List of works - Patrick M. Woster

(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators

scientific article published on July 2010

1-(N-alkylamino)-11-(N-ethylamino)-4,8-diazaundecanes: simple synthetic polyamine analogues that differentially alter tubulin polymerization

scientific article published on 01 April 1999

3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors

scientific article published in December 2014

6',7'-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein

scientific article published on 01 March 1999

A charge-deficient analogue of spermine with chelating properties

scientific article published in May 2005

A novel histone deacetylase inhibitor prevents IL-1beta induced metabolic dysfunction in pancreatic beta-cells

scientific article published on August 2009

A role for bioactivation and covalent binding within epidermal keratinocytes in sulfonamide-induced cutaneous drug reactions

scientific article

A small molecule polyamine oxidase inhibitor blocks androgen-induced oxidative stress and delays prostate cancer progression in the transgenic adenocarcinoma of the mouse prostate model

scientific article published on 22 September 2009

Alkyl-substituted polyaminohydroxamic acids: a novel class of targeted histone deacetylase inhibitors

scientific article published on October 2005

Bergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans

scientific article published in December 2004

Citizenship in the World of Medicinal Chemistry: 25 Years as an ACSMEDI Volunteer

scientific article published on 22 April 2019

Comparison of polyamine analogue toxicity in two cell lines (HL-60 & MCF-7)

scientific article published on 01 November 1998

Comparison of the in vitro cytotoxicity of hydroxylamine metabolites of sulfamethoxazole and dapsone

scientific article published on 01 March 1998

Crystal structures of multidrug-resistant HIV-1 protease in complex with two potent anti-malarial compounds

scientific article

Cyclic by peptide inhibitors of lysine-specific demethylase 1 with improved potency identified by alanine scanning mutagenesis.

scientific article published on 7 February 2018

Cytotoxicity of novel unsymmetrically substituted inhibitors of polyamine biosynthesis in human cancer cells

scientific article

Dapsone-induced hematologic toxicity: comparison of the methemoglobin-forming ability of hydroxylamine metabolites of dapsone in rat and human blood

scientific article published on 01 December 1994

Design of polyamine-based therapeutic agents: new targets and new directions

scientific article

Design of small molecule epigenetic modulators

scientific article

Discovery of a new class of histone deacetylase inhibitors with a novel zinc binding group

scientific article published on April 2015

Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities

scientific article

Dual inhibitors of LSD1 and spermine oxidase

scientific article published on 08 February 2019

Effect of S-adenosyl-1,12-diamino-3-thio-9-azadodecane, a multisubstrate adduct inhibitor of spermine synthase, on polyamine metabolism in mammalian cells

scientific article published on October 1989

Effect of pro-inflammatory cytokines on the toxicity of the arylhydroxylamine metabolites of sulphamethoxazole and dapsone in normal human keratinocytes

scientific article

Elevated ornithine decarboxylase activity promotes skin tumorigenesis by stimulating the recruitment of bulge stem cells but not via toxic polyamine catabolic metabolites

scientific article published on 25 July 2013

Elevated ornithine decarboxylase levels activate ataxia telangiectasia mutated-DNA damage signaling in normal keratinocytes

scientific article published on April 2008

Epigenetics: Novel Therapeutics Targeting Epigenetics

scientific article published on 29 January 2016

Epigenetics: novel therapeutics targeting epigenetics

scientific article published on 22 December 2014

Foreword: American Chemical Society Division of Medicinal Chemistry. Celebrating 100 years of excellence

scientific article published in December 2009

Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1

scientific article published on 01 January 1995

Histone deacetylase inhibition overcomes drug resistance through a miRNA-dependent mechanism.

scientific article published on 13 August 2013

Increased Helicobacter pylori-associated gastric cancer risk in the Andean region of Colombia is mediated by spermine oxidase.

scientific article

Induction of apoptosis in human leukaemic cells by IPENSpm, a novel polyamine analogue and anti-metabolite

scientific article published in October 2002

Induction of human spermine oxidase SMO(PAOh1) is regulated at the levels of new mRNA synthesis, mRNA stabilization and newly synthesized protein

scientific article published on March 2005

Induction of the PAOh1/SMO polyamine oxidase by polyamine analogues in human lung carcinoma cells

scientific article

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

scientific article published on 11 March 2012

Inhibition of the histone demethylase KDM4B leads to activation of KDM1A, attenuates bacterial-induced pro-inflammatory cytokine release, and reduces osteoclastogenesis

scientific article published on 07 August 2018

Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites

scientific article published on 28 January 2015

Irreversible inhibition of human S-adenosylmethionine decarboxylase by the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4- methylsulfonio-2-cyclopentene (AdoMac)

scientific article published on 01 April 1995

Knockdown of ornithine decarboxylase antizyme 1 causes loss of uptake regulation leading to increased N 1, N 11-bis(ethyl)norspermine (BENSpm) accumulation and toxicity in NCI H157 lung cancer cells ⬇️

scientific article published on August 4, 2011

Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease

scientific article

Loss of LSD1 (lysine-specific demethylase 1) suppresses growth and alters gene expression of human colon cancer cells in a p53- and DNMT1(DNA methyltransferase 1)-independent manner.

