, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2003 Oct;47(10):3123-9.

12.

The higher barrier of darunavir and tipranavir resistance for HIV-1 protease.

Wang Y, Liu Z, Brunzelle JS, Kovari IA, Dewdney TG, Reiter SJ, Kovari LC.

Biochem Biophys Res Commun. 2011 Sep 9;412(4):737-42. doi: 10.1016/j.bbrc.2011.08.045. Epub 2011 Aug 17.

13.

A novel tricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor, GRL-0739, effectively inhibits the replication of multidrug-resistant HIV-1 variants and has a desirable central nervous system penetration property in vitro.

Amano M, Tojo Y, Salcedo-Gómez PM, Parham GL, Nyalapatla PR, Das D, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2015 May;59(5):2625-35. doi: 10.1128/AAC.04757-14. Epub 2015 Feb 17.

14.

GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.

Koh Y, Das D, Leschenko S, Nakata H, Ogata-Aoki H, Amano M, Nakayama M, Ghosh AK, Mitsuya H.

Antimicrob Agents Chemother. 2009 Mar;53(3):997-1006. doi: 10.1128/AAC.00689-08. Epub 2008 Oct 27.

15.

Design of HIV-1 Protease Inhibitors with Amino-bis-tetrahydrofuran Derivatives as P2-Ligands to Enhance Backbone-Binding Interactions: Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies.

Ghosh AK, Martyr CD, Osswald HL, Sheri VR, Kassekert LA, Chen S, Agniswamy J, Wang YF, Hayashi H, Aoki M, Weber IT, Mitsuya H.

J Med Chem. 2015 Sep 10;58(17):6994-7006. doi: 10.1021/acs.jmedchem.5b00900. Epub 2015 Aug 25.

16.

Design of gem-difluoro-bis-tetrahydrofuran as P2 ligand for HIV-1 protease inhibitors to improve brain penetration: synthesis, X-ray studies, and biological evaluation.

Ghosh AK, Yashchuk S, Mizuno A, Chakraborty N, Agniswamy J, Wang YF, Aoki M, Gomez PM, Amano M, Weber IT, Mitsuya H.

ChemMedChem. 2015 Jan;10(1):107-15. doi: 10.1002/cmdc.201402358. Epub 2014 Oct 21.

17.

Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.

Agniswamy J, Shen CH, Wang YF, Ghosh AK, Rao KV, Xu CX, Sayer JM, Louis JM, Weber IT.

J Med Chem. 2013 May 23;56(10):4017-27. doi: 10.1021/jm400231v. Epub 2013 May 1.

18.

Binding kinetics of darunavir to human immunodeficiency virus type 1 protease explain the potent antiviral activity and high genetic barrier.

Dierynck I, De Wit M, Gustin E, Keuleers I, Vandersmissen J, Hallenberger S, Hertogs K.

J Virol. 2007 Dec;81(24):13845-51. Epub 2007 Oct 10.

19.

A potent human immunodeficiency virus type 1 protease inhibitor, UIC-94003 (TMC-126), and selection of a novel (A28S) mutation in the protease active site.

Yoshimura K, Kato R, Kavlick MF, Nguyen A, Maroun V, Maeda K, Hussain KA, Ghosh AK, Gulnik SV, Erickson JW, Mitsuya H.

J Virol. 2002 Feb;76(3):1349-58.

20.

Molecular characterization of clinical isolates of human immunodeficiency virus resistant to the protease inhibitor darunavir.

Sasková KG, Kozísek M, Rezácová P, Brynda J, Yashina T, Kagan RM, Konvalinka J.

J Virol. 2009 Sep;83(17):8810-8. doi: 10.1128/JVI.00451-09. Epub 2009 Jun 17.

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