List of works - Gerard Drewes

2,4-Dinitrophenyl [14C]cysteinyl disulfide allows selective radioactive labeling of protein thiols under spectrophotometric control

scientific article published on 01 July 1990

A physical and functional map of the human TNF-alpha/NF-kappa B signal transduction pathway

scientific article

A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation

scientific article

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

scientific article

Affinity profiling of the cellular kinome for the nucleotide cofactors ATP, ADP, and GTP.

scientific article published on 7 January 2013

Alzheimer-like paired helical filaments and antiparallel dimers formed from microtubule-associated protein tau in vitro ⬇️

scientific article published on August 1, 1992

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

scientific article

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

scientific article

CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model

scientific article published on 01 April 2020

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives

scientific article

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives

scientific article published on 15 January 2016

Chemical and pathway proteomics: powerful tools for oncology drug discovery and personalized health care.

scientific article published on August 2008

Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.

scientific article published on 23 August 2012

Chemical proteomics in drug discovery.

scientific article

Chemoproteomic approaches to drug target identification and drug profiling.

scientific article

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

scientific article

Chemoproteomics reveals time-dependent binding of histone deacetylase inhibitors to endogenous repressor complexes

scientific article published on 6 June 2014

Chemoproteomics-based kinome profiling and target deconvolution of clinical multi-kinase inhibitors in primary chronic lymphocytic leukemia cells.

scientific article

Click chemistry enables preclinical evaluation of targeted epigenetic therapies.

scientific article published on 15 June 2017

Cloning and sequencing of a cDNA encoding rat brain mitogen-activated protein (MAP) kinase activator.

scientific article

Collaborative approaches for Target ID in neglected diseases: identifying new antimalarial targets.

scientific article published on 22 September 2014

Comprehensive proteomic analysis of human Par protein complexes reveals an interconnected protein network

scientific article

Cooperative effects on filament stability in actin modified at the C-terminus by substitution or truncation

scientific article published on 01 February 1993

Correction to The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

scientific article

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

scientific article

Discovery of Novel Small Molecules that Activate Satellite Cell Proliferation and Enhance Repair of Damaged Muscle.

scientific article published on 22 December 2015

Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.

scientific article

Essential but not vulnerable: indazole sulfonamides targeting inosine monophosphate dehydrogenase as potential leads against Mycobacterium tuberculosis

scientific article

Functional interdependence of BRD4 and DOT1L in MLL leukemia

scientific article published on 13 June 2016

Functional organization of the yeast proteome by systematic analysis of protein complexes

scientific article

Hsp90 inhibition differentially destabilises MAP kinase and TGF-beta signalling components in cancer cells revealed by kinase-targeted chemoproteomics

scientific article

Human Proteinpedia enables sharing of human protein data

scientific article

Identification of KasA as the cellular target of an anti-tubercular scaffold

scientific article

Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

scientific article published on 22 September 2014

Increased expression of BIN1 mediates Alzheimer genetic risk by modulating tau pathology

scientific article

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

scientific article

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

scientific article published on 26 January 2015

Interactions of MAP/microtubule affinity regulating kinases with the adaptor complex AP-2 of clathrin-coated vesicles

scientific article published in August 2009

Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics

article

Kruidenier et al. reply

scientific article published in Nature

MAPs, MARKs and microtubule dynamics.

scientific article published in August 1998

MARK, a novel family of protein kinases that phosphorylate microtubule-associated proteins and trigger microtubule disruption

scientific article

MARK4 is a novel microtubule-associated proteins/microtubule affinity-regulating kinase that binds to the cellular microtubule network and to centrosomes

scientific article

MARKing tau for tangles and toxicity.

scientific article published in October 2004

Microtubule affinity-regulating kinase 2 functions downstream of the PAR-3/PAR-6/atypical PKC complex in regulating hippocampal neuronal polarity

scientific article

Microtubule-Affinity Regulating Kinase (MARK) Is Tightly Associated with Neurofibrillary Tangles in Alzheimer Brain: A Fluorescence Resonance Energy Transfer Study

scientific article published on 01 November 2000

Microtubule-associated protein tau, paired helical filaments, and phosphorylation.

scientific article

Microtubule-associated protein/microtubule affinity-regulating kinase (p110mark). A novel protein kinase that regulates tau-microtubule interactions and dynamic instability by phosphorylation at the Alzheimer-specific site serine 262

scientific article

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia

scientific article

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.

scientific article published on 17 November 2017

Pathway proteomics and chemical proteomics team up in drug discovery.

scientific article published on January 2007

Phosphorylation of Ser262 strongly reduces binding of tau to microtubules: distinction between PHF-like immunoreactivity and microtubule binding.

scientific article published in July 1993

Phosphorylation of microtubule-associated proteins MAP2 and MAP4 by the protein kinase p110mark. Phosphorylation sites and regulation of microtubule dynamics

scientific article

Probing the phalloidin binding site of actin

scientific article published on 01 March 1993

Proteome survey reveals modularity of the yeast cell machinery

scientific article

Proteomics-based strategies in kinase drug discovery

scientific article published on 01 January 2007

Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

scientific article

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

scientific article published on 13 November 2013

Running in the family

scientific article published on 06 July 2014

Screening Pools of Compounds against Multiple Endogenously Expressed Targets in a Chemoproteomics Binding Assay.

scientific article published on 13 July 2015

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

scientific article

Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor

scientific article

THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria

scientific article

Tau domains, phosphorylation, and interactions with microtubules.

scientific article

Tau interactome mapping based identification of Otub1 as Tau deubiquitinase involved in accumulation of pathological Tau forms in vitro and in vivo

scientific article

The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

scientific article published on 14 August 2017

The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains

scientific article

The frontotemporal dementia mutation R406W blocks tau's interaction with the membrane in an annexin A2-dependent manner.

scientific article

The protein kinase kin1, the fission yeast orthologue of mammalian MARK/PAR-1, localises to new cell ends after mitosis and is important for bipolar growth

scientific article published on 01 November 2003

Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry.

scientific article published on 17 September 2015

Thermal proteome profiling monitors ligand interactions with cellular membrane proteins.

scientific article published on 2 November 2015

Tracking cancer drugs in living cells by thermal profiling of the proteome

scientific article

Transgenic mouse proteomics identifies new 14-3-3-associated proteins involved in cytoskeletal rearrangements and cell signaling

scientific article

List of works by Gerard Drewes

2,4-Dinitrophenyl [14C]cysteinyl disulfide allows selective radioactive labeling of protein thiols under spectrophotometric control

A physical and functional map of the human TNF-alpha/NF-kappa B signal transduction pathway

A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

Affinity profiling of the cellular kinome for the nucleotide cofactors ATP, ADP, and GTP.

Alzheimer-like paired helical filaments and antiparallel dimers formed from microtubule-associated protein tau in vitro ⬇️

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives

Chemical and pathway proteomics: powerful tools for oncology drug discovery and personalized health care.

Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.

Chemical proteomics in drug discovery.

Chemoproteomic approaches to drug target identification and drug profiling.

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

Chemoproteomics reveals time-dependent binding of histone deacetylase inhibitors to endogenous repressor complexes

Chemoproteomics-based kinome profiling and target deconvolution of clinical multi-kinase inhibitors in primary chronic lymphocytic leukemia cells.

Click chemistry enables preclinical evaluation of targeted epigenetic therapies.

Cloning and sequencing of a cDNA encoding rat brain mitogen-activated protein (MAP) kinase activator.

Collaborative approaches for Target ID in neglected diseases: identifying new antimalarial targets.

Comprehensive proteomic analysis of human Par protein complexes reveals an interconnected protein network

Cooperative effects on filament stability in actin modified at the C-terminus by substitution or truncation

Correction to The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

Discovery of Novel Small Molecules that Activate Satellite Cell Proliferation and Enhance Repair of Damaged Muscle.

Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.

Essential but not vulnerable: indazole sulfonamides targeting inosine monophosphate dehydrogenase as potential leads against Mycobacterium tuberculosis

Functional interdependence of BRD4 and DOT1L in MLL leukemia

Functional organization of the yeast proteome by systematic analysis of protein complexes

Hsp90 inhibition differentially destabilises MAP kinase and TGF-beta signalling components in cancer cells revealed by kinase-targeted chemoproteomics

Human Proteinpedia enables sharing of human protein data

Identification of KasA as the cellular target of an anti-tubercular scaffold

Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

Increased expression of BIN1 mediates Alzheimer genetic risk by modulating tau pathology

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

Interactions of MAP/microtubule affinity regulating kinases with the adaptor complex AP-2 of clathrin-coated vesicles

Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics

Kruidenier et al. reply

MAPs, MARKs and microtubule dynamics.

MARK, a novel family of protein kinases that phosphorylate microtubule-associated proteins and trigger microtubule disruption

MARK4 is a novel microtubule-associated proteins/microtubule affinity-regulating kinase that binds to the cellular microtubule network and to centrosomes

MARKing tau for tangles and toxicity.

Microtubule affinity-regulating kinase 2 functions downstream of the PAR-3/PAR-6/atypical PKC complex in regulating hippocampal neuronal polarity

Microtubule-Affinity Regulating Kinase (MARK) Is Tightly Associated with Neurofibrillary Tangles in Alzheimer Brain: A Fluorescence Resonance Energy Transfer Study

Microtubule-associated protein tau, paired helical filaments, and phosphorylation.

Microtubule-associated protein/microtubule affinity-regulating kinase (p110mark). A novel protein kinase that regulates tau-microtubule interactions and dynamic instability by phosphorylation at the Alzheimer-specific site serine 262

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.

Pathway proteomics and chemical proteomics team up in drug discovery.

Phosphorylation of Ser262 strongly reduces binding of tau to microtubules: distinction between PHF-like immunoreactivity and microtubule binding.

Phosphorylation of microtubule-associated proteins MAP2 and MAP4 by the protein kinase p110mark. Phosphorylation sites and regulation of microtubule dynamics

Probing the phalloidin binding site of actin

Proteome survey reveals modularity of the yeast cell machinery

Proteomics-based strategies in kinase drug discovery

Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

Running in the family

Screening Pools of Compounds against Multiple Endogenously Expressed Targets in a Chemoproteomics Binding Assay.

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor

THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria

Tau domains, phosphorylation, and interactions with microtubules.

Tau interactome mapping based identification of Otub1 as Tau deubiquitinase involved in accumulation of pathological Tau forms in vitro and in vivo

The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains

The frontotemporal dementia mutation R406W blocks tau's interaction with the membrane in an annexin A2-dependent manner.

The protein kinase kin1, the fission yeast orthologue of mammalian MARK/PAR-1, localises to new cell ends after mitosis and is important for bipolar growth

Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry.

Thermal proteome profiling monitors ligand interactions with cellular membrane proteins.

Tracking cancer drugs in living cells by thermal profiling of the proteome

Transgenic mouse proteomics identifies new 14-3-3-associated proteins involved in cytoskeletal rearrangements and cell signaling