Structure-Based Identification of Potent Lysine-Specific Demethylase 1 Inhibitor Peptides and Temporary Cyclization to Enhance Proteolytic Stability and Cell Growth-Inhibitory Activity

Macrocyclic Peptides Uncover a Novel Binding Mode for Reversible Inhibitors of LSD1

(2020) Jie Yang et al.   ACS Omega

Development and Structural Evaluation of N ‐Alkylated trans ‐2‐Phenylcyclopropylamine‐Based LSD1 Inhibitors

(2020) Hideaki Niwa et al.   ChemMedChem

Epigenetic Reexpression of Hemoglobin F Using Reversible LSD1 Inhibitors: Potential Therapies for Sickle Cell Disease

(2020) Steven Holshouser et al.   ACS Omega

Understanding Cell Penetration of Cyclic Peptides

(2019) Patrick G. Dougherty et al.   CHEMICAL REVIEWS

Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP

(2019) Jinjin Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity

(2019) Paul M. Levine et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

(2019) Yuan Fang et al.   Journal of Hematology & Oncology

Advances in oral peptide therapeutics

(2019) Daniel J. Drucker   NATURE REVIEWS DRUG DISCOVERY

Facile Fabrication of 10-Hydroxycamptothecin-Backboned Amphiphilic Polyprodrug with Precisely Tailored Drug Loading Content for Controlled Release

(2018) Xiaolong Zhang et al.   BIOCONJUGATE CHEMISTRY

Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors

(2018) Taeko Kakizawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cyclic peptide inhibitors of lysine-specific demethylase 1 with improved potency identified by alanine scanning mutagenesis

(2018) Isuru R. Kumarasinghe et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Reversible stapling of unprotected peptides via chemoselective methionine bis-alkylation/dealkylation

(2018) Xiaodong Shi et al.   Chemical Science

Eradication of central nervous system leukemia of T-cell origin with a brain-permeable LSD1 inhibitor

(2018) Shiori Saito et al.   CLINICAL CANCER RESEARCH

Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases

(2017) Hideaki Niwa et al.   Epigenetics

Discovery of a Human Neuromedin U Receptor 1-Selective Hexapeptide Agonist with Enhanced Serum Stability

(2017) Kentaro Takayama et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

(2017) Akane Kawamura et al.   Nature Communications

Enhancing the Cell Permeability and Metabolic Stability of Peptidyl Drugs by Reversible Bicyclization

(2016) Ziqing Qian et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Site-Specific Difunctionalization of Structured RNAs Yields Probes for microRNA Maturation

(2016) Ugo Pradère et al.   BIOCONJUGATE CHEMISTRY

Transcriptional Selectivity of Epigenetic Therapy in Cancer

(2016) Takahiro Sato et al.   CANCER RESEARCH

Precise and Reversible Protein-Microtubule-Like Structure with Helicity Driven by Dual Supramolecular Interactions

(2016) Guang Yang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Blurring the Role of Oligonucleotides: Spherical Nucleic Acids as a Drug Delivery Vehicle

(2016) Xuyu Tan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Supramolecular complexes of bambusurils with dialkyl phosphates

(2016) Tomas Fiala et al.   SUPRAMOLECULAR CHEMISTRY

Intracellular Delivery of Peptidyl Ligands by Reversible Cyclization: Discovery of a PDZ Domain Inhibitor that Rescues CFTR Activity

(2015) Ziqing Qian et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes

(2015) Marta Pelay-Gimeno et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

(2015) Helai P. Mohammad et al.   CANCER CELL

Modulating protein–protein interactions: the potential of peptides

(2015) Laura Nevola et al.   CHEMICAL COMMUNICATIONS

Peptide therapeutics: current status and future directions

(2015) Keld Fosgerau et al.   DRUG DISCOVERY TODAY

Organic Carbamates in Drug Design and Medicinal Chemistry

(2015) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

A two-component 'double-click' approach to peptide stapling

(2015) Yu Heng Lau et al.   Nature Protocols

Substrate- and Cofactor-independent Inhibition of Histone Demethylase KDM4C

(2014) Ulrike Leurs et al.   ACS Chemical Biology

Cell-Penetrating Peptides: Design, Synthesis, and Applications

(2014) Dana Maria Copolovici et al.   ACS Nano

Synthesis of a Library of Propargylated and PEGylated α-Hydroxy Acids Toward “Clickable” Polylactides via Hydrolysis of Cyanohydrin Derivatives

(2014) Quanxuan Zhang et al.   JOURNAL OF ORGANIC CHEMISTRY

Protein Recognition by Short Peptide Reversible Inhibitors of the Chromatin-Modifying LSD1/CoREST Lysine Demethylase

(2013) Marcello Tortorici et al.   ACS Chemical Biology

Cell-penetrating peptides: 20 years later, where do we stand?

(2013) Chérine Bechara et al.   FEBS LETTERS

Synthesis and Evaluation of Novel Cyclic Peptide Inhibitors of Lysine-Specific Demethylase 1

(2013) Isuru R. Kumarasinghe et al.   ACS Medicinal Chemistry Letters

Sonication-induced self-assembly of flexible tris(ureidobenzyl)amine: from dimeric aggregates to supramolecular gels

(2012) Chao Deng et al.   CHEMICAL COMMUNICATIONS

Cell-penetrating peptides: classes, origin, and current landscape

(2012) Francesca Milletti   DRUG DISCOVERY TODAY

Azalysine Analogues as Probes for Protein Lysine Deacetylation and Demethylation

(2012) Blair C. R. Dancy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

Overview of theCCP4 suite and current developments

(2011) Martyn D. Winn et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Photocontrol of Peptide Function: Backbone Cyclization Strategy with Photocleavable Amino Acid

(2011) Naoki Umezawa et al.   CHEMBIOCHEM

On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds

(2011) Tina R White et al.   Nature Chemical Biology

Molecular Mimicry and Ligand Recognition in Binding and Catalysis by the Histone Demethylase LSD1-CoREST Complex

(2011) Riccardo Baron et al.   STRUCTURE

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structurally Designedtrans-2-Phenylcyclopropylamine Derivatives Potently Inhibit Histone Demethylase LSD1/KDM1,,§

(2010) Shinya Mimasu et al.   BIOCHEMISTRY

Synthesis and Biological Analysis of Prostate-Specific Membrane Antigen-Targeted Anticancer Prodrugs

(2010) Sumith A. Kularatne et al.   JOURNAL OF MEDICINAL CHEMISTRY

Serum Stabilities of Short Tryptophan- and Arginine-Rich Antimicrobial Peptide Analogs

(2010) Leonard T. Nguyen et al.   PLoS One

Molecular replacement withMOLREP

(2009) Alexei Vagin et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

N-Methylation of Peptides: A New Perspective in Medicinal Chemistry

(2008) Jayanta Chatterjee et al.   ACCOUNTS OF CHEMICAL RESEARCH

Peptide Tertiary Structure Nucleation by Side-Chain Crosslinking with Metal Complexation and Double “Click” Cycloaddition

(2008) Oscar Torres et al.   CHEMBIOCHEM

Fluorescence Imaging of Cellular Glutathione Using a Latent Rhodamine

(2008) Marcos M. Pires et al.   ORGANIC LETTERS

Methodological and cellular aspects that govern the internalization mechanisms of arginine-rich cell-penetrating peptides

(2007) Ikuhiko Nakase et al.   ADVANCED DRUG DELIVERY REVIEWS

Live-cell analysis of cell penetration ability and toxicity of oligo-arginines

(2007) Gisela Tünnemann et al.   JOURNAL OF PEPTIDE SCIENCE