Browsing by author "Collins, Ian"
Now showing items 21-28 of 28
-
Objective, Quantitative, Data-Driven Assessment of Chemical Probes.
Antolin, AA; Tym, JE; Komianou, A; Collins, I; Workman, P; et al. (CELL PRESS, 2018-02-15)Chemical probes are essential tools for understanding biological systems and for target validation, yet selecting probes for biomedical research is rarely based on objective assessment of all potential compounds. Here, we ... -
SimPLIT: Simplified Sample Preparation for Large-Scale Isobaric Tagging Proteomics.
Sialana, FJ; Roumeliotis, TI; Bouguenina, H; Chan Wah Hak, L; Wang, H; et al. (AMER CHEMICAL SOC, 2022-08-05)Large scale proteomic profiling of cell lines can reveal molecular signatures attributed to variable genotypes or induced perturbations, enabling proteogenomic associations and elucidation of pharmacological mechanisms of ... -
Solution NMR assignment of the ARC4 domain of human tankyrase 2.
Zaleska, M; Pollock, K; Collins, I; Guettler, S; Pfuhl, M (SPRINGER, 2019-04-15)Tankyrases are poly(ADP-ribose)polymerases (PARPs) which recognize their substrates via their ankyrin repeat cluster (ARC) domains. The human tankyrases (TNKS/TNKS2) contain five ARCs in their extensive N-terminal region; ... -
Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library.
Welford, AJ; Caldwell, JJ; Liu, M; Richards, M; Brown, N; et al. (WILEY-V C H VERLAG GMBH, 2016-04-11)The 2,11-cembranoid family of natural products has been used as inspiration for the synthesis of a structurally simplified, functionally diverse library of octahydroisobenzofuran-based compounds designed to augment a typical ... -
Synthesis of a Ribose-Incorporating Medium Ring Scaffold via a Challenging Ring-Closing Metathesis Reaction.
Rankin, SS; Caldwell, JJ; Cronin, NB; van Montfort, RLM; Collins, I (WILEY-V C H VERLAG GMBH, 2016-09-01)A practical synthesis of a novel oxabicyclo[6.2.1]undecenetriol useful as a medicinal chemistry scaffold has been developed starting from l-ribose. The sequence involves an oxidation/Grignard addition sequence and a ... -
Synthesis of trisubstituted pyrimidines by regioselective S<sub>N</sub>Ar and Suzuki reactions of polyhalopyrimidines
Large, JM; Clarke, M; Williamson, DM; McDonald, E; Collins, A (GEORG THIEME VERLAG KG, 2006-04-04)An efficient, regioselective approach to the synthesis of trisubstituted pyrimidines was developed. Sequential functionalization of com. available polyhalopyrimidines provided the target compds. in moderate to good overall ... -
Target 2035 - update on the quest for a probe for every protein.
Müller, S; Ackloo, S; Al Chawaf, A; Al-Lazikani, B; Antolin, A; et al. (ROYAL SOC CHEMISTRY, 2022-01-27)Twenty years after the publication of the first draft of the human genome, our knowledge of the human proteome is still fragmented. The challenge of translating the wealth of new knowledge from genomics into new medicines ... -
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Walton, MI; Eve, PD; Hayes, A; Henley, AT; Valenti, MR; et al. (IMPACT JOURNALS LLC, 2016-01-19)CCT245737 is the first orally active, clinical development candidate CHK1 inhibitor to be described. The IC50 was 1.4 nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently ...