A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
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A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors. / Bang, Claus G.; Jensen, Jakob F.; O'Hanlon Cohrt, Emil; Olsen, Lasse B.; Siyum, Saba G.; Mortensen, Kim T.; Skovgaard, Tine; Berthelsen, Jens; Yang, Liang; Givskov, Michael; Qvortrup, Katrine; Nielsen, Thomas E.
In: ACS Combinatorial Science, Vol. 19, No. 10, 10.2017, p. 657-669.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
AU - Bang, Claus G.
AU - Jensen, Jakob F.
AU - O'Hanlon Cohrt, Emil
AU - Olsen, Lasse B.
AU - Siyum, Saba G.
AU - Mortensen, Kim T.
AU - Skovgaard, Tine
AU - Berthelsen, Jens
AU - Yang, Liang
AU - Givskov, Michael
AU - Qvortrup, Katrine
AU - Nielsen, Thomas E.
PY - 2017/10
Y1 - 2017/10
N2 - We herein present broadly useful, readily available and nonintegral hydroxylamine linkers for the routine solid-phase synthesis of hydroxamic acids. The developed protocols enable the efficient synthesis and release of a wide range of hydroxamic acids from various resins, relying on high control and flexibility with respect to reagents and synthetic processes. A trityl-based hydroxylamine linker was used to synthesize a library of peptide hydroxamic acids. The inhibitory effects of the compounds were examined for seven HDAC enzyme subtypes using a chemiluminescence-based assay.
AB - We herein present broadly useful, readily available and nonintegral hydroxylamine linkers for the routine solid-phase synthesis of hydroxamic acids. The developed protocols enable the efficient synthesis and release of a wide range of hydroxamic acids from various resins, relying on high control and flexibility with respect to reagents and synthetic processes. A trityl-based hydroxylamine linker was used to synthesize a library of peptide hydroxamic acids. The inhibitory effects of the compounds were examined for seven HDAC enzyme subtypes using a chemiluminescence-based assay.
KW - HDAC inhibitor
KW - hydroxamic acid
KW - linker
KW - solid-phase synthesis
U2 - 10.1021/acscombsci.7b00068
DO - 10.1021/acscombsci.7b00068
M3 - Journal article
C2 - 28746804
AN - SCOPUS:85030788051
VL - 19
SP - 657
EP - 669
JO - ACS Combinatorial Science
JF - ACS Combinatorial Science
SN - 2156-8952
IS - 10
ER -
ID: 185035650