Lista de obras - Peter M. Fischer - Dominio Público Uruguay

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity

artículo científico publicado en 2004

2-[(1-methylpropyl)dithio]-1H-imidazole inhibits tubulin polymerization through cysteine oxidation.

artículo científico publicado en 2008

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects

artículo científico publicado en 2006

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

artículo científico publicado en 2013

A Cy5-labeled S100A10 tracer used to identify inhibitors of the protein interaction with annexin A2.

artículo científico publicado en 2010

A facile approach to tryptophan derivatives for the total synthesis of argyrin analogues

artículo científico publicado en 2014

A fluorescence-based assay suitable for quantitative analysis of deadenylase enzyme activity.

artículo científico publicado en 2013

A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin

artículo científico publicado en 2019

A peptide sequence from mouse tissue factor inhibits human tissue factor dependent factor X activation

artículo científico publicado en 1998

A quantitative study of the in vitro binding of the C-terminal domain of p21 to PCNA: affinity, stoichiometry, and thermodynamics

artículo científico publicado en 2000

A versatile polymer-supported 4-(4-Methylphenyl(chloro)methyl)phenoxy linker for solid-phase synthesis of pseudopeptides

scientific article published on 01 August 2000

Active site pressurization: a new tool for structure-guided drug design and other studies of protein flexibility.

artículo científico publicado en 2008

Analysis of 4-N,N-dimethylaminoazobenzene 4'-thiohydantoin amino acids at sub-picomole levels by high-performance liquid chromatography: simultaneous manual sequencing of picomole quantities of several polypeptides

artículo científico publicado en 1989

Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor.

artículo científico publicado en 2005

Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B.

artículo científico publicado en 2018

CDK inhibitors in clinical development for the treatment of cancer

artículo científico publicado en 2003

CDK versus GSK-3 inhibition: a purple haze no longer?

artículo científico publicado en 2003

CDKI-71, a novel CDK9 inhibitor, is preferentially cytotoxic to cancer cells compared to flavopiridol.

artículo científico publicado en 2011

CNIO cancer conference: targeted search for anticancer drugs

Cellular delivery of impermeable effector molecules in the form of conjugates with peptides capable of mediating membrane translocation.

artículo científico publicado en 2001

Cellular uptake mechanisms and potential therapeutic utility of peptidic cell delivery vectors: progress 2001-2006.

artículo científico publicado en 2007

Classical anticytokinins do not interact with cytokinin receptors but inhibit cyclin-dependent kinases

artículo científico publicado en 2007

Coagulation factor XII protease domain crystal structure.

artículo científico publicado en 2015

Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity

artículo científico publicado en 2013

Computational chemistry approaches to drug discovery in signal transduction.

artículo científico publicado en 2008

Crystallographic and mass spectrometric characterisation of eIF4E with N7-alkylated cap derivatives

artículo científico publicado en 2007

Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology.

artículo científico publicado en 2008

Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs

artículo científico publicado en 2017

Design of low molecular weight hematoregulatory agents from the structure-activity relationship of a dimeric pentapeptide

artículo científico publicado en 1997

Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents

artículo científico publicado en 2021

Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

artículo científico publicado en 2014

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors

artículo científico publicado en 2011

Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors

artículo científico publicado en 2010

Design, synthesis, and structure-activity relationship exploration of 1-substituted 4-aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one analogues as inhibitors of the annexin A2-S100A10 protein interaction.

artículo científico publicado en 2011

Design, synthesis, biological activity and structural analysis of cyclic peptide inhibitors targeting the substrate recruitment site of cyclin-dependent kinase complexes

scientific article published on 09 September 2004

Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines

artículo científico publicado en 2011

Development of a simple and sensitive HPLC-UV method for the simultaneous determination of cannabidiol and Δ(9)-tetrahydrocannabinol in rat plasma.

artículo científico publicado en 2015

Differential Binding of Inhibitors to Active and Inactive CDK2 Provides Insights for Drug Design

artículo científico publicado en 2006

Diketopiperazines in peptide and combinatorial chemistry.

