PMID- 10504731
OWN - NLM
STAT- MEDLINE
DCOM- 19991027
LR  - 20181201
IS  - 1072-8368 (Print)
IS  - 1072-8368 (Linking)
VI  - 6
IP  - 10
DP  - 1999 Oct
TI  - Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial 
      libraries of non-natural binding elements.
PG  - 953-60
AB  - The trimeric, alpha-helical coiled-coil core of the HIV-1 gp41 ectodomain is
      thought to be part of a transient, receptor-triggered intermediate in the
      refolding of the envelope glycoprotein into a fusion-active conformation. In an
      effort to discover small organic inhibitors that block gp41 activation, we have
      generated a biased combinatorial chemical library of non-natural binding elements
      targeted to the gp41 core. From this library of 61,275 potential ligands, we have
      identified elements that, when covalently attached to a peptide derived from the 
      gp41 outer-layer alpha-helix, contribute to the formation of a stable complex
      with the inner core and to inhibition of gp41-mediated cell fusion.
FAU - Ferrer, M
AU  - Ferrer M
AD  - Department of Molecular and Cellular Biology, Harvard University, 7 Divinity
      Ave., Cambridge, Massachusetts 02138, USA.
FAU - Kapoor, T M
AU  - Kapoor TM
FAU - Strassmaier, T
AU  - Strassmaier T
FAU - Weissenhorn, W
AU  - Weissenhorn W
FAU - Skehel, J J
AU  - Skehel JJ
FAU - Oprian, D
AU  - Oprian D
FAU - Schreiber, S L
AU  - Schreiber SL
FAU - Wiley, D C
AU  - Wiley DC
FAU - Harrison, S C
AU  - Harrison SC
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Nat Struct Biol
JT  - Nature structural biology
JID - 9421566
RN  - 0 (Anti-HIV Agents)
RN  - 0 (HIV Envelope Protein gp41)
RN  - 0 (Ligands)
RN  - 0 (Peptide Fragments)
RN  - 0 (Peptide Library)
RN  - 0 (Recombinant Fusion Proteins)
RN  - 19OWO1T3ZE (Enfuvirtide)
SB  - IM
SB  - X
CIN - Nat Struct Biol. 1999 Oct;6(10):895-6. PMID: 10504715
CIN - Nat Struct Biol. 1999 Oct;6(10):906-8. PMID: 10504719
CIN - Nat Struct Biol. 1999 Nov;6(11):1004. PMID: 10542088
MH  - Amino Acid Sequence
MH  - Anti-HIV Agents/*chemical synthesis/chemistry/metabolism/*pharmacology
MH  - Cell Fusion
MH  - Cell Line
MH  - Combinatorial Chemistry Techniques
MH  - Dose-Response Relationship, Drug
MH  - Drug Design
MH  - Drug Evaluation, Preclinical
MH  - Enfuvirtide
MH  - HIV Envelope Protein gp41/chemistry/*metabolism/pharmacology
MH  - HIV-1/*drug effects/metabolism/physiology
MH  - Humans
MH  - Ligands
MH  - Membrane Fusion/*drug effects
MH  - Models, Molecular
MH  - Molecular Sequence Data
MH  - Peptide Fragments/chemistry/metabolism/pharmacology
MH  - *Peptide Library
MH  - Protein Binding/drug effects
MH  - Protein Structure, Secondary
MH  - Recombinant Fusion Proteins/chemistry/metabolism
EDAT- 1999/10/03 09:00
MHDA- 2001/03/23 10:01
CRDT- 1999/10/03 09:00
PHST- 1999/10/03 09:00 [pubmed]
PHST- 2001/03/23 10:01 [medline]
PHST- 1999/10/03 09:00 [entrez]
AID - 10.1038/13324 [doi]
PST - ppublish
SO  - Nat Struct Biol. 1999 Oct;6(10):953-60. doi: 10.1038/13324.