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Camarasa MJ

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Publications:

Title Authors Year Journal
N-3 substituted TSAO derivatives as a probe to explore the dimeric interface of HIV-1 reverse transcriptase. Camarasa MJ Nucleosides, nucleotides & nucleic acids
Recent advances in thymidine kinase 2 (TK2) inhibitors and new perspectives for potential applications. Camarasa MJ 2012 Current pharmaceutical design
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket. Camarasa MJ 2011 Journal of medicinal chemistry
Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides. Camarasa MJ 2011 Antiviral research
4"-Benzoylureido-TSAO derivatives as potent and selective non-nucleoside HCMV inhibitors. Structure-activity relationship and mechanism of antiviral action. Camarasa MJ 2008 Journal of medicinal chemistry
Novel non-nucleoside human cytomegalovirus inhibitors based upon TSAO nucleoside derivatives: structure-activity relationships. Camarasa MJ 2007 Nucleosides, nucleotides & nucleic acids
Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: a single mode of inhibition for the three HIV enzymes? Camarasa MJ 2006 Antiviral research
TSAO derivatives, inhibitors of HIV-1 reverse transcriptase dimerization: recent progress. Camarasa MJ 2006 Current pharmaceutical design
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization. Camarasa MJ 2006 Journal of medicinal chemistry
The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs. Camarasa MJ 2005 FEBS letters
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors. Camarasa MJ 2005 Molecular pharmacology
TSAO derivatives the first non-peptide inhibitors of HIV-1 RT dimerization. Camarasa MJ 2005 Antiviral chemistry & chemotherapy
The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A. Camarasa MJ 2005 Molecular pharmacology
TSAO compounds: the comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase. Camarasa MJ 2004 Current topics in medicinal chemistry
Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors. Camarasa MJ 2003 Antiviral chemistry & chemotherapy
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach. Camarasa MJ 2002 Journal of medicinal chemistry
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase. Camarasa MJ 2001 Bioorganic & medicinal chemistry letters
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138. Camarasa MJ 2001 Virology
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. Camarasa MJ 2001 Journal of medicinal chemistry
Exploitation of the low fidelity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase and the nucleotide composition bias in the HIV-1 genome to alter the drug resistance development of HIV. Camarasa MJ 2001 Journal of virology
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients. Camarasa MJ 2000 AIDS research and human retroviruses
Human immunodeficiency virus type 1 reverse transcriptase dimer destabilization by 1-[Spiro[4"-amino-2",2" -dioxo-1",2" -oxathiole-5",3'-[2', 5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]]]-3-ethylthy mine. Camarasa MJ 2000 Biochemistry
Potential multifunctional inhibitors of HIV-1 reverse transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] heterodimers modified in the linker and in the dideoxynucleoside region. Camarasa MJ 1999 Journal of medicinal chemistry
An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase. Camarasa MJ 1998 Antiviral chemistry & chemotherapy
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase. Camarasa MJ 1998 Journal of medicinal chemistry
Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine. Camarasa MJ 1996 Molecular pharmacology
Novel L-lyxo and 5'-deoxy-5'-modified TSAO-T analogs: synthesis and anti-HIV-1 activity. Camarasa MJ 1996 Antiviral research
Differences in the inhibition of human immunodeficiency virus type 1 reverse transcriptase DNA polymerase activity by analogs of nevirapine and [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1", 2"-oxathiole-2",2"-dioxide] (TSAO). Camarasa MJ 1996 Molecular pharmacology
Sensitivity/resistance profile of a simian immunodeficiency virus containing the reverse transcriptase gene of human immunodeficiency virus type 1 (HIV-1) toward the HIV-1-specific non-nucleoside reverse transcriptase inhibitors. Camarasa MJ 1995 Biochemical and biophysical research communications
Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives). Camarasa MJ 1995 Proceedings of the National Academy of Sciences of the United States of America
Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. Camarasa MJ 1995 Journal of medicinal chemistry
Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit. Camarasa MJ 1994 The Journal of biological chemistry
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants. Camarasa MJ 1994 Proceedings of the National Academy of Sciences of the United States of America
Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors. Camarasa MJ 1994 Biochemical and biophysical research communications
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase. Camarasa MJ 1993 Virology
Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus. Camarasa MJ 1993 Virology
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues. Camarasa MJ 1993 Molecular pharmacology
Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy. Camarasa MJ 1993 Journal of virology
Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T). Camarasa MJ 1992 The Journal of biological chemistry
2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase. Camarasa MJ 1992 Proceedings of the National Academy of Sciences of the United States of America
[2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1. Camarasa MJ 1992 Antimicrobial agents and chemotherapy

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