Protein-Targeted Degradation Agents Based on Natural Products

Discovery of Pentacyclic Triterpenoid PROTACs as a Class of Effective Hemagglutinin Protein Degraders

(2022) Haiwei Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

PROTAC technology as a novel tool to identify the target of lathyrane diterpenoids

(2022) Yanli Wu et al.   Acta Pharmaceutica Sinica B

Atypical E3 ligase ZFP91 promotes small-molecule-induced E2F2 transcription factor degradation for cancer therapy

(2022) Ting-Ting Liu et al.   EBioMedicine

Coumarin-1,2,3-triazole Hybrid Molecules: An Emerging Scaffold for Combating Drug Resistance

(2021) Harish C. Upadhyay   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Cancer Selective Target Degradation by Folate-Caged PROTACs

(2021) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design and linkage optimization of ursane-thalidomide-based PROTACs and identification of their targeted-degradation properties to MDM2 protein

(2021) Zhiwen Qi et al.   BIOORGANIC CHEMISTRY

Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries

(2021) Bo Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP

(2021) Mengzhu Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

The prostate cancer drug market

(2021) Carolina do Pazo et al.   NATURE REVIEWS DRUG DISCOVERY

Attenuation of NLRP3 Inflammasome Activation by Indirubin-Derived PROTAC Targeting HDAC6

(2021) Zhuoxian Cao et al.   ACS Chemical Biology

Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase

(2020) Mei-Xin Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Unifying principles of bifunctional, proximity-inducing small molecules

(2020) Christopher J. Gerry et al.   Nature Chemical Biology

Exploiting the folate receptor α in oncology

(2020) Mariana Scaranti et al.   Nature Reviews Clinical Oncology

A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL

(2020) Bingqi Tong et al.   ACS Chemical Biology

Targeting Estrogen Receptor α for degradation with PROTACs: A Promising Approach to Overcome Endocrine Resistance

(2020) Xin Lin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

Manumycin polyketides act as molecular glues between UBR7 and P53

(2020) Yosuke Isobe et al.   Nature Chemical Biology

A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer

(2020) Hongwei Liao et al.   Cell Discovery

Wogonin Ameliorates Renal Inflammation and Fibrosis by Inhibiting NF-κB and TGF-β1/Smad3 Signaling Pathways in Diabetic Nephropathy

(2020) Zhi-chao Zheng et al.   Drug Design Development and Therapy

A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo

(2020) Lijie Zhao et al.   NEOPLASIA

PROTACs: New method to degrade transcription regulating proteins

(2020) Beichen Hu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

(2020) Guoshun Luo et al.   Acta Pharmaceutica Sinica B

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

Derivation of Rapamycin: Adventures in Natural Product Chemistry

(2019) Sylvain Cottens et al.   CHIMIA

Simple Structural Modifications Converting a Bona Fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

(2019) Jiuling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins

(2019) Nobumichi Ohoka et al.   ACS Chemical Biology

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons

(2018) Lucia Wang et al.   ACS Medicinal Chemistry Letters

Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

(2018) Jinlei Bian et al.   BIOORGANIC CHEMISTRY

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

(2018) John Hines et al.   CANCER RESEARCH

Targeted Degradation of MDM2 as a New Approach to Improve the Efficacy of MDM2-p53 Inhibitors

(2018) Ryan P. Wurz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a potent HMG-CoA reductase degrader that eliminates statin-induced reductase accumulation and lowers cholesterol

(2018) Shi-You Jiang et al.   Nature Communications

Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro

(2017) Jubo Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Spirooxindoles: Promising scaffolds for anticancer agents

(2015) Bin Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

CRABP1 is associated with a poor prognosis in breast cancer: adding to the complexity of breast cancer cell response to retinoic acid

(2015) Rong-Zong Liu et al.   Molecular Cancer

Targeted therapy for advanced gastric cancer: A review of current status and future prospects

(2015) Ozkan Kanat et al.   World Journal of Gastrointestinal Oncology

Design of Chemically Stable, Potent, and Efficacious MDM2 Inhibitors That Exploit the Retro-Mannich Ring-Opening-Cyclization Reaction Mechanism in Spiro-oxindoles

(2014) Angelo Aguilar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expression and clinical significance of CRABP1 and CRABP2 in non-small cell lung cancer

(2014) Irina Favorskaya et al.   TUMOR BIOLOGY

Drug Resistance to Molecular Targeted Therapy and Its Consequences for Treatment Decisions in Non-Small-Cell Lung Cancer

(2014) Johanna N. Spaans et al.   Frontiers in Oncology

Natural products as leads to antitumor drugs

(2013) David J. Newman et al.   PHYTOCHEMISTRY REVIEWS

Targeting protein–protein interactions as an anticancer strategy

(2013) Andrei A. Ivanov et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma

(2011) Karen M VanderMolen et al.   JOURNAL OF ANTIBIOTICS

Jostling for Position: Optimizing Linker Location in the Design of Estrogen Receptor-Targeting PROTACs

(2010) Kedra Cyrus et al.   ChemMedChem

Influence of Cellular ERα/ERβ Ratio on the ERα-Agonist Induced Proliferation of Human T47D Breast Cancer Cells

(2008) Ana Maria Sotoca Covaleda et al.   TOXICOLOGICAL SCIENCES