The biology and inhibition of glucose‐regulated protein 94/gp96

The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with pan-Hsp90 Inhibition

(2021) Sanket J. Mishra et al.   JOURNAL OF MEDICINAL CHEMISTRY

The HSP GRP94 interacts with macrophage intracellular complement C3 and impacts M2 profile during ER stress

(2021) Killian Chaumonnot et al.   Cell Death & Disease

Selective Inhibition of the Hsp90a isoform

(2021) Brian Blagg et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cell Surface GRP94 as a Novel Emerging Therapeutic Target for Monoclonal Antibody Cancer Therapy

(2021) Ji Woong Kim et al.   Cells

The glucose-regulated protein GRP94 interacts avidly in the endoplasmic reticulum with sucrase-isomaltase isoforms that are associated with congenital sucrase-isomaltase deficiency

(2021) Abdullah Hoter et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Secretion of a low‐molecular‐weight species of endogenous GRP94 devoid of the KDEL motif during endoplasmic reticulum stress in Chinese hamster ovary cells

(2021) Andrew Samy et al.   TRAFFIC

Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity

(2021) Sujae Yang et al.   ACS Medicinal Chemistry Letters

Endoplasmic Reticulum Chaperones in Viral Infection: Therapeutic Perspectives

(2021) Evelyne Kohli et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

The GRP94 Inhibitor PU-WS13 Decreases M2-like Macrophages in Murine TNBC Tumors: A Pharmaco-Imaging Study with 99mTc-Tilmanocept SPECT

(2021) Alexanne Bouchard et al.   Cells

Endoplasmic reticulum stress promotes inflammation-mediated proteolytic activity at the ocular surface

(2020) Ashley M. Woodward et al.   Scientific Reports

Overexpression of molecule GRP94 favors tumor progression in lung adenocarcinoma by interaction with regulatory T cells

(2020) Xiao‐Feng Duan et al.   Thoracic Cancer

Molecular Stressors Engender Protein Connectivity Dysfunction through Aberrant N-Glycosylation of a Chaperone

(2020) Pengrong Yan et al.   Cell Reports

GARP Dampens Cancer Immunity by Sustaining Function and Accumulation of Regulatory T Cells in the Colon

(2019) Mohammad Salem et al.   CANCER RESEARCH

A peptide-based inhibitor of gp96 suppresses HBsAg expression and HBV replication by upregulation of p53

(2019) Liyuan Qian et al.   JOURNAL OF GENERAL VIROLOGY

Small molecule grp94 inhibitors block dengue and Zika virus replication

(2019) Hussin A. Rothan et al.   ANTIVIRAL RESEARCH

NECA derivatives exploit the paralog-specific properties of the site 3 side pocket of Grp94, the endoplasmic reticulum Hsp90

(2019) John D. Huck et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

GRP94 promotes brain metastasis by engaging pro-survival autophagy

(2019) Naiara Santana-Codina et al.   NEURO-ONCOLOGY

GM2-GM3 gangliosides ratio is dependent on GRP94 through down-regulation of GM2-AP cofactor in brain metastasis cells

(2019) Carmen Bedia et al.   Scientific Reports

Antibody-Based Targeting of Cell Surface GRP94 Specifically Inhibits Cetuximab-Resistant Colorectal Cancer Growth

(2019) Mee Hyun Jeoung et al.   Biomolecules

Trifunctional High-Throughput Screen Identifies Promising Scaffold To Inhibit Grp94 and Treat Myocilin-Associated Glaucoma

(2018) Dustin J. E. Huard et al.   ACS Chemical Biology

Glucose-regulated protein of 94 kDa contributes to the development of an aggressive phenotype in breast cancer cells

(2018) Pedro Buc Calderon et al.   BIOMEDICINE & PHARMACOTHERAPY

Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding

(2018) Nanette L. S. Que et al.   JOURNAL OF MEDICINAL CHEMISTRY

HSP90 inhibitors disrupt a transient HSP90-HSF1 interaction and identify a noncanonical model of HSP90-mediated HSF1 regulation

(2018) Toshiki Kijima et al.   Scientific Reports

TRAP1 Regulation of Cancer Metabolism: Dual Role as Oncogene or Tumor Suppressor

(2018) Danilo Matassa et al.   Genes

The HSP90 Family: Structure, Regulation, Function, and Implications in Health and Disease

(2018) Abdullah Hoter et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cutting Edge: The Heat Shock Protein gp96 Activates Inflammasome-Signaling Platforms in APCs

(2018) Yifei Wang et al.   JOURNAL OF IMMUNOLOGY

Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis

(2018) Fen Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Resorcinol-Based Grp94-Selective Inhibitors

(2017) Anuj Khandelwal et al.   ACS Medicinal Chemistry Letters

Structural and Functional Analysis of GRP94 in the Closed State Reveals an Essential Role for the Pre-N Domain and a Potential Client-Binding Site

(2017) John D. Huck et al.   Cell Reports

Isoform-selective Hsp90 inhibition rescues model of hereditary open-angle glaucoma

(2017) Andrew R. Stothert et al.   Scientific Reports

Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold

(2016) Sanket J. Mishra et al.   ACS Chemical Biology

Surface Expression of TGFβ Docking Receptor GARP Promotes Oncogenesis and Immune Tolerance in Breast Cancer

(2016) Alessandra Metelli et al.   CANCER RESEARCH

Inhibition of Heat Shock Protein 90 Prevents HIV Rebound

(2016) Pheroze Joshi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide Scaffold

(2016) Vincent M. Crowley et al.   JOURNAL OF MEDICINAL CHEMISTRY

The epichaperome is an integrated chaperome network that facilitates tumour survival

(2016) Anna Rodina et al.   NATURE

Marked enhancement of lysosomal targeting and efficacy of ErbB2-targeted drug delivery by HSP90 inhibition

(2016) Srikumar M. Raja et al.   Oncotarget

Gp96-Ig/Costimulator (OX40L, ICOSL, or 4-1BBL) Combination Vaccine Improves T-cell Priming and Enhances Immunity, Memory, and Tumor Elimination

(2016) G. Fromm et al.   Cancer Immunology Research

Immunogenicity of multi-epitope-based vaccine candidates administered with the adjuvant Gp96 against rabies

(2016) Yange Niu et al.   VIROLOGICA SINICA

Heat shock protein gp96 decreases p53 stability by regulating Mdm2 E3 ligase activity in liver cancer

(2015) Bo Wu et al.   CANCER LETTERS

Cell membrane gp96 facilitates HER2 dimerization and serves as a novel target in breast cancer

(2015) Xin Li et al.   INTERNATIONAL JOURNAL OF CANCER

GP96 is a GARP chaperone and controls regulatory T cell functions

(2015) Yongliang Zhang et al.   JOURNAL OF CLINICAL INVESTIGATION

High expression of endoplasmic reticulum chaperone grp94 is a novel molecular hallmark of malignant plasma cells in multiple myeloma

(2015) Saurabh Chhabra et al.   Journal of Hematology & Oncology

Structure–Activity Relationship in a Purine-Scaffold Compound Series with Selectivity for the Endoplasmic Reticulum Hsp90 Paralog Grp94

(2015) Hardik J. Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Plasma membrane gp96 enhances invasion and metastatic potential of liver cancer via regulation of uPAR

(2015) Junwei Hou et al.   Molecular Oncology

Blockage of Conformational Changes of Heat Shock Protein gp96 on Cell Membrane by a α-Helix Peptide Inhibits HER2 Dimerization and Signaling in Breast Cancer

(2015) Xin Li et al.   PLoS One

Glucose-regulated protein 94 is a novel glioma biomarker and promotes the aggressiveness of glioma via Wnt/β-catenin signaling pathway

(2015) Tieyi Hu et al.   TUMOR BIOLOGY

Glucose-regulated protein 94 mediates metastasis by CCT8 and the JNK pathway in hepatocellular carcinoma

(2015) Po-Li Wei et al.   TUMOR BIOLOGY

Glucose-regulated protein 94 mediates cancer progression via AKT and eNOS in hepatocellular carcinoma

(2015) Chien-Yu Huang et al.   TUMOR BIOLOGY

FN14 and GRP94 expression are prognostic/predictive biomarkers of brain metastasis outcome that open up new therapeutic strategies

(2015) Antonio Martínez-Aranda et al.   Oncotarget

Proteomic Investigation on Grp94-IgG Complexes Circulating in Plasma of Type 1 Diabetic Subjects

(2015) Antonella Roveri et al.   Journal of Diabetes Research

Enhancement of HCV polytope DNA vaccine efficacy by fusion to an N-terminal fragment of heat shock protein gp96

(2014) Leila Pishraft-Sabet et al.   ARCHIVES OF VIROLOGY

Chemo-immunotherapy using saffron and its ingredients followed by E7-NT (gp96) DNA vaccine generates different anti-tumor effects against tumors expressing the E7 protein of human papillomavirus

(2014) Afshin Khavari et al.   ARCHIVES OF VIROLOGY

Development of radamide analogs as Grp94 inhibitors

(2014) Aaron Muth et al.   BIOORGANIC & MEDICINAL CHEMISTRY

MZB1 is a GRP94 cochaperone that enables proper immunoglobulin heavy chain biosynthesis upon ER stress

(2014) M. Rosenbaum et al.   GENES & DEVELOPMENT

Exploiting the interaction between Grp94 and aggregated myocilin to treat glaucoma

(2014) Andrew R. Stothert et al.   HUMAN MOLECULAR GENETICS

GP96 Interacts with HHV-6 during Viral Entry and Directs It for Cellular Degradation

(2014) Bhupesh K. Prusty et al.   PLoS One

Heat shock protein gp96 adjuvant induces T cell responses and cross-protection to a split influenza vaccine

(2014) Ying Ju et al.   VACCINE

Decreased functional expression of Grp78 and Grp94 inhibits proliferation and attenuates apoptosis in a human gastric cancer cell line in vitro

(2014) XINCHEN ZHANG et al.   Oncology Letters

ER stress-induced cell death mechanisms

(2013) Renata Sano et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Immune Chaperone gp96 Drives the Contributions of Macrophages to Inflammatory Colon Tumorigenesis

(2013) Crystal Morales et al.   CANCER RESEARCH

Molecular Chaperone gp96 Is a Novel Therapeutic Target of Multiple Myeloma

(2013) Y. Hua et al.   CLINICAL CANCER RESEARCH

Involvement of ER-α36 in the malignant growth of gastric carcinoma cells is associated with GRP94 overexpression

(2013) Zhengqi Fu et al.   HISTOPATHOLOGY

α7 Helix Region of αI Domain Is Crucial for Integrin Binding to Endoplasmic Reticulum Chaperone gp96

(2013) Feng Hong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Inhibition of N-terminal ATPase on HSP90 attenuates colitis through enhanced Treg function

(2013) C B Collins et al.   Mucosal Immunology

Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2

(2013) Pallav D Patel et al.   Nature Chemical Biology

Increased Expression of Gp96 by HBx-Induced NF-κB Activation Feedback Enhances Hepatitis B Virus Production

(2013) Hongxia Fan et al.   PLoS One

Essential roles of grp94 in gut homeostasis via chaperoning canonical Wnt pathway

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

Placenta-derived gp96 as a multivalent prophylactic cancer vaccine

(2013) Bao Zhao et al.   Scientific Reports

Glycoprotein 96 perpetuates the persistent inflammation of rheumatoid arthritis

(2012) Qi-Quan Huang et al.   ARTHRITIS AND RHEUMATISM

Heat shock protein gp96 regulates Toll-like receptor 9 proteolytic processing and conformational stability

(2012) James C. Brooks et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Role of epidermal growth factor receptor in breast cancer

(2012) Hiroko Masuda et al.   BREAST CANCER RESEARCH AND TREATMENT

Targeting the molecular chaperone heat shock protein 90 (HSP90): Lessons learned and future directions

(2012) David S. Hong et al.   CANCER TREATMENT REVIEWS

Quantitative Analysis of Hsp90-Client Interactions Reveals Principles of Substrate Recognition

(2012) Mikko Taipale et al.   CELL

Individual Patient-Specific Immunity against High-Grade Glioma after Vaccination with Autologous Tumor Derived Peptides Bound to the 96 KD Chaperone Protein

(2012) C. A. Crane et al.   CLINICAL CANCER RESEARCH

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet?

(2012) L. Neckers et al.   CLINICAL CANCER RESEARCH

Deletion of muscle GRP94 impairs both muscle and body growth by inhibiting local IGF production

(2012) Elisabeth R. Barton et al.   FASEB JOURNAL

Glucose-regulated Protein 94 Triage of Mutant Myocilin through Endoplasmic Reticulum-associated Degradation Subverts a More Efficient Autophagic Clearance Mechanism

(2012) Amirthaa Suntharalingam et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Molecular Chaperone gp96/GRP94 Interacts with Toll-like Receptors and Integrins via Its C-terminal Hydrophobic Domain

(2012) Shuang Wu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The hERG Channel Is Dependent upon the Hsp90α Isoform for Maturation and Trafficking

(2012) Laura B. Peterson et al.   MOLECULAR PHARMACEUTICS

Proteomic Analyses Reveal High Expression of Decorin and Endoplasmin (HSP90B1) Are Associated with Breast Cancer Metastasis and Decreased Survival

(2012) Thomas R. Cawthorn et al.   PLoS One

Gp96 enhances the immunogenicity of subunit vaccine of porcine reproductive and respiratory syndrome virus

(2012) Caiwei Chen et al.   VIRUS RESEARCH

GRP94: An HSP90-like protein specialized for protein folding and quality control in the endoplasmic reticulum

(2011) Michal Marzec et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Heat-shock protein gp96/grp94 is an essential chaperone for the platelet glycoprotein Ib-IX-V complex

(2011) M. Staron et al.   BLOOD

Anti-HSP90 autoantibodies in sera of infertile women identify a dominant, conserved epitope EP6 (380-389) of HSP90 beta protein

(2011) Eusebio S Pires et al.   Reproductive Biology and Endocrinology

Heat shock response and insulin-associated neurodegeneration

(2011) Michael J. Urban et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

A combination of Trastuzumab and 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells

(2010) Srikumar M. Raja et al.   CANCER BIOLOGY & THERAPY

Targeted Mutation of the Mouse Grp94 Gene Disrupts Development and Perturbs Endoplasmic Reticulum Stress Signaling

(2010) Changhui Mao et al.   PLoS One

GRP94 in ER quality control and stress responses

(2010) Davide Eletto et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

gp96, an endoplasmic reticulum master chaperone for integrins and Toll-like receptors, selectively regulates early T and B lymphopoiesis

(2009) M. Staron et al.   BLOOD

Different Poses for Ligand and Chaperone in Inhibitor-Bound Hsp90 and GRP94: Implications for Paralog-Specific Drug Design

(2009) Robert M. Immormino et al.   JOURNAL OF MOLECULAR BIOLOGY

The Chaperone Activity of GRP94 Toward Insulin-like Growth Factor II Is Necessary for the Stress Response to Serum Deprivation

(2009) Olga Ostrovsky et al.   MOLECULAR BIOLOGY OF THE CELL

GARP (LRRC32) is essential for the surface expression of latent TGF-  on platelets and activated FOXP3+ regulatory T cells

(2009) D. Q. Tran et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Grp94, the endoplasmic reticulum Hsp90, has a similar solution conformation to cytosolic Hsp90 in the absence of nucleotide

(2009) Kristin A. Krukenberg et al.   PROTEIN SCIENCE

Endoplasmic reticulum HSP90b1 (gp96, grp94) optimizes B-cell function via chaperoning integrin and TLR but not immunoglobulin

(2008) B. Liu et al.   BLOOD

Overexpressed cyclophilin B suppresses apoptosis associated with ROS and Ca2+ homeostasis after ER stress

(2008) J. Kim et al.   JOURNAL OF CELL SCIENCE