Search Results - "Endicott, Jane"

Structural insights into the functional diversity of the CDK–cyclin family by Wood, Daniel J., Endicott, Jane A.

“…Since their characterization as conserved modules that regulate progression through the eukaryotic cell cycle, cyclin-dependent protein kinases (CDKs) in…”
Get full text

The Structural Basis for Control of Eukaryotic Protein Kinases by Endicott, Jane A, Noble, Martin E.M, Johnson, Louise N

“…Eukaryotic protein kinases are key regulators of cell processes. Comparison of the structures of protein kinase domains, both alone and in complexes, allows…”
Get full text

CDK1 structures reveal conserved and unique features of the essential cell cycle CDK by Brown, Nicholas R., Korolchuk, Svitlana, Martin, Mathew P., Stanley, Will A., Moukhametzianov, Rouslan, Noble, Martin E. M., Endicott, Jane A.

“…CDK1 is the only essential cell cycle CDK in human cells and is required for successful completion of M-phase. It is the founding member of the CDK family and…”
Get full text

Cyclin A and Cks1 promote kinase consensus switching to non-proline-directed CDK1 phosphorylation by al-Rawi, Aymen, Kaye, Edward, Korolchuk, Svitlana, Endicott, Jane A., Ly, Tony

“…Ordered protein phosphorylation by CDKs is a key mechanism for regulating the cell cycle. How temporal order is enforced in mammalian cells remains unclear…”
Get full text

Chatterboxes: the structural and functional diversity of cyclins by Tatum, Natalie J., Endicott, Jane A.

“…Proteins of the cyclin family have divergent sequences and execute diverse roles within the cell while sharing a common fold: the cyclin box domain. Structural…”
Get full text

Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition by Wood, Daniel J, Korolchuk, Svitlana, Tatum, Natalie J, Wang, Lan-Zhen, Endicott, Jane A, Noble, Martin E M, Martin, Mathew P

“…Dysregulation of the cell cycle characterizes many cancer subtypes, providing a rationale for developing cyclin-dependent kinase (CDK) inhibitors. Potent CDK2…”
Get more information

FragLitesMinimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation by Wood, Daniel J, Lopez-Fernandez, J. Daniel, Knight, Leanne E, Al-Khawaldeh, Islam, Gai, Conghao, Lin, Shengying, Martin, Mathew P, Miller, Duncan C, Cano, Céline, Endicott, Jane A, Hardcastle, Ian R, Noble, Martin E. M, Waring, Michael J

“…Identifying ligand binding sites on proteins is a critical step in target-based drug discovery. Current approaches to this require resource-intensive screening…”
Get full text

Cryo-EM structure of the CDK2-cyclin A-CDC25A complex by Rowland, Rhianna J., Korolchuk, Svitlana, Salamina, Marco, Tatum, Natalie J., Ault, James R., Hart, Sam, Turkenburg, Johan P., Blaza, James N., Noble, Martin E. M., Endicott, Jane A.

“…The cell division cycle 25 phosphatases CDC25A, B and C regulate cell cycle transitions by dephosphorylating residues in the conserved glycine-rich loop of…”
Get full text

Structure-based discovery of cyclin-dependent protein kinase inhibitors by Martin, Mathew P, Endicott, Jane A, Noble, Martin E M

“…The cell fate-determining roles played by members of the cyclin-dependent protein kinase (CDK) family explain why their dysregulation can promote proliferative…”
Get more information

Cryo-EM structure of SKP1-SKP2-CKS1 in complex with CDK2-cyclin A-p27KIP1 by Rowland, Rhianna J., Heath, Richard, Maskell, Daniel, Thompson, Rebecca F., Ranson, Neil A., Blaza, James N., Endicott, Jane A., Noble, Martin E. M., Salamina, Marco

“…p27KIP1 (cyclin-dependent kinase inhibitor 1B, p27) is a member of the CIP/KIP family of CDK (cyclin dependent kinase) regulators that inhibit cell cycle CDKs…”
Get full text

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK‑2 Selectivity of 6‑Substituted 2‑Arylaminopurines by Coxon, Christopher R, Anscombe, Elizabeth, Harnor, Suzannah J, Martin, Mathew P, Carbain, Benoit, Golding, Bernard T, Hardcastle, Ian R, Harlow, Lisa K, Korolchuk, Svitlana, Matheson, Christopher J, Newell, David R, Noble, Martin E. M, Sivaprakasam, Mangaleswaran, Tudhope, Susan J, Turner, David M, Wang, Lan Z, Wedge, Stephen R, Wong, Christopher, Griffin, Roger J, Endicott, Jane A, Cano, Céline

“…Purines and related heterocycles substituted at C-2 with 4′-sulfamoylanilino and at C-6 with a variety of groups have been synthesized with the aim of…”
Get full text

Substituted 4‑(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X‑ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities by Shao, Hao, Shi, Shenhua, Huang, Shiliang, Hole, Alison J, Abbas, Abdullahi Y, Baumli, Sonja, Liu, Xiangrui, Lam, Frankie, Foley, David W, Fischer, Peter M, Noble, Martin, Endicott, Jane A, Pepper, Chris, Wang, Shudong

“…Cancer cells often have a high demand for antiapoptotic proteins in order to resist programmed cell death. CDK9 inhibition selectively targets survival…”
Get full text

Recent developments in cyclin-dependent kinase biochemical and structural studies by Echalier, Aude, Endicott, Jane A., Noble, Martin E.M.

