Porcupine inhibitors: Novel and emerging anti-cancer therapeutics targeting the Wnt signaling pathway

Wnt signaling in cancer: therapeutic targeting of Wnt signaling beyond β-catenin and the destruction complex

(2020) Youn-Sang Jung et al.   EXPERIMENTAL AND MOLECULAR MEDICINE

Utilizing porcupine (PORCN) and DKK1 inhibition to improve anti-tumor immunity in a murine model of ovarian cancer.

(2020) Jaclyn Wall et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the β-catenin signaling for cancer therapy

(2020) Xue Zhang et al.   PHARMACOLOGICAL RESEARCH

Wnt Signaling Drives Prostate Cancer Bone Metastatic Tropism and Invasion

(2020) Yugang Wang et al.   Translational Oncology

Triazole-Based Inhibitors of the Wnt/β-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice

(2019) Obinna N. Obianom et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Development of Wnt Signaling Pathway Inhibitors for Cancer Therapeutics

(2019) Jerry Harb et al.   Current Oncology Reports

Modulating Wnt signaling at the root: Porcupine and Wnt acylation

(2019) Viviana I. Torres et al.   PHARMACOLOGY & THERAPEUTICS

The effects of Wnt inhibition on tumor progression and the tumor microenvironment in a syngeneic mouse model of ovarian cancer.

(2019) Whitney Goldsberry et al.   JOURNAL OF CLINICAL ONCOLOGY

Inhibition of CBP/β-catenin and porcupine attenuates Wnt signaling and induces apoptosis in head and neck carcinoma cells

(2019) Robert Kleszcz et al.   CELLULAR ONCOLOGY

A Review of the Role of Wnt in Cancer Immunomodulation

(2019) Whitney N. Goldsberry et al.   Cancers

Small molecules from natural products targeting the Wnt/β-catenin pathway as a therapeutic strategy

(2019) Dan Liu et al.   BIOMEDICINE & PHARMACOTHERAPY

PORCN inhibition synergizes with PI3K/mTOR inhibition in Wnt-addicted cancers

(2019) Zheng Zhong et al.   ONCOGENE

Current Advance of Therapeutic Agents in Clinical Trials Potentially Targeting Tumor Plasticity

(2019) Xiao-Guang Yang et al.   Frontiers in Oncology

Mutation Spectrum of Cancer-Associated Genes in Patients With Early Onset of Colorectal Cancer

(2019) Gulnur Zhunussova et al.   Frontiers in Oncology

Pharmacological interventions targeting Wnt/β-catenin signaling pathway attenuate paclitaxel-induced peripheral neuropathy

(2019) Kahkashan Resham et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Wnt signaling pathways in myocardial infarction and the therapeutic effects of Wnt pathway inhibitors

(2018) Wen-bin Fu et al.   ACTA PHARMACOLOGICA SINICA

Targeting WNT signaling in the treatment of osteoporosis

(2018) Roland Baron et al.   CURRENT OPINION IN PHARMACOLOGY

A Novel PORCN Frameshift Mutation Leading to Focal Dermal Hypoplasia: A Case Report

(2018) Ceren D. Durmaz et al.   CYTOGENETIC AND GENOME RESEARCH

Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor

(2018) Haikuo Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Itraconazole targets cell cycle heterogeneity in colorectal cancer

(2018) Simon J.A. Buczacki et al.   JOURNAL OF EXPERIMENTAL MEDICINE

A novel porcupine inhibitor blocks WNT pathways and attenuates cardiac hypertrophy

(2018) Jiahui Jiang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Identification of RSPO2 Fusion Mutations and Target Therapy Using a Porcupine Inhibitor

(2018) Chong Li et al.   Scientific Reports

Activating Wnt/β-catenin signaling pathway for disease therapy: Challenges and opportunities

(2018) Piao Huang et al.   PHARMACOLOGY & THERAPEUTICS

Therapeutic potential of targeting the Wnt/β-catenin signaling pathway in colorectal cancer

(2018) Xiaofei Cheng et al.   BIOMEDICINE & PHARMACOTHERAPY

Therapeutic Potential of Targeting Wnt/β-Catenin Pathway in Treatment of Colorectal Cancer: Rational and Progress

(2017) Afsane Bahrami et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors

(2017) Soo Yei Ho et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Wnt-producing niche drives proliferative potential and progression in lung adenocarcinoma

(2017) Tuomas Tammela et al.   NATURE

Modulating the wnt signaling pathway with small molecules

(2017) Freddi Huan Tran et al.   PROTEIN SCIENCE

Inhibition of porcupine prolongs metastasis free survival in a mouse xenograft model of Ewing sarcoma

(2017) Masanori Hayashi et al.   Oncotarget

Recent developments in the treatment of metastatic colorectal cancer

(2017) Jonathan M. Loree et al.   Therapeutic Advances in Medical Oncology

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

Genetically engineered mouse models to evaluate the role of Wnt secretion in bone development and homeostasis

(2016) Bart O. Williams   AMERICAN JOURNAL OF MEDICAL GENETICS PART C-SEMINARS IN MEDICAL GENETICS

Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold

(2016) Zhixiang Xu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of a triazole class of highly potent Porcn inhibitors

(2016) Lin You et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system

(2016) Zhixiang Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Developing drugs that target the Wnt pathway: recent approaches in cancer and neurodegenerative diseases

(2016) Annalucia Serafino et al.   Expert Opinion on Drug Discovery

Wnt signaling in cancer

(2016) T Zhan et al.   ONCOGENE

Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors

(2016) Dai Cheng et al.   ACS Medicinal Chemistry Letters

Wnt Ligands Secreted by Subepithelial Mesenchymal Cells Are Essential for the Survival of Intestinal Stem Cells and Gut Homeostasis

