List of works - Stephen W. Fesik

1H, 13C and 15N resonance assignments of a Bcl-xL/Bad peptide complex

scientific article published on 01 July 2005

A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia.

scientific article

A Strategy for High-Throughput Assay Development Using Leads Derived from Nuclear Magnetic Resonance-Based Screening ⬇️

scientific article published on October 1, 2002

A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation

scientific article

A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A.

scientific article

A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand

scientific article

A robust in vivo positive-readout system for monitoring siRNA delivery to xenograft tumors

scientific article

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo

scientific article published on September 2006

ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

scientific article published on October 2008

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models

scientific article

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

scientific article

BCL-2 AND IAP Proteins As Potential Drug Targets

scientific article published on 09 February 2001

Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization

scientific article

Defining the optimal parameters for hairpin-based knockdown constructs

scientific article published on 13 August 2007

Defining the p53 DNA-binding domain/Bcl-x(L)-binding interface using NMR.

scientific article published in February 2004

Developing lipid nanoparticle-based siRNA therapeutics for hepatocellular carcinoma using an integrated approach

scientific article published on 13 August 2013

Development of a tightly regulated U6 promoter for shRNA expression

scientific article

Diphenylpyrazoles as replication protein a inhibitors

scientific article

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction

scientific article published on 05 December 2019

Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

scientific article published on 28 September 2018

Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core

scientific article published on 07 January 2020

Discovery and Structure−Activity Relationship of Oxalylarylaminobenzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B ⬇️

scientific article (publication date: 22 May 2003)

Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors

scientific article published on 23 November 2016

Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies

scientific article

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo

scientific article published on February 2006

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods

scientific article

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.

scientific article published in June 2018

Discovery of Inhibitors of Protein-Protein Interactions Using Fragment-Based Methods

Discovery of Potent 2-Aryl-6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design

scientific article published on 29 June 2018

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

scientific article

Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer

scientific article published on 16 April 2019

Discovery of Protein–Protein Interaction Inhibitors of Replication Protein A

scientific article

Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS

scientific article published on 08 August 2018

Discovery of Small Molecules that Bind to K‐Ras and Inhibit Sos‐Mediated Activation ⬇️

scientific article published on May 8, 2012

Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design

scientific article published on 09 April 2020

Discovery of a Potent Inhibitor of Replication Protein A Protein–Protein Interactions Using a Fragment-Linking Approach

scientific article

Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A

scientific article

Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR ⬇️

scientific article published on September 15, 2010

Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis

scientific article published in January 2006

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy

scientific article (publication date: 9 April 2003)

Discovery of aminoglycoside mimetics by NMR-based screening of Escherichia coli A-site RNA.

scientific article

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins

scientific article published on 8 October 2008

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer

scientific article published on August 2004

Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design

scientific article

Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity

scientific article published on 01 March 2019

Druggability indices for protein targets derived from NMR-based screening data

scientific article

Drugging an undruggable pocket on KRAS

scientific article published on 22 July 2019

Drugging the undruggable RAS: Mission possible?

scientific article

Evaluating hypoxia-inducible factor-1alpha as a cancer therapeutic target via inducible RNA interference in vivo

scientific article published on August 2005

Fragment-based drug discovery using NMR spectroscopy

scientific article

Fragment-based screening of programmed death ligand 1 (PD-L1)

scientific article published on 24 January 2019

Fragment-based screening of the bromodomain of ATAD2.

scientific article

From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae

scientific article published on 01 June 2007

Growth inhibition and radiosensitization of glioblastoma and lung cancer cells by small interfering RNA silencing of tumor necrosis factor receptor-associated factor 2.

scientific article

Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo

scientific article published on August 2006

Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A

scientific article published on 8 January 2016

Identification of Ras-related nuclear protein, targeting protein for xenopus kinesin-like protein 2, and stearoyl-CoA desaturase 1 as promising cancer targets from an RNAi-based screen.

scientific article

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

scientific article published on February 2007

Interaction of the oncoprotein transcription factor MYC with its chromatin cofactor WDR5 is essential for tumor maintenance

scientific article published on 25 November 2019

Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC

scientific article

Ligand binding to domain-3 of human serum albumin: a chemometric analysis

scientific article

NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability

scientific article published in December 2002

NMR-driven discovery of benzoylanthranilic acid inhibitors of far upstream element binding protein binding to the human oncogene c-myc promoter.

scientific article published in September 2004

Non-peptidic small molecule inhibitors of XIAP

scientific article published on 01 February 2005

Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors Using Structure-Based Design.

scientific article published on 11 January 2018

Over-expression of the human MDM2 p53 binding domain by fusion to a p53 transactivation peptide.

scientific article

Promoting apoptosis as a strategy for cancer drug discovery

scientific article

Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A.

scientific article published on 4 November 2016

Regulation of the Apaf-1/caspase-9 apoptosome by caspase-3 and XIAP.

scientific article published on 27 December 2002

Reply to Tran et al.: Dimeric KRAS protein-protein interaction stabilizers

scientific article published on 11 February 2020

Resolving Resonance Overlap in the NMR Spectra of Proteins from Differential Lanthanide-Induced Shifts

scientific article published in 1997

Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses

scientific article published on 18 February 2019

Small molecule Mcl-1 inhibitors for the treatment of cancer

scientific article

Solution structure of a Bcl-2 homolog from Kaposi sarcoma virus

scientific article

Solution structure of the BHRF1 protein from Epstein-Barr virus, a homolog of human Bcl-2

scientific article

Specificity of short interfering RNA determined through gene expression signatures ⬇️

scientific article published on May 13, 2003

Structural Elucidation of Peptide Binding to KLHL-12, a Substrate Specific Adapter Protein in a Cul3-Ring E3 Ligase Complex

scientific article published on 17 February 2020

Structural biology of the Bcl-2 family of proteins

scientific article published on March 2004

Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.

scientific article

Structure of the N-terminal RNA-binding domain of the SARS CoV nucleocapsid protein.

scientific article

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL

scientific article

Surface Reengineering of RPA70N Enables Cocrystallization with an Inhibitor of the Replication Protein A Interaction Motif of ATR Interacting Protein

scientific article

Survivin depletion preferentially reduces the survival of activated K-Ras-transformed cells.

scientific article

Targeting MYC through WDR5

scientific article published on 10 January 2020

Targeting WDR5: A WINning Anti-Cancer Strategy?

scientific article published on 18 July 2019

The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo

scientific article

Twenty years on: the impact of fragments on drug discovery

scientific article

Understanding the Species Selectivity of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors

scientific article published on 31 July 2018

WDR5 is a conserved regulator of protein synthesis gene expression

scientific article published on 01 April 2020

siRNA-mediated gene silencing: a global genome view

scientific article

siRNA-mediated off-target gene silencing triggered by a 7 nt complementation

scientific article

List of works by Stephen W. Fesik

1H, 13C and 15N resonance assignments of a Bcl-xL/Bad peptide complex

A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia.

A Strategy for High-Throughput Assay Development Using Leads Derived from Nuclear Magnetic Resonance-Based Screening ⬇️

A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation

A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A.

A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand

A robust in vivo positive-readout system for monitoring siRNA delivery to xenograft tumors

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo

ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

BCL-2 AND IAP Proteins As Potential Drug Targets

Bcl-XL represents a druggable molecular vulnerability during aurora B inhibitor-mediated polyploidization

Defining the optimal parameters for hairpin-based knockdown constructs

Defining the p53 DNA-binding domain/Bcl-x(L)-binding interface using NMR.

Developing lipid nanoparticle-based siRNA therapeutics for hepatocellular carcinoma using an integrated approach

Development of a tightly regulated U6 promoter for shRNA expression

Diphenylpyrazoles as replication protein a inhibitors

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction

Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core

Discovery and Structure−Activity Relationship of Oxalylarylaminobenzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B ⬇️

Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors

Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.

Discovery of Inhibitors of Protein-Protein Interactions Using Fragment-Based Methods

Discovery of Potent 2-Aryl-6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design

Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer

Discovery of Protein–Protein Interaction Inhibitors of Replication Protein A

Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS

Discovery of Small Molecules that Bind to K‐Ras and Inhibit Sos‐Mediated Activation ⬇️

Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design

Discovery of a Potent Inhibitor of Replication Protein A Protein–Protein Interactions Using a Fragment-Linking Approach

Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A

Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR ⬇️

Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy

Discovery of aminoglycoside mimetics by NMR-based screening of Escherichia coli A-site RNA.

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer

Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design

Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity

Druggability indices for protein targets derived from NMR-based screening data

Drugging an undruggable pocket on KRAS

Drugging the undruggable RAS: Mission possible?

Evaluating hypoxia-inducible factor-1alpha as a cancer therapeutic target via inducible RNA interference in vivo

Fragment-based drug discovery using NMR spectroscopy

Fragment-based screening of programmed death ligand 1 (PD-L1)

Fragment-based screening of the bromodomain of ATAD2.

From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae

Growth inhibition and radiosensitization of glioblastoma and lung cancer cells by small interfering RNA silencing of tumor necrosis factor receptor-associated factor 2.

Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo

Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A

Identification of Ras-related nuclear protein, targeting protein for xenopus kinesin-like protein 2, and stearoyl-CoA desaturase 1 as promising cancer targets from an RNAi-based screen.

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

Interaction of the oncoprotein transcription factor MYC with its chromatin cofactor WDR5 is essential for tumor maintenance

Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC

Ligand binding to domain-3 of human serum albumin: a chemometric analysis

NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability

NMR-driven discovery of benzoylanthranilic acid inhibitors of far upstream element binding protein binding to the human oncogene c-myc promoter.

Non-peptidic small molecule inhibitors of XIAP

Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors Using Structure-Based Design.

Over-expression of the human MDM2 p53 binding domain by fusion to a p53 transactivation peptide.

Promoting apoptosis as a strategy for cancer drug discovery

Recent advancements in the discovery of protein-protein interaction inhibitors of replication protein A.

Regulation of the Apaf-1/caspase-9 apoptosome by caspase-3 and XIAP.

Reply to Tran et al.: Dimeric KRAS protein-protein interaction stabilizers

Resolving Resonance Overlap in the NMR Spectra of Proteins from Differential Lanthanide-Induced Shifts

Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses

Small molecule Mcl-1 inhibitors for the treatment of cancer

Solution structure of a Bcl-2 homolog from Kaposi sarcoma virus

Solution structure of the BHRF1 protein from Epstein-Barr virus, a homolog of human Bcl-2

Specificity of short interfering RNA determined through gene expression signatures ⬇️

Structural Elucidation of Peptide Binding to KLHL-12, a Substrate Specific Adapter Protein in a Cul3-Ring E3 Ligase Complex

Structural biology of the Bcl-2 family of proteins

Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.