S. Fletcher

发表

Therapeutic potential of Bcl-xL/Mcl-1 synthetic inhibitor JY-1-106 and retinoids for human triple-negative breast cancer treatment.

M. Perri, J. Yap, S. Fletcher, 2018, Oncology letters.

Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity.

M. Minden, P. Yue, J. Turkson, 2012, Journal of medicinal chemistry.

Targeting protein–protein interactions by rational design: mimicry of protein surfaces

S. Fletcher, A. Hamilton, 2006, Journal of The Royal Society Interface.

Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling.

Alexander D. MacKerell, J. Yap, S. Fletcher, 2013, Organic & biomolecular chemistry.

Molecular Approaches towards the Inhibition of the Signal Transducer and Activator of Transcription 3 (Stat3) Protein

J. Turkson, S. Fletcher, P. Gunning, 2008, ChemMedChem.

Structure–activity exploration of a small-molecule Lipid II inhibitor

Alexander D. MacKerell, Jing Huang, S. Fletcher, 2015, Drug design, development and therapy.

Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.

J. Yap, S. Fletcher, M. Lanning, 2017, Journal of medicinal chemistry.

Mechanistic Analysis of an Extracellular Signal–Regulated Kinase 2–Interacting Compound that Inhibits Mutant BRAF-Expressing Melanoma Cells by Inducing Oxidative Stress

S. Fletcher, M. Kane, P. Shapiro, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.

Alexander D. MacKerell, P. Wilder, J. Yap, 2016, European journal of medicinal chemistry.

Nanotherapy delivery of c-myc inhibitor targets Protumor Macrophages and preserves Antitumor Macrophages in Breast Cancer

S. Achilefu, S. Fletcher, A. Schmieder, 2020, Theranostics.

Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.

D. Chakrabarti, F. Buckner, S. Fletcher, 2006, Journal of medicinal chemistry.

A Photostable, pH-Invariant Fluorescein Derivative for Single-Molecule Microscopy

C. Gradinaru, S. Fletcher, P. Gunning, 2009, Journal of Fluorescence.

3JC48-3 (methyl 4′-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1′-biphenyl]-3-carboxylate): a novel MYC/MAX dimerization inhibitor reduces prostate cancer growth

S. Shukla, S. Fletcher, Y. Mackeyev, 2022, Cancer Gene Therapy.

VLA4-Targeted Nanoparticles Hijack Cell Adhesion–Mediated Drug Resistance to Target Refractory Myeloma Cells and Prolong Survival

R. Vij, J. Dipersio, S. Fletcher, 2020, Clinical Cancer Research.

Structural Modifications of (Z)-3-(2-aminoethyl)-5-(4- ethoxybenzylidene)thiazolidine-2,4-dione that Improve Selectivity for the Inhibition of Melanoma Cells Containing Active ERK Signaling

J. Yap, S. Fletcher, P. Shapiro, 2014 .

Synthesis and cytotoxic evaluation of some 6-arylidene-2-(alpha-hydroxyamino-alpha-arylmethyl)cyclohexanone oximes and related compounds.

M. Duffy, D. Kirkpatrick, Z. Jia, 1992, Journal of pharmaceutical sciences.

Dual Farnesyl and Geranylgeranyl Transferase Inhibitor Thwarts Mutant KRAS-Driven Patient-Derived Pancreatic Tumors

Huan Yang, S. Fletcher, J. Fleming, 2019, Clinical Cancer Research.

Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.

William P. Katt, M. Gelb, L. Beese, 2010, Journal of medicinal chemistry.

Fine-tuning the chemo- and regioselective alkylation of 1,4-benzodiazepines: further applications of the Mitsunobu reaction

S. Fletcher, K. Jung, 2012 .

Coordination complex SH2 domain proteomimetics: an alternative approach to disrupting oncogenic protein-protein interactions.