(2016) Tomas Valenta et al.   Cell Reports

Wnt Signaling in Renal Cell Carcinoma

(2016) Qi Xu et al.   Cancers

Wnt Signaling in Cancer Stem Cell Biology

(2016) Felipe de Sousa e Melo et al.   Cancers

Targeting Wnt signaling in colorectal cancer. A Review in the Theme: Cell Signaling: Proteins, Pathways and Mechanisms

(2015) Laura Novellasdemunt et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors

(2015) Yan Dong et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The use of porcupine inhibitors to target Wnt-driven cancers

(2015) Soo Yei Ho et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Prospective Derivation of a Living Organoid Biobank of Colorectal Cancer Patients

(2015) Marc van de Wetering et al.   CELL

Targeting the Wnt signaling pathway in colorectal cancer

(2015) Masaaki Sawa et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Discovery and Optimization of a Porcupine Inhibitor

(2015) Athisayamani Jeyaraj Duraiswamy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Wnts at the Source--New Mechanisms, New Biomarkers, New Drugs

(2015) B. Madan et al.   MOLECULAR CANCER THERAPEUTICS

Wnt addiction of genetically defined cancers reversed by PORCN inhibition

(2015) B Madan et al.   ONCOGENE

Therapeutic targets in the Wnt signaling pathway: Feasibility of targeting TNIK in colorectal cancer

(2015) Mari Masuda et al.   PHARMACOLOGY & THERAPEUTICS

Porcupine inhibitor suppresses paracrine Wnt-driven growth ofRnf43;Znrf3-mutant neoplasia

(2015) Bon-Kyoung Koo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CRISPR/CAS9-Mediated Genome Editing of miRNA-155 Inhibits Proinflammatory Cytokine Production by RAW264.7 Cells

(2015) Weixia Jing et al.   Biomed Research International

Wnt signaling and osteoporosis

(2014) Stavros C. Manolagas   MATURITAS

RNF43 is frequently mutated in colorectal and endometrial cancers

(2014) Marios Giannakis et al.   NATURE GENETICS

Can we safely target the WNT pathway?

(2014) Michael Kahn   NATURE REVIEWS DRUG DISCOVERY

The Development of Highly Potent Inhibitors for Porcupine

(2013) Xiaolei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Wnt Signaling Pathway in Non-Small Cell Lung Cancer

(2013) D. J. Stewart   JNCI-Journal of the National Cancer Institute

Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma

(2013) X. Jiang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974

(2013) J. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of the Wnt palmitoyltransferase porcupine suppresses cell growth and downregulates the Wnt/β-catenin pathway in gastric cancer

(2013) MIN-LI MO et al.   Oncology Letters

Functional Genomic Studies: Insights into the Pathogenesis of Liver Cancer

(2012) Ze-Guang Han   Annual Review of Genomics and Human Genetics

Pharmacological Inhibition of the Wnt Acyltransferase PORCN Prevents Growth of WNT-Driven Mammary Cancer

(2012) K. D. Proffitt et al.   CANCER RESEARCH

Wnt/beta-Catenin Signaling and Small Molecule Inhibitors

(2012) Andrey Voronkov et al.   CURRENT PHARMACEUTICAL DESIGN

Drugging Wnt signalling in cancer

(2012) Paul Polakis   EMBO JOURNAL

Recurrent R-spondin fusions in colon cancer

(2012) Somasekar Seshagiri et al.   NATURE

Tumour suppressor RNF43 is a stem-cell E3 ligase that induces endocytosis of Wnt receptors

(2012) Bon-Kyoung Koo et al.   NATURE

The Unusual Case of Porcupine

(2012) L. Lum et al.   SCIENCE

WNT secretion and signalling in human disease

(2012) Patrick Herr et al.   TRENDS IN MOLECULAR MEDICINE

Wnt Proteins

(2012) K. Willert et al.   Cold Spring Harbor Perspectives in Biology

Wnt Signaling in Bone Development and Disease: Making Stronger Bone with Wnts

(2012) J. B. Regard et al.   Cold Spring Harbor Perspectives in Biology

A review of the evidence for the canonical Wnt pathway in autism spectrum disorders

(2012) Hans Kalkman   Molecular Autism

Role of the Wnt Pathway in Thyroid Cancer

(2012) Ana Sastre-Perona et al.   Frontiers in Endocrinology

Drugging the Cancer Stem Cell Compartment: Lessons Learned from the Hedgehog and Wnt Signal Transduction Pathways

(2011) Michael E. Dodge et al.   Annual Review of Pharmacology and Toxicology

Embryonic stem cells require Wnt proteins to prevent differentiation to epiblast stem cells

(2011) Derk ten Berge et al.   NATURE CELL BIOLOGY

Modulation of aberrant CDK5 signaling rescues impaired neurogenesis in models of Alzheimer's disease

(2011) L Crews et al.   Cell Death & Disease

Gene Expression Analysis of Macrophages That Facilitate Tumor Invasion Supports a Role for Wnt-Signaling in Mediating Their Activity in Primary Mammary Tumors

(2009) L. S. Ojalvo et al.   JOURNAL OF IMMUNOLOGY

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen et al.   Nature Chemical Biology

Wnt Signaling Is Regulated by Endoplasmic Reticulum Retention

(2009) J. Susie Zoltewicz et al.   PLoS One

Oral benfotiamine plus α-lipoic acid normalises complication-causing pathways in type 1 diabetes

(2008) X. Du et al.   DIABETOLOGIA

Wnt signaling: relevance to β-cell biology and diabetes

(2008) Hannah J. Welters et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Wnt signaling in ovarian tumorigenesis

(2007) T.A. GATCLIFFE et al.   INTERNATIONAL JOURNAL OF GYNECOLOGICAL CANCER