artículo científico publicado en 2003

Direct enzyme-linked immunosorbent assay of anti-peptide antibodies using capture of biotinylated peptides by immobilized avidin

artículo científico publicado en 1990

Direct immunization with synthetic peptidyl-polyamide resin. Comparison with antibody production from free peptide and conjugates with carrier proteins

artículo científico publicado en 1989

Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents ⬇️

artículo científico publicado el 29 de octubre de 2010

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors

artículo científico publicado en 2010

Discovery of a novel family of CDK inhibitors with the program LIDAEUS: structural basis for ligand-induced disordering of the activation loop

artículo científico publicado en 2003

Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1.

artículo científico publicado en 2015

Efficient Palladium-Catalyzed Cross-Coupling of β-Chloroalkylidene/arylidene Malonates Using Microwave Chemistry

scientific article published on 01 October 2004

End-stapled homo and hetero collagen triple helices: a click chemistry approach

artículo científico publicado en 2011

Exploiting glycogen synthase kinase 3beta flexibility in molecular recognition

artículo científico publicado en 2008

GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors.

artículo científico publicado en 2016

Highly potent p21(WAF1)-derived peptide inhibitors of CDK-mediated pRb phosphorylation: delineation and structural insight into their interactions with cyclin A

artículo científico publicado en 2002

Immunosuppressive but non-LasR-inducing analogues of the Pseudomonas aeruginosa quorum-sensing molecule N-(3-oxododecanoyl)-l-homoserine lactone

scientific article published on 13 April 2011

In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)

artículo científico publicado en 2002

In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.

artículo científico publicado en 2005

In vitro antitumor mechanism of a novel cyclin-dependent kinase inhibitor CDKI-83.

artículo científico publicado en 2011

Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance

artículo científico publicado en 2006

Insights into cyclin groove recognition: complex crystal structures and inhibitor design through ligand exchange

artículo científico publicado en 2003

Investigation of the flexibility of protein kinases implicated in the pathology of Alzheimer's disease.

artículo científico publicado en 2014

Linear analogues derived from the first EGF-like domain of human blood coagulation factor VII: enhanced inhibition of FVIIa/TF complex activity by backbone modification through aspartimide formation

artículo científico publicado en 1999

Liquid-phase peptide synthesis on polyethylene glycol (PEG) supports using strategies based on the 9-fluorenylmethoxycarbonyl amino protecting group: application of PEGylated peptides in biochemical assays

artículo científico publicado en 2002

Long-Term Amorphous Drug Stability Predictions Using Easily Calculated, Predicted, and Measured Parameters

artículo científico publicado en 2015

Multiple Linear Regression Modeling To Predict the Stability of Polymer-Drug Solid Dispersions: Comparison of the Effects of Polymers and Manufacturing Methods on Solid Dispersion Stability

artículo científico publicado en 2018

New lupane derived compounds with pro-apoptotic activity in cancer cells: synthesis and structure-activity relationships

artículo científico publicado en 2003

Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice

artículo científico publicado en 2013

PPP1R15A-mediated dephosphorylation of eIF2α is unaffected by Sephin1 or Guanabenz.

artículo científico publicado en 2017

Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity

artículo científico publicado en 2015

Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe.

artículo científico publicado en 2002

Peptide, Peptidomimetic, and Small-molecule Antagonists of the p53-HDM2 Protein-Protein Interaction.

artículo científico publicado en 2006

Peptidomimetic design of CDK inhibitors targeting the recruitment site of the cyclin subunit

artículo científico publicado en 2003

Pharmacological targeting of lysine acetyltransferases in human disease: a progress report.

artículo científico publicado en 2006

Progress in the discovery of polo-like kinase inhibitors.

artículo científico publicado en 2005

REPLACE: a strategy for iterative design of cyclin-binding groove inhibitors.

artículo científico publicado en 2006

Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human beta1-adrenoceptor.

artículo científico publicado en 2008

Small molecules that bind the Mdm2 RING stabilize and activate p53.