P. Yue, J. Turkson, C. Gradinaru, 2010, Chemical communications.

The downregulation of Mcl-1 via USP9X inhibition sensitizes solid tumors to Bcl-xl inhibition

J. Yap, S. Fletcher, P. Rascoe, 2012, BMC Cancer.

Small-molecule inhibitors of ERK-mediated immediate early gene expression and proliferation of melanoma cells expressing mutated BRaf.

Alexander D. MacKerell, U. D. Priyakumar, S. Fletcher, 2015, The Biochemical journal.

Discovery and lead identification of quinazoline-based BRD4 inhibitors.

D. Urban, J. Strovel, A. Jadhav, 2018, Bioorganic & medicinal chemistry letters.

CG223, a novel BET inhibitor, exerts TGF-β1-mediated antifibrotic effects in a murine model of bleomycin-induced pulmonary fibrosis.

J. Strovel, M. Yoshioka, S. Fletcher, 2021, Pulmonary pharmacology & therapeutics.

MCL-1 inhibitors – where are we now (2019)?

S. Fletcher, 2019, Expert opinion on therapeutic patents.

Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain

Michelle H. W. Laird, A. MacKerell, S. Fletcher, 2015, Proceedings of the National Academy of Sciences.

Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain.

P. Yue, J. Turkson, S. Trudel, 2011, Bioorganic & medicinal chemistry letters.

Protein recognition and denaturation by self-assembling fragments on a DNA quadruplex scaffold.

S. Fletcher, A. Hamilton, J. Jayawickramarajah, 2007, Angewandte Chemie.

Discovery of Mcl-1 inhibitors based on a thiazolidine-2,4-dione scaffold.

P. Wilder, S. Fletcher, Jay Chauhan, 2017, Bioorganic & medicinal chemistry letters.

Small-Molecule Inhibitors of the Mcl-1 Oncoprotein

S. Fletcher, M. Lanning, Lijia Chen, 2014 .

Synthesis and in vitro evaluation of gabapentin prodrugs that target the human apical sodium-dependent bile acid transporter (hASBT).

J. Polli, S. Fletcher, R. Rais, 2011, Journal of pharmaceutical sciences.

Kröhnke pyridines: Rapid and facile access to Mcl-1 inhibitors.

R. Godoy-Ruiz, P. Wilder, S. Fletcher, 2018, Bioorganic & medicinal chemistry letters.

Regioselective alkylation of the exocyclic nitrogen of adenine and adenosine by the Mitsunobu reaction

S. Fletcher, 2010 .

Ortho-selectivity in the nucleophilic aromatic substitution (SNAr) reactions of 3-substituted, 2,6-dichloropyridines with alkali metal alkoxides

J. Yap, S. Fletcher, K. Hom, 2011 .

One-pot synthesis of 2,1-benzisoxazoles (anthranils) by a stannous chloride-mediated tandem reduction–heterocyclization of 2-nitroacylbenzenes under neutral conditions

S. Fletcher, Jay Chauhan, 2012 .

The Mitsunobu reaction in the 21st century

S. Fletcher, 2015 .

Synthesis, characterization and antineoplastic activity of bis-aziridinyl dimeric naphthoquinone - A novel class of compounds with potent activity against acute myeloid leukemia cells.

E. Sausville, S. Fletcher, D. Ferraris, 2017, Bioorganic & medicinal chemistry letters.

Concise access to N9-mono-, N2-mono- and N2,N9-di-substituted guanines via efficient Mitsunobu reactions

S. Fletcher, A. Lough, P. Gunning, 2010 .

One‐Pot Synthesis of 2,1‐Benzisoxazoles (Anthranils) by a Stannous Chloride Mediated Tandem Reduction—Heterocyclization of 2‐Nitroacylbenzenes under Neutral Conditions.

S. Fletcher, Jay Chauhan, 2012 .

Construction of 1H-indazoles from ortho-aminobenzoximes by the Mitsunobu reaction

S. Fletcher, Ivie L. Conlon, Yulemni Morel, 2019, Tetrahedron Letters.

Small‐Molecule Inhibitors of the ERK Signaling Pathway: Towards Novel Anticancer Therapeutics

Alexander D. MacKerell, J. Yap, S. Fletcher, 2011, ChemMedChem.

Mild, efficient and rapid O-debenzylation of ortho-substituted phenols with trifluoroacetic acid

S. Fletcher, P. Gunning, 2008 .

Facile and efficient access to 2,6,9-tri-substituted purines through sequential N9, N2 Mitsunobu reactions

S. Fletcher, P. Gunning, V. Shahani, 2009 .

Chromatography-free entry to substituted salicylonitriles: Mitsunobu-triggered domino reactions of salicylaldoximes.

S. Fletcher, M. Lanning, Ellis Whiting, 2015, The Journal of organic chemistry.

Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function.

J. DeStefano, E. Freire, S. Fletcher, 2015, Bioorganic & medicinal chemistry.

Recognition of solvent exposed protein surfaces using anthracene derived receptors.

S. Fletcher, A. Hamilton, Andrew J. Wilson, 2007, Organic & biomolecular chemistry.

Protein surface recognition and proteomimetics: mimics of protein surface structure and function.

Steven Fletcher, S. Fletcher, A. Hamilton, 2005, Current opinion in chemical biology.

Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.

Alexander D. MacKerell, P. Wilder, J. Yap, 2012, Organic & biomolecular chemistry.

Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion

E. Prochownik, Huabo Wang, S. Fletcher, 2015, Oncotarget.

Small-molecule inhibitors of the Myc oncoprotein.

E. Prochownik, S. Fletcher, 2015, Biochimica et biophysica acta.

Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.

E. Prochownik, Huabo Wang, N. Cosford, 2015, Journal of medicinal chemistry.

Novel asymmetrically functionalized bis-dipicolylamine metal complexes: peripheral decoration of a potent anion recognition scaffold.

S. Fletcher, P. Gunning, J. Drewry, 2009, Organic & biomolecular chemistry.

Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.

Steven Fletcher, M. Gelb, L. Beese, 2009, Chemistry & biology.

Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.

William P. Katt, D. Chakrabarti, M. Gelb, 2008, Journal of medicinal chemistry.

Artificially induced protein-membrane anchorage with cholesterol-based recognition agents as a new therapeutic concept.

P. Yue, J. Turkson, C. Gradinaru, 2011, Angewandte Chemie.

Small‐Molecule Inhibitors of the ERK Signaling Pathway: Towards Novel Anticancer Therapeutics

Alexander D. MacKerell, Paul Shapiro, Steven Fletcher, 2011, ChemMedChem.

Concise Access to N9-Mono-, N2-Mono- and N2,N9-Disubstituted Guanines via Efficient Mitsunobu Reactions.

S. Fletcher, A. Lough, P. Gunning, 2010 .

Disruption of Myc-Max Heterodimerization with Improved Cell-Penetrating Analogs of the Small Molecule 10074-G5

Kelsey P. Pendleton, Jace W. Jones, E. Prochownik, 2013, Oncotarget.

A novel small-molecule disrupts Stat3 SH2 domain-phosphotyrosine interactions and Stat3-dependent tumor processes.

P. Yue, J. Turkson, S. Fletcher, 2010, Biochemical pharmacology.

Pharmacophore identification of c-Myc inhibitor 10074-G5.

E. Prochownik, Huabo Wang, J. Yap, 2013, Bioorganic & medicinal chemistry letters.

Shifting the paradigm in treating multi-factorial diseases: polypharmacological co-inhibitors of HDAC6.

S. Fletcher, Alexandria M Chan, 2021, RSC medicinal chemistry.

Mechanistic analysis of an ERK2-interacting compound that inhibits mutant-BRAF expressing melanoma cells by inducing oxidative stress

S. Fletcher, M. Kane, P. Shapiro, 2020 .

Small-molecule inhibitors of dimeric transcription factors: Antagonism of protein–protein and protein–DNA interactions

E. Prochownik, J. Yap, S. Fletcher, 2012 .

BCL-xL/MCL-1 inhibition and RARγ antagonism work cooperatively in human HL60 leukemia cells.

