Abstract
A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 μM, and 2, IC50 = 8 μM) to be reported for this class of integrins.
| Original language | English |
|---|---|
| Pages (from-to) | 2297-2302 |
| Number of pages | 6 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 8 |
| Issue number | 17 |
| DOIs | |
| State | Published - Sep 8 1998 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening. / Souers, Andrew J.; Virgilio, Alex A.; Schuerer, Stephan C; Ellman, Jonathan A.; Kogan, Timothy P.; West, Henry E.; Ankener, Wendy; Vanderslice, Peter.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 8, No. 17, 08.09.1998, p. 2297-2302.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Novel inhibitors of α4β1 integrin receptor interactions through library synthesis and screening
AU - Souers, Andrew J.
AU - Virgilio, Alex A.
AU - Schuerer, Stephan C
AU - Ellman, Jonathan A.
AU - Kogan, Timothy P.
AU - West, Henry E.
AU - Ankener, Wendy
AU - Vanderslice, Peter
PY - 1998/9/8
Y1 - 1998/9/8
N2 - A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 μM, and 2, IC50 = 8 μM) to be reported for this class of integrins.
AB - A library of 2302 small molecule β-turn mimetics was screened for inhibition of the α4β1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 μM, and 2, IC50 = 8 μM) to be reported for this class of integrins.
UR - http://www.scopus.com/inward/record.url?scp=0032497423&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032497423&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(98)00416-8
DO - 10.1016/S0960-894X(98)00416-8
M3 - Article
VL - 8
SP - 2297
EP - 2302
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 17
ER -