“…The cyclin-dependent kinases (CDKs) have been intensely studied because of their involvement in regulating essential cellular activities that include…”
Get full text

Emerging approaches to CDK inhibitor development, a structural perspective by Hope, Ian, Endicott, Jane A, Watt, Jessica E

“…Aberrant activity of the cyclin-dependent kinase family is frequently noted in a number of diseases identifying them as potential targets for drug development…”
Get full text

Structural characterization of the cyclin-dependent protein kinase family by Endicott, Jane A, Noble, Martin E M

“…Structural studies of members of the CDK (cyclin-dependent protein kinase) family have made a significant contribution to our understanding of the regulation…”
Get more information

Differential Regulation of G1 CDK Complexes by the Hsp90-Cdc37 Chaperone System by Hallett, Stephen T., Pastok, Martyna W., Morgan, R. Marc L., Wittner, Anita, Blundell, Katie L.I.M., Felletar, Ildiko, Wedge, Stephen R., Prodromou, Chrisostomos, Noble, Martin E.M., Pearl, Laurence H., Endicott, Jane A.

“…Selective recruitment of protein kinases to the Hsp90 system is mediated by the adaptor co-chaperone Cdc37. We show that assembly of CDK4 and CDK6 into protein…”
Get full text

Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction by Chessari, Gianni, Hardcastle, Ian R, Ahn, Jong Sook, Anil, Burcu, Anscombe, Elizabeth, Bawn, Ruth H, Bevan, Luke D, Blackburn, Timothy J, Buck, Ildiko, Cano, Celine, Carbain, Benoit, Castro, Juan, Cons, Ben, Cully, Sarah J, Endicott, Jane A, Fazal, Lynsey, Golding, Bernard T, Griffin, Roger J, Haggerty, Karen, Harnor, Suzannah J, Hearn, Keisha, Hobson, Stephen, Holvey, Rhian S, Howard, Steven, Jennings, Claire E, Johnson, Christopher N, Lunec, John, Miller, Duncan C, Newell, David R, Noble, Martin E. M, Reeks, Judith, Revill, Charlotte H, Riedinger, Christiane, St. Denis, Jeffrey D, Tamanini, Emiliano, Thomas, Huw, Thompson, Neil T, Vinković, Mladen, Wedge, Stephen R, Williams, Pamela A, Wilsher, Nicola E, Zhang, Bian, Zhao, Yan

“…Inhibition of murine double minute 2 (MDM2)-p53 protein–protein interaction with small molecules has been shown to reactivate p53 and inhibit tumor growth…”
Get full text

Mapping Ligand Interactions of Bromodomains BRD4 and ATAD2 with FragLites and PepLitesHalogenated Probes of Druglike and Peptide-like Molecular Interactions by Davison, Gemma, Martin, Mathew P., Turberville, Shannon, Dormen, Selma, Heath, Richard, Heptinstall, Amy B., Lawson, Marie, Miller, Duncan C., Ng, Yi Min, Sanderson, James N., Hope, Ian, Wood, Daniel J., Cano, Céline, Endicott, Jane A., Hardcastle, Ian R., Noble, Martin E. M., Waring, Michael J.

“…The development of ligands for biological targets is critically dependent on the identification of sites on proteins that bind molecules with high affinity. A…”
Get full text

Protein Kinase Inhibitors: Insights into Drug Design from Structure by Martin E. M. Noble, Endicott, Jane A., Johnson, Louise N.

“…Protein kinases are targets for treatment of a number of diseases. This review focuses on kinase inhibitors that are in the clinic or in clinical trials and…”
Get full text

Discriminative SKP2 Interactions with CDK-Cyclin Complexes Support a Cyclin A-Specific Role in p27KIP1 Degradation by Salamina, Marco, Montefiore, Bailey C., Liu, Mengxi, Wood, Daniel J., Heath, Richard, Ault, James R., Wang, Lan-Zhen, Korolchuk, Svitlana, Baslé, Arnaud, Pastok, Martyna W., Reeks, Judith, Tatum, Natalie J., Sobott, Frank, Arold, Stefan T., Pagano, Michele, Noble, Martin E.M., Endicott, Jane A.

“…[Display omitted] •SKP2 engages a site on the N-terminal lobe of cyclin A.•SKP2 recruits a catalytic CDK2-cyclin A to CDK2-cyclin A-CKS1-p27KIP1-SKP1-SKP2.•The…”
Get full text