List of works - Peter M. Fischer

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

scientific article published on March 2004

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

scientific article

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

scientific article published on November 2006

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

scientific article published on 25 September 2013

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

scientific article

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

scientific article published in December 2014

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

scientific article

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

scientific article published on 31 October 2019

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

scientific article published on 01 November 1998

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

scientific article published on 01 June 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.

scientific article

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

scientific article published on 01 February 1989

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

scientific article published on August 2005

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

scientific article published in March 2018

CDK inhibitors in clinical development for the treatment of cancer

scientific article

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

scientific article

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

scientific article published on 21 June 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.

scientific article

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

scientific article published on November 2007

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

scientific article published on 5 March 2007

Coagulation factor XII protease domain crystal structure.

scientific article

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

scientific article

Computational chemistry approaches to drug discovery in signal transduction.

scientific article published on April 2008

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

scientific article

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

scientific article published on 16 April 2008

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

scientific article published on 26 October 2017

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

scientific article published on August 1997

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

scientific article published in June 2021

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

scientific article published on 7 August 2014

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

scientific article published on 31 August 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

scientific article

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.

scientific article published on 4 March 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

scientific article

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

scientific article published on 22 May 2015

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

scientific article published on 01 February 2006

Diketopiperazines in peptide and combinatorial chemistry.

scientific article

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

scientific article published in January 1990

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

scientific article published on 01 March 1989

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

scientific article published on October 29, 2010

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

scientific article

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

scientific article (publication date: April 2003)

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

scientific article

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

scientific article

Exploiting glycogen synthase kinase 3beta flexibility in molecular recognition

scientific article published on 01 February 2008

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

scientific article published on 17 August 2016

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

scientific article published on 01 November 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)

scientific article published on 01 December 2002

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

scientific article published on July 2005

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

scientific article published on 18 February 2011

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

scientific article published on 8 October 2006

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

scientific article

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

scientific article

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

scientific article published on 01 July 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

scientific article published in September 2002

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

scientific article published on 3 August 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

scientific article published on 29 March 2018

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

scientific article published on December 2003

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

scientific article

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

scientific article published on 27 April 2017

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

scientific article

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

scientific article published in September 2002

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

scientific article published on 15 March 2006

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

scientific article

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

scientific article published on December 2006

Progress in the discovery of polo-like kinase inhibitors.

scientific article

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

scientific article

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

scientific article published on 7 August 2008

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

scientific article published on 2 February 2012

Small-molecule inhibitors of MDM2 as new anticancer therapeutics

scientific article

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

scientific article published in July 2004

Strategies for the design of potent and selective kinase inhibitors.

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article published on August 2004

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

scientific article published on 2 March 2006

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

scientific article published on 10 May 2013

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

scientific article

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

scientific article published on 15 September 2013

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

scientific article published on 28 March 2012

Synthetic peptide antigens of tetanus toxin

scientific article published on 01 October 1994

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

scientific article (publication date: October 2003)

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

scientific article published on 29 May 2012

Turning down tau phosphorylation.

scientific article published on August 2008

Turning the key on p53.

scientific article published in February 2004

Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases.

scientific article published on June 2007

List of works by 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.