PMID- 8774754
OWN - NLM
STAT- MEDLINE
DCOM- 19961003
LR  - 20190629
IS  - 0014-4754 (Print)
IS  - 0014-4754 (Linking)
VI  - 52
IP  - 8
DP  - 1996 Aug 15
TI  - Inhibition mechanisms of HIV-1, Mo-MuLV and AMV reverse transcriptases by 
      Kelletinin A from Buccinulum corneum.
PG  - 812-7
AB  - Kelletinin A [ribity pentakis (p-hydroxybenzoate)] (KA), an inhibitor of HTLV-1 
      replication isolated from Buccinulum corneum, showed a noncompetitive inhibitory 
      activity with respect to the template primer and to dTTP in the 
      poly(rA).oligo(dT)12-18-directed reaction of HIV-1, Mo-MuLV and AMV reverse 
      transcriptases (RT). Analysis of natural and synthetic KA-related compounds 
      showed that the inhibitory activity was strictly related to the structural 
      peculiarities of the molecule. In the presence of DNA as template primer the 
      inhibition mechanism was drastically modified: HIV-1 RT activity was stimulated 
      by low concentrations of KA and was inhibited by increasing the concentration of 
      the compound, while Mo-MuLV and AMV activities were irreversibly inhibited by the 
      formation of a non-reactive complex. The RNase H activities of these RTs were not 
      affected by KA. The results of this study suggest a different mechanism of 
      interaction of Kelletinins with HIV-1 RT compared with other non-nucleoside 
      inhibitors. A possible use of these drugs in combination therapy and in the 
      design of structure-based reverse transcriptase inhibitors is discussed.
FAU - Orlando, P
AU  - Orlando P
AD  - Istituto Biochimica delle Proteine ed Enzimologia, CNR, Arco Felice, Naples, 
      Italy.
FAU - Strazzullo, G
AU  - Strazzullo G
FAU - Carretta, F
AU  - Carretta F
FAU - De Falco, M
AU  - De Falco M
FAU - Grippo, P
AU  - Grippo P
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Switzerland
TA  - Experientia
JT  - Experientia
JID - 0376547
RN  - 0 (Antiviral Agents)
RN  - 0 (DNA, Viral)
RN  - 0 (Hydroxybenzoates)
RN  - 0 (Oligodeoxyribonucleotides)
RN  - 0 (Reverse Transcriptase Inhibitors)
RN  - 112727-22-7 (kelletinin A)
RN  - 24937-83-5 (Poly A)
RN  - 488-81-3 (Ribitol)
RN  - 60164-00-3 (poly(rA).oligo(dT))
RN  - EC 2.7.7.49 (HIV Reverse Transcriptase)
RN  - EC 2.7.7.49 (RNA-Directed DNA Polymerase)
RN  - EC 3.1.26.4 (Ribonuclease H)
SB  - IM
MH  - Animals
MH  - Antiviral Agents/pharmacology
MH  - Avian Myeloblastosis Virus/drug effects/*enzymology
MH  - DNA, Viral/metabolism
MH  - HIV Reverse Transcriptase
MH  - HIV-1/drug effects/*enzymology
MH  - Hydroxybenzoates/*pharmacology
MH  - Kinetics
MH  - Mollusca/chemistry
MH  - Moloney murine leukemia virus/drug effects/*enzymology
MH  - Oligodeoxyribonucleotides/metabolism
MH  - Poly A/metabolism
MH  - RNA-Directed DNA Polymerase/*metabolism
MH  - Reverse Transcriptase Inhibitors/*pharmacology
MH  - Ribitol/*analogs & derivatives/pharmacology
MH  - Ribonuclease H/metabolism
MH  - Templates, Genetic
EDAT- 1996/08/15 00:00
MHDA- 1996/08/15 00:01
CRDT- 1996/08/15 00:00
PHST- 1996/08/15 00:00 [pubmed]
PHST- 1996/08/15 00:01 [medline]
PHST- 1996/08/15 00:00 [entrez]
AID - 10.1007/BF01923995 [doi]
PST - ppublish
SO  - Experientia. 1996 Aug 15;52(8):812-7. doi: 10.1007/BF01923995.