Drug delivery challenges and formulation aspects of proteolysis targeting chimera (PROTACs)

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Susceptibility of Lung Carcinoma Cells to Nanostructured Lipid Carrier of ARV-825, a BRD4 Degrading Proteolysis Targeting Chimera

(2022) Richa Vartak et al.   PHARMACEUTICAL RESEARCH

A BRD4 PROTAC nanodrug for glioma therapy via the intervention of tumor cells proliferation, apoptosis and M2 macrophages polarization

(2022) Tingting Yang et al.   Acta Pharmaceutica Sinica B

Galactose-decorated liver tumor-specific nanoliposomes incorporating selective BRD4-targeted PROTAC for hepatocellular carcinoma therapy

(2022) Aishwarya Saraswat et al.   Heliyon

Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy

(2022) Jing Gao et al.   Nature Communications

Advances in Oral Drug Delivery

(2021) Mohammed S. Alqahtani et al.   Frontiers in Pharmacology

BRD4 PROTAC degrader ARV-825 inhibits T-cell acute lymphoblastic leukemia by targeting 'Undruggable' Myc-pathway genes

(2021) Shuiyan Wu et al.   Cancer Cell International

Aerosolized nanoliposomal carrier of remdesivir: an effective alternative for COVID-19 treatment in vitro

(2021) Richa Vartak et al.   Nanomedicine

A novel gene therapy for neurodegenerative Lafora disease via EPM2A-loaded DLinDMA lipoplexes

(2021) Hari Priya Vemana et al.   Nanomedicine

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

(2021) Si-Min Qi et al.   Frontiers in Pharmacology

From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation

(2021) Carlotta Cecchini et al.   Frontiers in Chemistry

Development of Dual ARV-825 and Nintedanib-Loaded PEGylated Nano-Liposomes for Synergistic Efficacy in Vemurafnib-Resistant Melanoma

(2021) Yige Fu et al.   Pharmaceutics

Stromal disruption facilitating invasion of a ‘nano-arsenal’ into the solid tumor

(2021) Yige Fu et al.   DRUG DISCOVERY TODAY

Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

(2020) Marı́a Maneiro et al.   ACS Chemical Biology

Targeted degradation of anaplastic lymphoma kinase by gold nanoparticle-based multi-headed proteolysis targeting chimeras

(2020) Yingming Wang et al.   COLLOIDS AND SURFACES B-BIOINTERFACES

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

(2020) Daniel Peter Petrylak et al.   JOURNAL OF CLINICAL ONCOLOGY

PROTAC Technology: Opportunities and Challenges

(2020) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Nanoformulation of PROteolysis TArgeting Chimera targeting ‘undruggable’ c-Myc for the treatment of pancreatic cancer

(2020) Aishwarya Saraswat et al.   Nanomedicine

Nanoformulation of BRD4-Degrading PROTAC: Improving Druggability To Target the ‘Undruggable’ MYC in Pancreatic Cancer

(2020) Tamara Minko   TRENDS IN PHARMACOLOGICAL SCIENCES

Controlled Delivery of BET-PROTACs: In Vitro Evaluation of MZ1-Loaded Polymeric Antibody Conjugated Nanoparticles in Breast Cancer

(2020) Francisco J. Cimas et al.   Pharmaceutics

PROTAC Bromodomain Inhibitor ARV-825 Displays Anti-Tumor Activity in Neuroblastoma by Repressing Expression of MYCN or c-Myc

(2020) Zhiheng Li et al.   Frontiers in Oncology

Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles

(2020) Jinjin Chen et al.   JOURNAL OF CONTROLLED RELEASE

Active Targeting Strategies Using Biological Ligands for Nanoparticle Drug Delivery Systems

(2019) Jihye Yoo et al.   Cancers

PROTACs– a game-changing technology

(2019) Markella Konstantinidou et al.   Expert Opinion on Drug Discovery

BRD4 PROTAC as a novel therapeutic approach for the treatment of vemurafenib resistant melanoma: Preformulation studies, formulation development and in vitro evaluation

(2019) Drishti Rathod et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

(2019) Peter S. Dragovich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development and optimization of stealth liposomal system for enhanced in vitro cytotoxic effect of quercetin

(2019) Aishwarya L. Saraswat et al.   JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

Delivering CRISPR: a review of the challenges and approaches

(2018) Christopher A. Lino et al.   DRUG DELIVERY

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

(2018) Nicola E. A. Chessum et al.   JOURNAL OF MEDICINAL CHEMISTRY

Progress and challenges towards targeted delivery of cancer therapeutics

(2018) Daniel Rosenblum et al.   Nature Communications

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

(2018) Sainan An et al.   EBioMedicine

Non-invasive delivery strategies for biologics

(2018) Aaron C. Anselmo et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted Drug Delivery via Folate Receptors for the Treatment of Brain Cancer: Can the Promise Deliver?

(2017) Jianfeng Guo et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Advances in the delivery of RNA therapeutics: from concept to clinical reality

(2017) James C. Kaczmarek et al.   Genome Medicine

Genetic compensation: A phenomenon in search of mechanisms

(2017) Mohamed A. El-Brolosy et al.   PLoS Genetics

Therapeutic miRNA and siRNA: Moving from Bench to Clinic as Next Generation Medicine

(2017) Chiranjib Chakraborty et al.   Molecular Therapy-Nucleic Acids

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

(2016) Honorine Lebraud et al.   ACS Central Science

Cancer active targeting by nanoparticles: a comprehensive review of literature

(2014) Remon Bazak et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Trends in the exploitation of novel drug targets

(2011) Mathias Rask-Andersen et al.   NATURE REVIEWS DRUG DISCOVERY

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space

(2011) Alexander Alex et al.   MedChemComm

Physicochemical Space for Optimum Oral Bioavailability: Contribution of Human Intestinal Absorption and First-Pass Elimination

(2010) Manthena V. S. Varma et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS