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List of works by Brian Blagg

3-Arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition

scientific article

3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues.

scientific article

A High-Throughput TNP-ATP Displacement Assay for Screening Inhibitors of ATP-Binding in Bacterial Histidine Kinases ⬇️

scientific article published on November 4, 2010

A Scaffold Merging Approach to Hsp90 C-terminal Inhibition: Synthesis and Evaluation of a Chimeric Library.

scientific article

A library of noviosylated coumarin analogues

scientific article

A new approach for enhancing differential selectivity of drugs to cancer cells

scientific article published on June 2006

A non-toxic Hsp90 inhibitor protects neurons from Abeta-induced toxicity

scientific article published on 17 January 2007

A novel heat shock protein 90 inhibitor potently targets adrenocortical carcinoma tumor suppression

scientific article published on 24 September 2019

A novel heat shock protein inhibitor KU757 with efficacy in lenvatinib-resistant follicular thyroid cancer cells overcomes up-regulated glycolysis in drug-resistant cells in vitro

scientific article published on 24 July 2020

A systematic protocol for the characterization of Hsp90 modulators.

scientific article

A versatile approach toward the ansamycin antibiotics

scientific article published on 01 March 2006

Alternate strategies of Hsp90 modulation for the treatment of cancer and other diseases

scientific article published on January 2009

Alternative approaches to Hsp90 modulation for the treatment of cancer

scientific article published on September 2014

An Isoform-Selective PTP1B Inhibitor Derived from Nitrogen-Atom Augmentation of Radicicol

scientific article published on 18 July 2019

Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects

scientific article published on 10 February 2016

Assay design and development strategies for finding Hsp90 inhibitors and their role in human diseases

scientific article published on 24 November 2020

Biosynthesis of Squalene. Evidence for a Tertiary Cyclopropylcarbinyl Cationic Intermediate in the Rearrangement of Presqualene Diphosphate to Squalene

article

Biotinylated geldanamycin

scientific article

C-Terminal Heat Shock Protein 90 Inhibitor Decreases Hyperglycemia-induced Oxidative Stress and Improves Mitochondrial Bioenergetics in Sensory Neurons ⬇️

scientific article published on March 28, 2012

Catalysis-Enabled Access to Cryptic Geldanamycin Oxides

scientific article published on 9 January 2020

Catalysis-Enabled Access to Cryptic Geldanamycin Oxides

scientific article published on 24 February 2020

Chaperone substrate provides missing link for cancer drug discovery

scientific article published in February 2018

Characterization of a novel novobiocin analogue as a putative C-terminal inhibitor of heat shock protein 90 in prostate cancer cells

scientific article

Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues

scientific article published on 6 May 2010

Compound Ranking Based on a New Mathematical Measure of Effectiveness Using Time Course Data from Cell-Based Assays ⬇️

scientific article published on March 1, 2013

Cruentaren A binds F1F0 ATP synthase to modulate the Hsp90 protein folding machinery

scientific article published on 12 February 2014

Cucurbitacin D Is a Disruptor of the HSP90 Chaperone Machinery

scientific article published on 10 March 2015

Current Status of SUMOylation Inhibitors

scientific article published on 10 August 2020

Cytotoxic small molecule dimers and their inhibitory activity against human breast cancer cells

scientific article

Derrubone, an inhibitor of the Hsp90 protein folding machinery

scientific article

Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface

scientific article published on 23 March 2015

Design, synthesis and biological evaluation of alkylamino biphenylamides as Hsp90 C-terminal inhibitors

scientific article published on 19 November 2016

Design, synthesis and biological evaluation of biphenylamide derivatives as Hsp90 C-terminal inhibitors

scientific article published on 14 October 2014

Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

scientific article

Design, synthesis, and biological evaluation of conformationally constrained cis-amide Hsp90 inhibitors

scientific article published on June 2009

Design, synthesis, and biological evaluation of ring-constrained novobiocin analogues as hsp90 C-terminal inhibitors

scientific article published on 12 December 2014

Design, synthesis, and evaluation of a radicicol and geldanamycin chimera, radamide

scientific article

Design, synthesis, and structure--activity relationships for chimeric inhibitors of Hsp90

scientific article published on 01 September 2006

Development and characterization of a novel C-terminal inhibitor of Hsp90 in androgen dependent and independent prostate cancer cells ⬇️

scientific article published on October 31, 2011

Development and optimization of a useful assay for determining Hsp90's inherent ATPase activity

scientific article

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

scientific article published on 22 March 2016

Development of Noviomimetics as C-Terminal Hsp90 Inhibitors

scientific article

Development of Phenyl Cyclohexylcarboxamides as a Novel Class of Hsp90 C-terminal Inhibitors

scientific article

Development of a Grp94 inhibitor ⬇️

scientific article published on May 29, 2012

Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors

scientific article

Development of noviomimetics that modulate molecular chaperones and manifest neuroprotective effects

scientific article published on 18 October 2017

Development of novobiocin analogues that manifest anti-proliferative activity against several cancer cell lines

scientific article

Development of radamide analogs as Grp94 inhibitors

scientific article

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

scientific article

Discovery of Novel Hsp90 C-Terminal Inhibitors Using 3D-Pharmacophores Derived from Molecular Dynamics Simulations

scientific article published on 20 September 2020

Diverging Novobiocin Anti-Cancer Activity from Neuroprotective Activity through Modification of the Amide Tail

scientific article published on 5 July 2016

E. coli MEP synthase: steady-state kinetic analysis and substrate binding

scientific article

Elucidation of the Hsp90 C-terminal inhibitor binding site

scientific article (publication date: 19 August 2011)

Endoplasmic Reticulum-resident Heat Shock Protein 90 (HSP90) Isoform Glucose-regulated Protein 94 (GRP94) Regulates Cell Polarity and Cancer Cell Migration by Affecting Intracellular Transport

scientific article

Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-proliferative Agents ⬇️

scientific article published on May 9, 2011

Exploiting conformational dynamics in drug discovery: design of C-terminal inhibitors of Hsp90 with improved activities

scientific article published on 15 January 2014

Exploiting polarity and chirality to probe the Hsp90 C-terminus

scientific article published on 13 April 2018

Exploiting the interaction between Grp94 and aggregated myocilin to treat glaucoma

scientific article published on 15 July 2014

From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition

scientific article published on 11 June 2020

Gambogic Acid, a Natural Product Inhibitor of Hsp90 ⬇️

scientific article published on April 12, 2011

Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates Il1a transcription in rat Sertoli cells

scientific journal article

Gedunin inactivates the co-chaperone p23 protein causing cancer cell death by apoptosis

scientific article published on 25 January 2013

Gedunin, a novel hsp90 inhibitor: semisynthesis of derivatives and preliminary structure-activity relationships

scientific article published on 25 September 2008

Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site

scientific article

Glucose-regulated protein 94 triage of mutant myocilin through endoplasmic reticulum-associated degradation subverts a more efficient autophagic clearance mechanism

scientific article

Grp94 Protein Delivers γ-Aminobutyric Acid Type A (GABAA) Receptors to Hrd1 Protein-mediated Endoplasmic Reticulum-associated Degradation.

scientific article published on 4 March 2016

Heat shock protein 70 is necessary to improve mitochondrial bioenergetics and reverse diabetic sensory neuropathy following KU-32 therapy

scientific article

Heat shock response and insulin-associated neurodegeneration ⬇️

scientific article published on December 13, 2011

Hepatitis C Virus NS3 Helicase Inhibitor Discovery

High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding of firefly luciferase

scientific article published on 4 January 2007

High-throughput screen of natural product libraries for hsp90 inhibitors

scientific article

High-throughput screening for Hsp90 ATPase inhibitors

scientific article published on 10 March 2006

Hsp90 C-terminal inhibitors exhibit antimigratory activity by disrupting the Hsp90α/Aha1 complex in PC3-MM2 cells

scientific article

Hsp90 activator Aha1 drives production of pathological tau aggregates

scientific article published on 21 August 2017

Hsp90 as a target for drug development

scientific article published on December 2006

Hsp90 inhibition: elimination of shock and stress

scientific article

Hsp90 inhibitors identified from a library of novobiocin analogues

scientific article published in September 2005

Hsp90 inhibitors: small molecules that transform the Hsp90 protein folding machinery into a catalyst for protein degradation

scientific article

Hsp90 modulation for the treatment of Alzheimer's disease

scientific article published on January 2012

Hsp90: a novel target for the disruption of multiple signaling cascades

scientific article published on June 2007

Hydrating for resistance to radicicol

scientific article published on April 2009

Identification and initial SAR of silybin: An Hsp90 inhibitor ⬇️

scientific article published on December 28, 2010

Identification of a new scaffold for hsp90 C-terminal inhibition

scientific article published on 26 November 2013

Induction of Heat Shock Protein 70 (Hsp70) prevents Neuregulin-Induced Demyelination by Enhancing the Proteasomal Clearance of c-Jun ⬇️

scientific article published on December 6, 2012

Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice

scientific article

Inhibition and function of heat shock proteins 70 and 90.

scientific article published in January 2009

Inhibition of Hsp90 in the spinal cord enhances the antinociceptive effects of morphine by activating an ERK-RSK pathway

scientific article published on 05 May 2020

Intramolecular Diels-Alder and tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition reactions of 1,3,4-oxadiazoles

scientific article published in September 2002

Intramolecular diels-alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles

scientific article published on August 2006

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

scientific article published on 20 December 2017

KU-32, a novel drug for diabetic neuropathy, is safe for human islets and improves in vitro insulin secretion and viability

scientific article

KU-596 decreases mitochondrial superoxide and improves bioenergetics following downregulation of manganese superoxide dismutase in diabetic sensory neurons

scientific article published on 15 December 2018

KU135, a novel novobiocin-derived C-terminal inhibitor of the 90-kDa heat shock protein, exerts potent antiproliferative effects in human leukemic cells

scientific article published on 09 September 2009

KU675, a Concomitant Heat-Shock Protein Inhibitor of Hsp90 and Hsc70 that Manifests Isoform Selectivity for Hsp90α in Prostate Cancer Cells

scientific article published on 4 May 2015

Methods to validate Hsp90 inhibitor specificity, to identify off-target effects, and to rethink approaches for further clinical development

scientific article published in February 2018

Mitochondrial-targeted Hsp90 C-terminal inhibitors manifest anti-proliferative activity

scientific article published on 06 September 2019

Modified biphenyl Hsp90 C-terminal inhibitors for the treatment of cancer

scientific article published on 11 July 2017

Modulating Molecular Chaperones Improves Mitochondrial Bioenergetics and Decreases the Inflammatory Transcriptome in Diabetic Sensory Neurons

scientific article

Modulating molecular chaperones improves sensory fiber recovery and mitochondrial function in diabetic peripheral neuropathy ⬇️

scientific article published on March 20, 2012

Molecular Defects in Cardiac Myofilament Ca2+-Regulation Due to Cardiomyopathy-Linked Mutations Can Be Reversed by Small Molecules Binding to Troponin.

scientific article published on 27 March 2018

Molecular insights into the interaction of Hsp90 with allosteric inhibitors targeting the C-terminal domain

scientific article published on 02 July 2018

Monoenomycin: A Simplified Trienomycin A Analogue That Manifests Anticancer Activity ⬇️

scientific article published on October 13, 2011

Natural Product Inspired N-Terminal Hsp90 Inhibitors: From Bench to Bedside?

scientific article published on 25 May 2015

Natural products and other inhibitors of F1FO ATP synthase

scientific article published on 03 September 2020

Neuroprotective activity and evaluation of Hsp90 inhibitors in an immortalized neuronal cell line

scientific article

Novel C-Terminal Hsp90 Inhibitor for Head and Neck Squamous Cell Cancer (HNSCC) with in vivo Efficacy and Improved Toxicity Profiles Compared with Standard Agents ⬇️

scientific article published on August 12, 2011

Novel C-terminal heat shock protein 90 inhibitors target breast cancer stem cells and block migration, self-renewal, and epithelial-mesenchymal transition

scientific article published on 07 April 2020

Novel HSP90 inhibitors effectively target functions of thyroid cancer stem cell preventing migration and invasion

scientific article

Novobiocin Analogues That Inhibit the MAPK Pathway

scientific article published on 8 January 2016

Novobiocin analogues with second-generation noviose surrogates ⬇️

scientific article published on November 22, 2012

Novobiocin and additional inhibitors of the Hsp90 C-terminal nucleotide-binding pocket

scientific article published on January 2008

Novobiocin: redesigning a DNA gyrase inhibitor for selective inhibition of hsp90.

scientific article

Novologues containing a benzamide side chain manifest anti-proliferative activity against two breast cancer cell lines

scientific article

Optimization of potent hepatitis C virus NS3 helicase inhibitors isolated from the yellow dyes thioflavine S and primuline

scientific article

Pharmacologic dissection of the overlapping impact of heat shock protein family members on platelet function

scientific article published on 05 February 2020

Radanamycin, a macrocyclic chimera of radicicol and geldanamycin

scientific article published on 7 February 2006

Radester, a novel inhibitor of the Hsp90 protein folding machinery

scientific article published on 01 May 2005

Recent advances in medicinal chemistry

scientific article published on 01 May 2011

Recombinant squalene synthase. A mechanism for the rearrangement of presqualene diphosphate to squalene

scientific article

Resorcinol-Based Grp94-Selective Inhibitors

scientific article

Second Generation Grp94-Selective Inhibitors Provide Opportunities for the Inhibition of Metastatic Cancer.

scientific article published on 30 August 2017

Stimulation of heat shock protein 90 chaperone function through binding of a novobiocin analog KU-32

scientific article published on 21 February 2019

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

scientific article published on 12 March 2018

Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor

scientific article published on 30 January 2018

Syntheses of photolabile novobiocin analogues

scientific article published on 01 December 2004

Synthesis and Biological Evaluation of Novobiocin Core Analogues as Hsp90 Inhibitors

scientific article published on April 2016

Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors.

scientific article

Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors

scientific article published on 24 September 2020

Synthesis and Evaluation of Noviose Replacements on Novobiocin That Manifest Antiproliferative Activity ⬇️

scientific article published on July 13, 2010

Synthesis and Evaluation of Novologues as C-Terminal Hsp90 Inhibitors with Cytoprotective Activity against Sensory Neuron Glucotoxicity ⬇️

scientific article published on June 15, 2012

Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors ⬇️

scientific article published on December 1, 2011

Synthesis and biological evaluation of coumarin replacements of novobiocin as Hsp90 inhibitors

scientific article published on 03 January 2014

Synthesis and evaluation of Hsp90 inhibitors that contain the 1,4-naphthoquinone scaffold

scientific article

Synthesis and evaluation of a ring-constrained Hsp90 C-terminal inhibitor that exhibits neuroprotective activity

scientific article published on 26 March 2018

Synthesis and evaluation of coumermycin A1 analogues that inhibit the Hsp90 protein folding machinery

scientific article published on 01 October 2006

Synthesis and evaluation of derrubone and select analogues

scientific article published on 22 December 2007

Synthesis and evaluation of electron-rich curcumin analogues

scientific article published on 29 October 2008

Synthesis and evaluation of radamide analogues, a chimera of radicicol and geldanamycin

scientific article

Synthesis and structure-activity relationships of EGCG analogues, a recently identified Hsp90 inhibitor

scientific article published on August 2013

Synthesis of (-)-noviose from 2,3-O-isopropylidene-D-erythronolactol

scientific article published in October 2004

Synthesis of 1-Deoxy-D-xylulose and 1-Deoxy-D-xylulose-5-phosphate

scientific article published on 01 March 1999

Synthesis of Cruentaren A ⬇️

scientific article published on December 3, 2012

Synthesis of a versatile metacyclophane macrolactam

scientific article published on January 2008

Synthesis of mono- and dihydroxylated furanoses, pyranoses, and an oxepanose for the preparation of natural product analogue libraries

scientific article published in July 2005

Synthesis of paramagnetic ligands that target the C-terminal binding site of Hsp90

scientific article published on 02 June 2020

Targeting Heat Shock Protein 70 to Ameliorate c-Jun Expression and Improve Demyelinating Neuropathy.

scientific article published on 9 November 2017

Targeting the Heat Shock Protein 90 Dimer with Dimeric Inhibitors ⬇️

scientific article published on August 23, 2011

The Alpha Isoform of Heat Shock Protein 90 and the Co-chaperones p23 and Cdc37 Promote Opioid Anti-nociception in the Brain

scientific article published on 29 November 2019

The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with <i>pan</i>-Hsp90 Inhibition

scientific article published on 11 January 2021

The Right Tool for the Job: An Overview of Hsp90 Inhibitors

scientific article published on 01 January 2020

The design, synthesis, and evaluation of coumarin ring derivatives of the novobiocin scaffold that exhibit antiproliferative activity

scientific article published on 22 October 2008

The hERG channel is dependent upon the Hsp90α isoform for maturation and trafficking ⬇️

scientific article published on May 3, 2012

The role and therapeutic potential of Hsp90, Hsp70, and smaller heat shock proteins in peripheral and central neuropathies

scientific article published on 25 August 2020

The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

scientific article published on 23 April 2019

The synthesis and evaluation of flavone and isoflavone chimeras of novobiocin and derrubone

scientific article

To fold or not to fold: modulation and consequences of Hsp90 inhibition

scientific article

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

scientific article

Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors

scientific article published on September 2014

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

scientific article published on 5 February 2018

Uptake, distribution and diffusivity of reactive fluorophores in cells: implications toward target identification

scientific article published on August 2010

c-Abl Mediated Tyrosine Phosphorylation of Aha1 Activates Its Co-chaperone Function in Cancer Cells

scientific article published on 28 July 2015

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