M. Perri, J. Yap, S. Fletcher, 2014, Experimental cell research.

Azodicarbonyl dimorpholide (ADDM): an effective, versatile, and water-soluble Mitsunobu reagent

S. Fletcher, M. Lanning, 2013 .

BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.

J. Strovel, M. Yoshioka, J. Yap, 2015, ACS medicinal chemistry letters.

Orthogonal targeting of osteoclasts and myeloma cells for radionuclide stimulated dynamic therapy induces multidimensional cell death pathways

S. Achilefu, S. Fletcher, Baogang Xu, 2021, Theranostics.

The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein–protein interactions with Bak

Alexander D. MacKerell, Xiaobo Cao, Kenno Vanommeslaeghe, 2013, Molecular Cancer.

Modified Suberoylanilide Hydroxamic Acid Reduced Drug-Associated Immune Cell Death and Organ Damage under Lipopolysaccharide Inflammatory Challenge.

Ryan M. Pearson, S. Fletcher, N. Truong, 2022, ACS pharmacology & translational science.

Discovery and anti-tumor activity of 4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinoline-2(1H)-one (CG13250), a potent, selective and orally bioavailable BET bromodomain inhibitor.

J. Strovel, M. Yoshioka, S. Fletcher, 2023, Bioorganic & medicinal chemistry letters.

Mcl-1 inhibitors: a patent review

S. Fletcher, Lijia Chen, 2017, Expert opinion on therapeutic patents.

CG13250, a novel bromodomain inhibitor, suppresses proliferation of multiple myeloma cells in an orthotopic mouse model.

J. Strovel, Susumu Nakata, K. Takata, 2017, Biochemical and biophysical research communications.

Discovery of Methyl 4′‐Methyl‐5‐(7‐nitrobenzo[c][1,2,5]oxadiazol‐4‐yl)‐[1,1′‐biphenyl]‐3‐carboxylate, an Improved Small‐Molecule Inhibitor of c‐Myc–Max Dimerization

E. Prochownik, Huabo Wang, J. Yap, 2014, ChemMedChem.

Parallel syntheses of disulfide inhibitors of the thioredoxin redox system as potential antitumor agents.

M. Kunkel, D. Kirkpatrick, G. Powis, 1999, Anti-cancer drug design.

Surface Binding Inhibitors of the SCF–KIT Protein–Protein Interaction

D. Margulies, I. Lax, J. Schlessinger, 2009, Chembiochem : a European journal of chemical biology.

Recent applications of covalent chemistries in protein-protein interaction inhibitors.

S. Fletcher, Elie Pommier, Alexandria M Chan, 2022, RSC medicinal chemistry.

O-Alkylation of 3-hydroxyisoxazoles predominates under Mitsunobu conditions

S. Fletcher, Lijia Chen, 2014 .

Multi-Facial, Non-Peptidic α-Helix Mimetics

S. Fletcher, M. Lanning, 2015, Biology.

Molecular disruption of oncogenic signal transducer and activator of transcription 3 (STAT3) protein.

S. Fletcher, B. Page, P. Gunning, 2009, Biochemistry and cell biology = Biochimie et biologie cellulaire.

Structure-based design of 3-carboxy-substituted 1,2,3,4-tetrahydroquinolines as inhibitors of myeloid cell leukemia-1 (Mcl-1).

P. Wilder, S. Fletcher, P. Shapiro, 2016, Organic & biomolecular chemistry.

Structural Re‐engineering of the α‐Helix Mimetic JY‐1‐106 into Small Molecules: Disruption of the Mcl‐1–Bak‐BH3 Protein–Protein Interaction with 2,6‐Di‐Substituted Nicotinates

P. Wilder, J. Yap, S. Fletcher, 2016, ChemMedChem.

Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold.

P. Wilder, J. Yap, S. Fletcher, 2015, Organic & biomolecular chemistry.

Recapitulating the α-helix: nonpeptidic, low-molecular-weight ligands for the modulation of helix-mediated protein-protein interactions.

S. Fletcher, M. Lanning, 2013, Future medicinal chemistry.

Amphipathic α-helix mimetics based on a 1,2-diphenylacetylene scaffold.

Alexander D. MacKerell, P. Wilder, J. Yap, 2013, Organic letters.

Antagonism of the Stat3–Stat3 Protein Dimer with Salicylic Acid Based Small Molecules

Steven Fletcher, Patrick T. Gunning, P. Yue, 2011, ChemMedChem.

Disruption of Transcriptionally Active Stat3 Dimers with Non‐phosphorylated, Salicylic Acid‐Based Small Molecules: Potent in vitro and Tumor Cell Activities

P. Yue, J. Turkson, S. Fletcher, 2009, Chembiochem : a European journal of chemical biology.

A quantitative, surface plasmon resonance-based approach to evaluating DNA binding by the c-Myc oncoprotein and its disruption by small molecule inhibitors.

E. Prochownik, Huabo Wang, S. Fletcher, 2015, Journal of biological methods.

Protein-protein interaction inhibitors: small molecules from screening techniques.

Steven Fletcher, S. Fletcher, A. Hamilton, 2007, Current topics in medicinal chemistry.

Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.

P. Yue, J. Turkson, M. Sukhai, 2011, Bioorganic & medicinal chemistry.

Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B

S. Fletcher, M. Tremblay, B. Page, 2013 .

An activatable multimodal/multifunctional nanoprobe for direct imaging of intracellular drug delivery.

J. Turkson, S. Fletcher, G. Walter, 2012, Biomaterials.

Ethyl 2,5-di-tert-butyl-5-ethoxy-4-oxo-4,5-dihydro-1H-pyrrole-3-carboxylate

J. Kao, P. Zavalij, S. Fletcher, 2013, Acta crystallographica. Section E, Structure reports online.

Alexander D. MacKerell, P. Wilder, J. Yap, 2013, Molecular Cancer.

Expedient access to pre-organized α-helix mimetics based on an isocinchomeronic acid core

Alexander D. MacKerell, S. Fletcher, B. Drennen, 2015 .

Recapitulating the a-helix: nonpeptidic, low-molecular-weight ligands for the modulation of helix-mediated protein-protein

S. Fletcher, M. Lanning, 2013 .

Cover Picture: Molecular Approaches towards the Inhibition of the Signal Transducer and Activator of Transcription 3 (Stat3) Protein (ChemMedChem 8/2008)

J. Turkson, S. Fletcher, P. Gunning, 2008 .

1‐Sulfonylated 1,2,3,4‐tetrahydroquinoline‐6‐carboxylic acids as simple, readily‐accessible MCL‐1 inhibitors

P. Wilder, S. Fletcher, Lijia Chen, 2022, Drug development research.

Optimization of a Benzothiazole Indolene Scaffold Targeting Bacterial Cell Wall Assembly

A. MacKerell, S. Fletcher, E. D. de Leeuw, 2020, Drug design, development and therapy.

Towards Development of Small Molecule Lipid II Inhibitors as Novel Antibiotics

Alexander D. MacKerell, Jing Huang, S. Fletcher, 2016, PloS one.

DDDT_A_226313 567..574

A. MacKerell, S. Fletcher, Wenbo Yu, 2020 .

Rationally Designed Polypharmacology: α‐Helix Mimetics as Dual Inhibitors of the Oncoproteins Mcl‐1 and HDM2

A. MacKerell, P. Wilder, S. Fletcher, 2020, ChemMedChem.

Denaturation and accelerated proteolysis of sizeable heme proteins by synthetic metalloporphyrins

S. Fletcher, A. Hamilton, 2007 .

The Bivalent Bromodomain Inhibitor MT-1 Inhibits Prostate Cancer Growth

S. Shukla, S. Fletcher, J. Copland, 2023, Cancers.