artículo científico publicado en 2012

Small-molecule inhibitors of MDM2 as new anticancer therapeutics

artículo científico publicado en 2009

Small-molecule inhibitors of the p53 suppressor HDM2: have protein-protein interactions come of age as drug targets?

artículo científico publicado en 2004

Strategies for the design of potent and selective kinase inhibitors.

artículo científico publicado en 2005

Stress responses. Mutations in a translation initiation factor identify the target of a memory-enhancing compound

artículo científico publicado en 2015

Structural and biochemical studies of human proliferating cell nuclear antigen complexes provide a rationale for cyclin association and inhibitor design

artículo científico publicado en 2005

Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.

artículo científico publicado en 2004

Structure of free MDM2 N-terminal domain reveals conformational adjustments that accompany p53-binding.

artículo científico publicado en 2005

Structure-activity relationship of truncated and substituted analogues of the intracellular delivery vector Penetratin

scientific article published on 01 February 2000

Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors

artículo científico publicado en 2004

Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin.

artículo científico publicado en 2006

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

artículo científico publicado en 2013

Synthesis, biological activity, and solution structures of a cyclic dodecapeptide from the EGF-2 domain of blood coagulation factor VII.

artículo científico publicado en 2001

Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.

artículo científico publicado en 2013

Synthetic lethal targeting of DNA double-strand break repair deficient cells by human apurinic/apyrimidinic endonuclease inhibitors

artículo científico publicado en 2012

Synthetic peptide antigens of tetanus toxin

artículo científico publicado en 1994

The design, synthesis and application of stereochemical and directional peptide isomers: a critical review

artículo científico publicado en 2003

Three-dimensional pharmacophore design and biochemical screening identifies substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

artículo científico publicado en 2012

Turning down tau phosphorylation.

artículo científico publicado en 2008

Turning the key on p53.

artículo científico publicado en 2004

Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases.

artículo científico publicado en 2007

Lista de obras de Peter M. Fischer

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity

2-[(1-methylpropyl)dithio]-1H-imidazole inhibits tubulin polymerization through cysteine oxidation.

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

A Cy5-labeled S100A10 tracer used to identify inhibitors of the protein interaction with annexin A2.

A facile approach to tryptophan derivatives for the total synthesis of argyrin analogues

A fluorescence-based assay suitable for quantitative analysis of deadenylase enzyme activity.

A novel nucleoside rescue metabolic pathway may be responsible for therapeutic effect of orally administered cordycepin

A peptide sequence from mouse tissue factor inhibits human tissue factor dependent factor X activation

A quantitative study of the in vitro binding of the C-terminal domain of p21 to PCNA: affinity, stoichiometry, and thermodynamics

A versatile polymer-supported 4-(4-Methylphenyl(chloro)methyl)phenoxy linker for solid-phase synthesis of pseudopeptides

Active site pressurization: a new tool for structure-guided drug design and other studies of protein flexibility.

Analysis of 4-N,N-dimethylaminoazobenzene 4'-thiohydantoin amino acids at sub-picomole levels by high-performance liquid chromatography: simultaneous manual sequencing of picomole quantities of several polypeptides

Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor.

Binding of ISRIB reveals a regulatory site in the nucleotide exchange factor eIF2B.

CDK inhibitors in clinical development for the treatment of cancer

CDK versus GSK-3 inhibition: a purple haze no longer?

CDKI-71, a novel CDK9 inhibitor, is preferentially cytotoxic to cancer cells compared to flavopiridol.

CNIO cancer conference: targeted search for anticancer drugs

Cellular delivery of impermeable effector molecules in the form of conjugates with peptides capable of mediating membrane translocation.

Cellular uptake mechanisms and potential therapeutic utility of peptidic cell delivery vectors: progress 2001-2006.

Classical anticytokinins do not interact with cytokinin receptors but inhibit cyclin-dependent kinases

Coagulation factor XII protease domain crystal structure.

Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity

Computational chemistry approaches to drug discovery in signal transduction.

Crystallographic and mass spectrometric characterisation of eIF4E with N7-alkylated cap derivatives

Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology.

Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs

Design of low molecular weight hematoregulatory agents from the structure-activity relationship of a dimeric pentapeptide

Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents

Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors

Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors

Design, synthesis, and structure-activity relationship exploration of 1-substituted 4-aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one analogues as inhibitors of the annexin A2-S100A10 protein interaction.

Design, synthesis, biological activity and structural analysis of cyclic peptide inhibitors targeting the substrate recruitment site of cyclin-dependent kinase complexes

Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines

Development of a simple and sensitive HPLC-UV method for the simultaneous determination of cannabidiol and Δ(9)-tetrahydrocannabinol in rat plasma.

Differential Binding of Inhibitors to Active and Inactive CDK2 Provides Insights for Drug Design

Diketopiperazines in peptide and combinatorial chemistry.

Direct enzyme-linked immunosorbent assay of anti-peptide antibodies using capture of biotinylated peptides by immobilized avidin

Direct immunization with synthetic peptidyl-polyamide resin. Comparison with antibody production from free peptide and conjugates with carrier proteins

Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents ⬇️

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors

Discovery of a novel family of CDK inhibitors with the program LIDAEUS: structural basis for ligand-induced disordering of the activation loop

Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1.

Efficient Palladium-Catalyzed Cross-Coupling of β-Chloroalkylidene/arylidene Malonates Using Microwave Chemistry

End-stapled homo and hetero collagen triple helices: a click chemistry approach

Exploiting glycogen synthase kinase 3beta flexibility in molecular recognition

GPCRs through the keyhole: the role of protein flexibility in ligand binding to β-adrenoceptors.

Highly potent p21(WAF1)-derived peptide inhibitors of CDK-mediated pRb phosphorylation: delineation and structural insight into their interactions with cyclin A

Immunosuppressive but non-LasR-inducing analogues of the Pseudomonas aeruginosa quorum-sensing molecule N-(3-oxododecanoyl)-l-homoserine lactone

In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)

In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.

In vitro antitumor mechanism of a novel cyclin-dependent kinase inhibitor CDKI-83.

Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance

Insights into cyclin groove recognition: complex crystal structures and inhibitor design through ligand exchange

Investigation of the flexibility of protein kinases implicated in the pathology of Alzheimer's disease.

Linear analogues derived from the first EGF-like domain of human blood coagulation factor VII: enhanced inhibition of FVIIa/TF complex activity by backbone modification through aspartimide formation

Liquid-phase peptide synthesis on polyethylene glycol (PEG) supports using strategies based on the 9-fluorenylmethoxycarbonyl amino protecting group: application of PEGylated peptides in biochemical assays

Long-Term Amorphous Drug Stability Predictions Using Easily Calculated, Predicted, and Measured Parameters

Multiple Linear Regression Modeling To Predict the Stability of Polymer-Drug Solid Dispersions: Comparison of the Effects of Polymers and Manufacturing Methods on Solid Dispersion Stability

New lupane derived compounds with pro-apoptotic activity in cancer cells: synthesis and structure-activity relationships

Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice

PPP1R15A-mediated dephosphorylation of eIF2α is unaffected by Sephin1 or Guanabenz.

Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity

Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe.

Peptide, Peptidomimetic, and Small-molecule Antagonists of the p53-HDM2 Protein-Protein Interaction.

Peptidomimetic design of CDK inhibitors targeting the recruitment site of the cyclin subunit

Pharmacological targeting of lysine acetyltransferases in human disease: a progress report.

Progress in the discovery of polo-like kinase inhibitors.

REPLACE: a strategy for iterative design of cyclin-binding groove inhibitors.

Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human beta1-adrenoceptor.

Small molecules that bind the Mdm2 RING stabilize and activate p53.

Small-molecule inhibitors of MDM2 as new anticancer therapeutics

Small-molecule inhibitors of the p53 suppressor HDM2: have protein-protein interactions come of age as drug targets?

Strategies for the design of potent and selective kinase inhibitors.

Stress responses. Mutations in a translation initiation factor identify the target of a memory-enhancing compound

Structural and biochemical studies of human proliferating cell nuclear antigen complexes provide a rationale for cyclin association and inhibitor design

Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.