scientific article

Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1

scientific article published on 4 September 2012

Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents

scientific article published in May 2010

Metabolism of an alkyl polyamine analog by a polyamine oxidase from the microsporidian Encephalitozoon cuniculi.

scientific article published on 17 February 2009

Molecular basis for the polyamine-ompF porin interactions: inhibitor and mutant studies

scientific article published on 01 April 2000

Novel Pt(II) and Pd(II) complexes with polyamine analogues: synthesis and vibrational analysis.

scientific article

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

scientific article published on 17 April 2006

Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes

scientific article

P1 and P1' para-fluoro phenyl groups show enhanced binding and favorable predicted pharmacological properties: structure-based virtual screening of extended lopinavir analogs against multi-drug resistant HIV-1 protease.

scientific article

Photoaffinity labeling of a cell surface polyamine binding protein

scientific article published on 01 December 1995

Polyamine analogs modulate gene expression by inhibiting lysine-specific demethylase 1 (LSD1) and altering chromatin structure in human breast cancer cells

scientific article published on 30 July 2011

Polyamine analogues targeting epigenetic gene regulation

scientific article

Polyamine catabolism contributes to enterotoxigenic Bacteroides fragilis -induced colon tumorigenesis ⬇️

scientific article published on August 29, 2011

Polyamine-based analogues as biochemical probes and potential therapeutics

scientific article published on April 2007

Polyamine-based small molecule epigenetic modulators.

scientific article published on 26 November 2011

Polyamines and cancer: implications for chemotherapy and chemoprevention

scientific article

Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors

scientific article

Preparation of the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-methylsulfonio-2-cyclopentene and their evaluation as irreversible inhibitors of S-adenosylmethionine decarboxylase from Escherichia coli.

scientific article

Properties of purified recombinant human polyamine oxidase, PAOh1/SMO

scientific journal article

Reactive oxygen species generation and its role in the differential cytotoxicity of the arylhydroxylamine metabolites of sulfamethoxazole and dapsone in normal human epidermal keratinocytes

scientific article published in July 2005

Recent advances in the development of polyamine analogues as antitumor agents

scientific article published on August 2009

Role of p53/p21(Waf1/Cip1) in the regulation of polyamine analogue-induced growth inhibition and cell death in human breast cancer cells.

scientific article published on 23 September 2005

S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity

scientific article published on May 1995

S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-(methylsulfonio)-2-cyclopentene: A potent, enzyme-activated irreversible inhibitor of S-adenosylmethionine decarboxylase

scientific article published in August 1992

Spermine analogue-regulated expression of spermidine/spermine N1-acetyltransferase and its effects on depletion of intracellular polyamine pools in mouse fetal fibroblasts

scientific article published on 29 July 2009

Spermine and spermidine mediate protection against oxidative damage caused by hydrogen peroxide

scientific article

Spermine oxidase (SMO) activity in breast tumor tissues and biochemical analysis of the anticancer spermine analogues BENSpm and CPENSpm.

scientific article

Spermine oxidase SMO(PAOh1), Not N1-acetylpolyamine oxidase PAO, is the primary source of cytotoxic H2O2 in polyamine analogue-treated human breast cancer cell lines.

scientific article

Structural specificity of polyamines and polyamine analogues in the protection of DNA from strand breaks induced by reactive oxygen species

scientific article published on 01 March 1998

Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures

scientific article

Studies of the mechanism by which increased spermidine/spermine N1-acetyltransferase activity increases susceptibility to skin carcinogenesis

scientific article published on 03 August 2007

Suppression of exogenous gene expression by spermidine/spermine N1-acetyltransferase 1 (SSAT1) cotransfection.

scientific article

Synthesis and biological evaluation of S-adenosyl-1,12-diamino-3-thio-9-azadodecane, a multisubstrate adduct inhibitor of spermine synthase

scientific article published in June 1989

Synthesis and biological evaluation of cyclic analogues of 1-carnitine as potential agents in the treatment of myocardial ischemia

scientific article published on 01 May 1986

Synthesis and evaluation of a polyamine phosphinate and phosphonamidate as transition-state analogue inhibitors of spermidine/spermine-N1-acetyltransferase

scientific article published on 01 June 1996

Synthesis and evaluation of novel cyclic Peptide inhibitors of lysine-specific demethylase 1.

