Modular Biomimetic Strategy Enabled Discovery of Simplified Pseudo-Natural Macrocyclic P-Glycoprotein Inhibitors Capable of Overcoming Multidrug Resistance

Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore

(2022) Amila Agampodi Dewa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Concise Total Synthesis of Dysoxylactam A and a Simplified Analog

(2022) Guan‐Zhou Yang et al.   CHINESE JOURNAL OF CHEMISTRY

Preclinical studies of the triazolo[1,5-a]pyrimidine derivative WS-716 as a highly potent, specific and orally active P-glycoprotein (P-gp) inhibitor

(2022) Sai-Qi Wang et al.   Acta Pharmaceutica Sinica B

Multicomponent coupling and macrocyclization enabled by Rh(III)-catalyzed dual C–H activation: Macrocyclic oxime inhibitor of influenza H1N1

(2022) Hao Wang et al.   Chem

Pseudo Natural Products ‐ Chemical Evolution of Natural Product Structure

(2021) Herbert Waldmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell

(2021) Ya-Sheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor

(2021) Michael P. Smolinski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- and BCRP-Mediated Multidrug Resistance

(2021) Qianqian Qiu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors

(2021) Shuo Yuan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Advances in understanding the role of P-gp in doxorubicin resistance: Molecular pathways, therapeutic strategies, and prospects

(2021) Sepideh Mirzaei et al.   DRUG DISCOVERY TODAY

Targeting multidrug resistance-associated protein 1 (MRP1)-expressing cancers: Beyond pharmacological inhibition

(2021) Kimberley M. Hanssen et al.   DRUG RESISTANCE UPDATES

Principle and design of pseudo-natural products

(2020) George Karageorgis et al.   Nature Chemistry

Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue

(2020) Yao Ma et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pd-Catalyzed Decarboxylative Olefination: Stereoselective Synthesis of Polysubstituted Butadienes and Macrocyclic P-glycoprotein Inhibitors

(2020) Bichao Song et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A modular biomimetic strategy for the synthesis of macrolide P-glycoprotein inhibitors via Rh-catalyzed C-H activation

(2020) Lu Chen et al.   Nature Communications

Gastric cancer

(2020) Elizabeth C Smyth et al.   LANCET

Dysoxylactam A: A Macrocyclolipopeptide Reverses P-Glycoprotein-Mediated Multidrug Resistance in Cancer Cells

(2019) Cui-Ping Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The multi-factorial nature of clinical multidrug resistance in cancer

(2019) Yehuda G. Assaraf et al.   DRUG RESISTANCE UPDATES

Advances in the systemic treatment of triple-negative breast cancer

(2018) J.M. Lebert et al.   Current Oncology

Chemotherapy for hepatocellular carcinoma: current status and future perspectives

(2017) Masafumi Ikeda et al.   JAPANESE JOURNAL OF CLINICAL ONCOLOGY

9-Deazapurines as Broad-Spectrum Inhibitors of the ABC Transport Proteins P-Glycoprotein, Multidrug Resistance-Associated Protein 1, and Breast Cancer Resistance Protein

(2017) Katja Stefan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Toward a Better Understanding of the Complexity of Cancer Drug Resistance

(2016) Michael M. Gottesman et al.   Annual Review of Pharmacology and Toxicology

Structures of the Multidrug Transporter P-glycoprotein Reveal Asymmetric ATP Binding and the Mechanism of Polyspecificity

(2016) Lothar Esser et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure–Activity Relationships and Discovery of Promising MDR Reversal Agents

(2016) Jianyong Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bladder cancer

(2016) Ashish M Kamat et al.   LANCET

The modulation of ABC transporter-mediated multidrug resistance in cancer: A review of the past decade

(2015) Rishil J. Kathawala et al.   DRUG RESISTANCE UPDATES

Diversity-Oriented Synthesis of Drug-Like Macrocyclic Scaffolds Using an Orthogonal Organo- and Metal Catalysis Strategy

(2014) André Grossmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Multi-drug resistance in cancer chemotherapeutics: Mechanisms and lab approaches

(2014) Qiong Wu et al.   CANCER LETTERS

Structural basis for gating mechanisms of a eukaryotic P-glycoprotein homolog

(2014) A. Kodan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

(2013) Fabrizio Giordanetto et al.   JOURNAL OF MEDICINAL CHEMISTRY

A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling

(2013) Henning S. G. Beckmann et al.   Nature Chemistry

Structures of P-glycoprotein reveal its conformational flexibility and an epitope on the nucleotide-binding domain

(2013) A. B. Ward et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Refined structures of mouse P-glycoprotein

(2013) Jingzhi Li et al.   PROTEIN SCIENCE

Mechanisms and insights into drug resistance in cancer

(2013) Hiba Zahreddine et al.   Frontiers in Pharmacology

Macrocycles in new drug discovery

(2012) Jamie Mallinson et al.   Future Medicinal Chemistry

Crystal structure of the multidrug transporter P-glycoprotein from Caenorhabditis elegans

(2012) Mi Sun Jin et al.   NATURE

Macrocycles Are Great Cycles: Applications, Opportunities, and Challenges of Synthetic Macrocycles in Drug Discovery

(2011) Eric Marsault et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of P-Glycoprotein Reveals a Molecular Basis for Poly-Specific Drug Binding

(2009) S. G. Aller et al.   SCIENCE

The exploration of macrocycles for drug discovery — an underexploited structural class

(2008) Edward M. Driggers et al.   NATURE REVIEWS DRUG DISCOVERY