List of works - Jane A Endicott

4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.

scientific article published on January 2003

8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode

scientific article

A code for RanGDP binding in ankyrin repeats defines a nuclear import pathway

scientific article

A new crystal form of Lys48-linked diubiquitin

scientific article

All change: protein conformation and the ubiquitination reaction cascade ⬇️

scientific article published on March 17, 2009

Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects

scientific article published in January 2003

An inhibitor's-eye view of the ATP-binding site of CDKs in different regulatory states.

scientific article

Analysis of chemical shift changes reveals the binding modes of isoindolinone inhibitors of the MDM2-p53 interaction

scientific article published in November 2008

Budding yeast Dsk2 protein forms a homodimer via its C-terminal UBA domain

scientific article published in October 2005

CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells

scientific article

CDK1 structures reveal conserved and unique features of the essential cell cycle CDK.

scientific article published on 13 April 2015

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

Complete cDNA sequences encoding the Chinese hamster P-glycoprotein gene family ⬇️

scientific article published on January 1, 1991

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.

scientific article published on 22 December 2016

Cyclin-dependent kinase homologues of Plasmodium falciparum

scientific article

Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition

scientific article published on 21 November 2018

Differential Regulation of G1 CDK Complexes by the Hsp90-Cdc37 Chaperone System.

scientific article published in October 2017

Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity

scientific article

Exploiting structural principles to design cyclin-dependent kinase inhibitors.

scientific article

FragLites-Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation

scientific article published on 26 March 2019

Halogen bonds form the basis for selective P-TEFb inhibition by DRB

scientific article

How tyrosine 15 phosphorylation inhibits the activity of cyclin-dependent kinase 2-cyclin A.

scientific article published on 9 November 2006

Identification and Characterization of an Irreversible Inhibitor of CDK2.

scientific article published on 27 August 2015

Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach.

scientific article published on 22 February 2018

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4

scientific article published on 25 May 2019

Inhibition of the cell cycle with chemical inhibitors: a targeted approach.

scientific article

Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency

scientific article published on 11 February 2011

MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.

scientific article

Mechanism of Lys48-linked polyubiquitin chain recognition by the Mud1 UBA domain

scientific article published on September 2005

Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.

scientific article published on 31 January 2008

Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases

scientific article

Methods for preparation of proteins and protein complexes that regulate the eukaryotic cell cycle for structural studies.

scientific article

Molecular basis for the recognition of phosphorylated and phosphoacetylated histone h3 by 14-3-3

scientific article

N-&-N, a new class of cell death-inducing kinase inhibitors derived from the purine roscovitine

scientific article

N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2

scientific article

Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives

scientific article

Protein kinase inhibitors: insights into drug design from structure.

scientific article published on March 2004

Protein kinases as targets for antimalarial intervention: Kinomics, structure-based design, transmission-blockade, and targeting host cell enzymes

scientific article

Recent developments in cyclin-dependent kinase biochemical and structural studies.

scientific article published on 12 October 2009

Restoring p53 Function in Human Melanoma Cells by Inhibiting MDM2 and Cyclin B1/CDK1-Phosphorylated Nuclear iASPP.

scientific article

Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP

scientific article

Structural and functional characterization of Rpn12 identifies residues required for Rpn10 proteasome incorporation

scientific article

Structural characterization of the cyclin-dependent protein kinase family ⬇️

scientific article published on August 1, 2013

Structural insights into the functional diversity of the CDK-cyclin family

scientific article published on 01 September 2018

Structural principles in cell-cycle control: beyond the CDKs ⬇️

scientific article published on May 15, 1998

Structural studies with inhibitors of the cell cycle regulatory kinase cyclin-dependent protein kinase 2.

scientific article

Structure of Rpn10 and Its Interactions with Polyubiquitin Chains and the Proteasome Subunit Rpn12

scientific article

Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2

scientific article published on 23 April 2007

Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2

scientific article

Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor

scientific article

Structure-based design of cyclin-dependent kinase inhibitors

scientific article

Structure-based discovery of cyclin-dependent protein kinase inhibitors.

scientific article published on 8 November 2017

Structures of P. falciparum PfPK5 test the CDK regulation paradigm and suggest mechanisms of small molecule inhibition

scientific article

Structures of P. falciparum protein kinase 7 identify an activation motif and leads for inhibitor design

scientific article

Structures of the Dsk2 UBL and UBA domains and their complex

scientific article

Substituted 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X-ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities

scientific article

The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508

scientific article

The CDK9 Tail Determines the Reaction Pathway of Positive Transcription Elongation Factor b

scientific article

The role of structure in kinase-targeted inhibitor design.

scientific article published in July 2004

The structural basis for control of eukaryotic protein kinases

scientific article published on 05 April 2012

The structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant

scientific article

The ubiquitin-associated (UBA) 1 domain of Schizosaccharomyces pombe Rhp23 is essential for the recognition of ubiquitin-proteasome system substrates both in vitro and in vivo

scientific article published on 4 October 2012

Understanding small-molecule binding to MDM2: insights into structural effects of isoindolinone inhibitors from NMR spectroscopy

scientific article published on March 2011

List of works by Jane A Endicott

4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2.

8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode

A code for RanGDP binding in ankyrin repeats defines a nuclear import pathway

A new crystal form of Lys48-linked diubiquitin

All change: protein conformation and the ubiquitination reaction cascade ⬇️

Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects

An inhibitor's-eye view of the ATP-binding site of CDKs in different regulatory states.

Analysis of chemical shift changes reveals the binding modes of isoindolinone inhibitors of the MDM2-p53 interaction

Budding yeast Dsk2 protein forms a homodimer via its C-terminal UBA domain

CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells

CDK1 structures reveal conserved and unique features of the essential cell cycle CDK.

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

Complete cDNA sequences encoding the Chinese hamster P-glycoprotein gene family ⬇️

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.

Cyclin-dependent kinase homologues of Plasmodium falciparum

Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition

Differential Regulation of G1 CDK Complexes by the Hsp90-Cdc37 Chaperone System.

Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity

Exploiting structural principles to design cyclin-dependent kinase inhibitors.

FragLites-Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation

Halogen bonds form the basis for selective P-TEFb inhibition by DRB

How tyrosine 15 phosphorylation inhibits the activity of cyclin-dependent kinase 2-cyclin A.

Identification and Characterization of an Irreversible Inhibitor of CDK2.

Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach.

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4

Inhibition of the cell cycle with chemical inhibitors: a targeted approach.

Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency

MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.

Mechanism of Lys48-linked polyubiquitin chain recognition by the Mud1 UBA domain

Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.

Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases

Methods for preparation of proteins and protein complexes that regulate the eukaryotic cell cycle for structural studies.

Molecular basis for the recognition of phosphorylated and phosphoacetylated histone h3 by 14-3-3

N-&-N, a new class of cell death-inducing kinase inhibitors derived from the purine roscovitine

N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2

Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives

Protein kinase inhibitors: insights into drug design from structure.

Protein kinases as targets for antimalarial intervention: Kinomics, structure-based design, transmission-blockade, and targeting host cell enzymes

Recent developments in cyclin-dependent kinase biochemical and structural studies.

Restoring p53 Function in Human Melanoma Cells by Inhibiting MDM2 and Cyclin B1/CDK1-Phosphorylated Nuclear iASPP.

Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP

Structural and functional characterization of Rpn12 identifies residues required for Rpn10 proteasome incorporation

Structural characterization of the cyclin-dependent protein kinase family ⬇️

Structural insights into the functional diversity of the CDK-cyclin family

Structural principles in cell-cycle control: beyond the CDKs ⬇️

Structural studies with inhibitors of the cell cycle regulatory kinase cyclin-dependent protein kinase 2.

Structure of Rpn10 and Its Interactions with Polyubiquitin Chains and the Proteasome Subunit Rpn12

Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2

Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2

Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor

Structure-based design of cyclin-dependent kinase inhibitors

Structure-based discovery of cyclin-dependent protein kinase inhibitors.

Structures of P. falciparum PfPK5 test the CDK regulation paradigm and suggest mechanisms of small molecule inhibition

Structures of P. falciparum protein kinase 7 identify an activation motif and leads for inhibitor design

Structures of the Dsk2 UBL and UBA domains and their complex

Substituted 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X-ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities

The CDK9 C-helix Exhibits Conformational Plasticity That May Explain the Selectivity of CAN508

The CDK9 Tail Determines the Reaction Pathway of Positive Transcription Elongation Factor b

The role of structure in kinase-targeted inhibitor design.

The structural basis for control of eukaryotic protein kinases

The structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant

The ubiquitin-associated (UBA) 1 domain of Schizosaccharomyces pombe Rhp23 is essential for the recognition of ubiquitin-proteasome system substrates both in vitro and in vivo

Understanding small-molecule binding to MDM2: insights into structural effects of isoindolinone inhibitors from NMR spectroscopy