Literature summary for 3.1.13.2 extracted from

Arion, D.; Sluis-Cremer, N.; Min, K.L.; Abram, M.E.; Fletcher, R.S.; Parniak, M.A.
Mutational analysis of Tyr-501 of HIV-1 reverse transcriptase: effects on ribonuclease H activity and inhibition of this activity by N-acylhydrazones (2002), J. Biol. Chem., 277, 1370-1374.

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Cloned(Commentary)

Cloned (Comment)	Organism
-	Human immunodeficiency virus 1

Protein Variants

Protein Variants	Comment	Organism
Y501A	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501E	25% activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501F	85% activity in comparison to wild-type enzyme, the mutant remains sensitive to N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone inhibition	Human immunodeficiency virus 1
Y501G	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501H	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501L	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501Q	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501R	90% activity in comparison to wild-type enzyme, the mutant is completely resistant to N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone inhibition	Human immunodeficiency virus 1
Y501S	complete loss of activity in comparison to wild-type enzyme	Human immunodeficiency virus 1
Y501W	100% activity in comparison to wild-type enzyme, 6fold decreased sensitivity to inhibition N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone	Human immunodeficiency virus 1

Inhibitors

Inhibitors	Comment	Organism	Structure
N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone	BBNH, the residue Tyr501 is integral in the binding interaction, mechanism	Human immunodeficiency virus 1

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 1	P03366	HIV-1	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
additional information	-	comparison of relative activities of wild-type and mutant enzymes	Human immunodeficiency virus 1

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
5' RNA-DNA duplex + H2O	-	Human immunodeficiency virus 1	oligonucleotides terminated with 5'-phosphate and 3'-hydroxyl moiety	-	?

Synonyms

Synonyms	Comment	Organism
RT RNase H	-	Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0043	-	N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone	pH 7.9, 37°C, wild-type enzyme	Human immunodeficiency virus 1
0.0047	-	N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone	pH 7.9, 37°C, mutant Y501F	Human immunodeficiency virus 1
0.0206	-	N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone	pH 7.9, 37°C, mutant Y501W	Human immunodeficiency virus 1

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Release 2023.1 (January 2023)