Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Jianming Lu; Zhiqiang Ma; Jen Chieh Hsieh; Chih Wei Fan; Baozhi Chen; Jamie C. Longgood; Noelle S. Williams; James F. Amatruda; Lawrence Lum; Chuo Chen

doi:10.1016/j.bmcl.2009.04.040

Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Jianming Lu, Zhiqiang Ma, Jen Chieh Hsieh, Chih Wei Fan, Baozhi Chen, Jamie C. Longgood, Noelle S. Williams, James F. Amatruda, Lawrence Lum, Chuo Chen

Research output: Contribution to journal › Article › peer-review

118 Scopus citations

Abstract

Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

Original language	English (US)
Pages (from-to)	3825-3827
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2009.04.040
State	Published - Jul 15 2009

Keywords

IWR
Inhibitor
SAR
Wnt

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2009.04.040

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title = "Structure-activity relationship studies of small-molecule inhibitors of Wnt response",

abstract = "Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.",

keywords = "IWR, Inhibitor, SAR, Wnt",

author = "Jianming Lu and Zhiqiang Ma and Hsieh, {Jen Chieh} and Fan, {Chih Wei} and Baozhi Chen and Longgood, {Jamie C.} and Williams, {Noelle S.} and Amatruda, {James F.} and Lawrence Lum and Chuo Chen",

note = "Funding Information: We thank UT Southwestern Medical Center, NIH (NCI P01-CA095471, NIGMS R01-GM079554, NIGMS R01-GM076398), American Cancer Society (RSG GMC-112251) and Welch Foundation (I-1596, I-1665) for financial support. L.L. is a Virginia Murchison Linthicum Scholar in Medical Research and C.C. is a Southwestern Medical Foundation Scholar in Biomedical Research. We thank Michael Dodge for critical reading of this Letter.",

year = "2009",

month = jul,

day = "15",

doi = "10.1016/j.bmcl.2009.04.040",

language = "English (US)",

volume = "19",

pages = "3825--3827",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "14",

}

TY - JOUR

T1 - Structure-activity relationship studies of small-molecule inhibitors of Wnt response

AU - Lu, Jianming

AU - Ma, Zhiqiang

AU - Hsieh, Jen Chieh

AU - Fan, Chih Wei

AU - Chen, Baozhi

AU - Longgood, Jamie C.

AU - Williams, Noelle S.

AU - Amatruda, James F.

AU - Lum, Lawrence

AU - Chen, Chuo

N1 - Funding Information: We thank UT Southwestern Medical Center, NIH (NCI P01-CA095471, NIGMS R01-GM079554, NIGMS R01-GM076398), American Cancer Society (RSG GMC-112251) and Welch Foundation (I-1596, I-1665) for financial support. L.L. is a Virginia Murchison Linthicum Scholar in Medical Research and C.C. is a Southwestern Medical Foundation Scholar in Biomedical Research. We thank Michael Dodge for critical reading of this Letter.

PY - 2009/7/15

Y1 - 2009/7/15

N2 - Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

AB - Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

KW - IWR

KW - Inhibitor

KW - SAR

KW - Wnt

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U2 - 10.1016/j.bmcl.2009.04.040

DO - 10.1016/j.bmcl.2009.04.040

M3 - Article

C2 - 19410457

AN - SCOPUS:67649651945

SN - 0960-894X

VL - 19

SP - 3825

EP - 3827

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 14

ER -

Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Abstract

Keywords

ASJC Scopus subject areas

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