Campbell McInnes - Irmo SC, US Shu Liu - Columbia SC, US
Assignee:
University of South Carolina - Columbia SC
International Classification:
G06K 19/16 G06K 19/18 C07K 7/06
US Classification:
703 11, 530330, 702 19
Abstract:
Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
Shudong Wang - Nottingham, GB Christopher Meades - Dundee, GB Gavin Wood - Cupar Fife, GB Janice O'Boyle - Dundee, GB Campbell McInnes - Irmo SC, US Peter Martin Fischer - Beeston, GB
Assignee:
Cyclacel Limited - Dundee
International Classification:
A61K 31/506 C07D 415/00 A61P 35/00 A61P 35/04
US Classification:
5142358, 544122, 51425219, 544295, 544297, 514275
Abstract:
The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.
4-Heteroaryl Pyrimidine Derivatives And Use Thereof As Protein Kinase Inhibitors
Gavin Wood - Cupar Fife, GB Christopher Meades - Dundee, GB Peter Martin Fischer - Nottingham, GB Shudong Wang - Nottingham, GB Kenneth Duncan - Waltham MA, US Daniella I. Zheleva - Fife, GB Campbell Mcinnes - Irmo SC, US Mark Thomas - Dundee, GB
The present invention relates to compounds of formula (I) or formula (II), or pharmaceutically acceptable salts thereof. Further aspects relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
Fragment Ligated Inhibitors Selective For The Polo Box Domain Of Plk1
Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.
Campbell McInnes - Irmo SC, US Shu Liu - West Columbia SC, US
International Classification:
G06F 19/12 C07K 5/11
US Classification:
530330, 530331, 703 11
Abstract:
Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
3-Amino-4-[4-[4 (Dimethylcarbamoyl) Phenyl]-1,4-Diazepan-1-Yl]Thieno[2,3-B]Pyridine-2-Carboxamide For Use In Cancer Therapy And Formulations Comprising The Same
- Columbia SC, US Jing LI - Columbia SC, US Jiaxin LIANG - Quincy MA, US Donald C. PORTER - Lexington SC, US Campbell MCINNES - Irmo SC, US
International Classification:
A61K 31/551 A61P 35/00 A61P 35/02
Abstract:
Disclosed herein are methods of using 3-amino-4-(4-(4 (dimethylcarbamoyl) phenyl)-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2-carboxamide or deuterated analogues thereof for treating cancers and pharmaceutical compositions comprising the same.
Selective Inhibitors Of The Polo-Like Kinase 1 Polo-Box Domain
Inhibitors that are specific for the PBD domain of the PLK1 protein are described. The inhibitors include fragment ligated inhibitors that include one or more amino acids of a starting peptide upon which the inhibitors are based and also include non-peptidic inhibitors. The inhibitors include a benzoic acid-based derivative that mimics the structure activity relationship of amino acid residues of known peptide inhibitors. The inhibitors exhibit high selectivity for the PLK1 isotype.
Campbell McInnes - Irmo SC, US Shu Liu - Belmont CA, US
International Classification:
C07K 7/06
US Classification:
530328
Abstract:
Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
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