scientific article published on 8 November 2013

Synthesis and evaluation of unsymmetrically substituted polyamine analogues as modulators of human spermidine/spermine-N1-acetyltransferase (SSAT) and as potential antitumor agents

scientific article published in October 1993

Terminally alkylated polyamine analogues as chemotherapeutic agents.

scientific article

The activator-binding site of Onchocerca volvulus S-adenosylmethionine decarboxylase, a potential drug target

scientific article published on August 2003

The natural polyamine spermine functions directly as a free radical scavenger.

scientific article

The re-expression of the epigenetically silenced e-cadherin gene by a polyamine analogue lysine-specific demethylase-1 (LSD1) inhibitor in human acute myeloid leukemia cell lines

scientific article published on 19 March 2013

The role of polyamine catabolism in polyamine analogue-induced programmed cell death

scientific article published on October 1997

Transcriptional activity of the islet β cell factor Pdx1 is augmented by lysine methylation catalyzed by the methyltransferase Set7/9.

scientific article

Use of Polyamine Derivatives as Selective Histone Deacetylase Inhibitors ⬇️

scientific article published on January 1, 2011

List of works by Patrick M. Woster

(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators

1-(N-alkylamino)-11-(N-ethylamino)-4,8-diazaundecanes: simple synthetic polyamine analogues that differentially alter tubulin polymerization

3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors

6',7'-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein

A charge-deficient analogue of spermine with chelating properties

A novel histone deacetylase inhibitor prevents IL-1beta induced metabolic dysfunction in pancreatic beta-cells

A role for bioactivation and covalent binding within epidermal keratinocytes in sulfonamide-induced cutaneous drug reactions

A small molecule polyamine oxidase inhibitor blocks androgen-induced oxidative stress and delays prostate cancer progression in the transgenic adenocarcinoma of the mouse prostate model

Alkyl-substituted polyaminohydroxamic acids: a novel class of targeted histone deacetylase inhibitors

Bergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans

Citizenship in the World of Medicinal Chemistry: 25 Years as an ACSMEDI Volunteer

Comparison of polyamine analogue toxicity in two cell lines (HL-60 & MCF-7)

Comparison of the in vitro cytotoxicity of hydroxylamine metabolites of sulfamethoxazole and dapsone

Crystal structures of multidrug-resistant HIV-1 protease in complex with two potent anti-malarial compounds

Cyclic by peptide inhibitors of lysine-specific demethylase 1 with improved potency identified by alanine scanning mutagenesis.

Cytotoxicity of novel unsymmetrically substituted inhibitors of polyamine biosynthesis in human cancer cells

Dapsone-induced hematologic toxicity: comparison of the methemoglobin-forming ability of hydroxylamine metabolites of dapsone in rat and human blood

Design of polyamine-based therapeutic agents: new targets and new directions

Design of small molecule epigenetic modulators

Discovery of a new class of histone deacetylase inhibitors with a novel zinc binding group

Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities

Dual inhibitors of LSD1 and spermine oxidase

Effect of S-adenosyl-1,12-diamino-3-thio-9-azadodecane, a multisubstrate adduct inhibitor of spermine synthase, on polyamine metabolism in mammalian cells

Effect of pro-inflammatory cytokines on the toxicity of the arylhydroxylamine metabolites of sulphamethoxazole and dapsone in normal human keratinocytes

Elevated ornithine decarboxylase activity promotes skin tumorigenesis by stimulating the recruitment of bulge stem cells but not via toxic polyamine catabolic metabolites

Elevated ornithine decarboxylase levels activate ataxia telangiectasia mutated-DNA damage signaling in normal keratinocytes

Epigenetics: Novel Therapeutics Targeting Epigenetics

Epigenetics: novel therapeutics targeting epigenetics

Foreword: American Chemical Society Division of Medicinal Chemistry. Celebrating 100 years of excellence

Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1

Histone deacetylase inhibition overcomes drug resistance through a miRNA-dependent mechanism.

Increased Helicobacter pylori-associated gastric cancer risk in the Andean region of Colombia is mediated by spermine oxidase.

Induction of apoptosis in human leukaemic cells by IPENSpm, a novel polyamine analogue and anti-metabolite

Induction of human spermine oxidase SMO(PAOh1) is regulated at the levels of new mRNA synthesis, mRNA stabilization and newly synthesized protein

Induction of the PAOh1/SMO polyamine oxidase by polyamine analogues in human lung carcinoma cells

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

Inhibition of the histone demethylase KDM4B leads to activation of KDM1A, attenuates bacterial-induced pro-inflammatory cytokine release, and reduces osteoclastogenesis

Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites

Irreversible inhibition of human S-adenosylmethionine decarboxylase by the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4- methylsulfonio-2-cyclopentene (AdoMac)

Knockdown of ornithine decarboxylase antizyme 1 causes loss of uptake regulation leading to increased N 1, N 11-bis(ethyl)norspermine (BENSpm) accumulation and toxicity in NCI H157 lung cancer cells ⬇️

Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease

Loss of LSD1 (lysine-specific demethylase 1) suppresses growth and alters gene expression of human colon cancer cells in a p53- and DNMT1(DNA methyltransferase 1)-independent manner.

Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1

Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents

Metabolism of an alkyl polyamine analog by a polyamine oxidase from the microsporidian Encephalitozoon cuniculi.

Molecular basis for the polyamine-ompF porin interactions: inhibitor and mutant studies

Novel Pt(II) and Pd(II) complexes with polyamine analogues: synthesis and vibrational analysis.

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes

P1 and P1' para-fluoro phenyl groups show enhanced binding and favorable predicted pharmacological properties: structure-based virtual screening of extended lopinavir analogs against multi-drug resistant HIV-1 protease.

Photoaffinity labeling of a cell surface polyamine binding protein

Polyamine analogs modulate gene expression by inhibiting lysine-specific demethylase 1 (LSD1) and altering chromatin structure in human breast cancer cells

Polyamine analogues targeting epigenetic gene regulation

Polyamine catabolism contributes to enterotoxigenic Bacteroides fragilis -induced colon tumorigenesis ⬇️

Polyamine-based analogues as biochemical probes and potential therapeutics

Polyamine-based small molecule epigenetic modulators.

Polyamines and cancer: implications for chemotherapy and chemoprevention

Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors

Preparation of the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-methylsulfonio-2-cyclopentene and their evaluation as irreversible inhibitors of S-adenosylmethionine decarboxylase from Escherichia coli.

Properties of purified recombinant human polyamine oxidase, PAOh1/SMO

Reactive oxygen species generation and its role in the differential cytotoxicity of the arylhydroxylamine metabolites of sulfamethoxazole and dapsone in normal human epidermal keratinocytes

Recent advances in the development of polyamine analogues as antitumor agents

Role of p53/p21(Waf1/Cip1) in the regulation of polyamine analogue-induced growth inhibition and cell death in human breast cancer cells.

S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity

S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-(methylsulfonio)-2-cyclopentene: A potent, enzyme-activated irreversible inhibitor of S-adenosylmethionine decarboxylase

Spermine analogue-regulated expression of spermidine/spermine N1-acetyltransferase and its effects on depletion of intracellular polyamine pools in mouse fetal fibroblasts

Spermine and spermidine mediate protection against oxidative damage caused by hydrogen peroxide

Spermine oxidase (SMO) activity in breast tumor tissues and biochemical analysis of the anticancer spermine analogues BENSpm and CPENSpm.

Spermine oxidase SMO(PAOh1), Not N1-acetylpolyamine oxidase PAO, is the primary source of cytotoxic H2O2 in polyamine analogue-treated human breast cancer cell lines.

Structural specificity of polyamines and polyamine analogues in the protection of DNA from strand breaks induced by reactive oxygen species

Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures

Studies of the mechanism by which increased spermidine/spermine N1-acetyltransferase activity increases susceptibility to skin carcinogenesis

Suppression of exogenous gene expression by spermidine/spermine N1-acetyltransferase 1 (SSAT1) cotransfection.

Synthesis and biological evaluation of S-adenosyl-1,12-diamino-3-thio-9-azadodecane, a multisubstrate adduct inhibitor of spermine synthase

Synthesis and biological evaluation of cyclic analogues of 1-carnitine as potential agents in the treatment of myocardial ischemia

Synthesis and evaluation of a polyamine phosphinate and phosphonamidate as transition-state analogue inhibitors of spermidine/spermine-N1-acetyltransferase

Synthesis and evaluation of novel cyclic Peptide inhibitors of lysine-specific demethylase 1.

Synthesis and evaluation of unsymmetrically substituted polyamine analogues as modulators of human spermidine/spermine-N1-acetyltransferase (SSAT) and as potential antitumor agents

Terminally alkylated polyamine analogues as chemotherapeutic agents.