Alignment of Synthesis, Medicinal Chemistry and Structural Genomics to Accelerate UK Drug Discovery: Network SMS-Drug
Alignment of Synthesis, Medicinal Chemistry and Structural Genomics to Accelerate UK Drug Discovery: Network SMS-Drug
批准号:
EP/I037229/1
负责人:
Nicholas Tomkinson
金额:
$23.46万
依托单位国家:
英国
项目类别:
Research Grant
财政年份:
2011
资助国家:
英国
项目状态:
已结题
起止时间:
2011 至 --
中文摘要
该计划将建立一个化学生物学的学术-用户网络,以发起、建立和培育合作项目,以促进药物发现过程。它旨在通过新的药物靶点、验证靶点的新工具和新的多学科合作伙伴关系来探索未来的平台、工具和靶点,扩大英国药物发现的能力。在后基因组时代,为药物发现和最终药物开发新的临床验证靶点的机会是相当大的。学术界和产业界的药物发现资源没有得到有效利用,给行业和社会带来了不利影响。通过在开放获取的产学研伙伴关系中进行基础生物学和临床概念证明,可以减少重复,提高生产力。新药物靶点的临床验证和新药发明的主要障碍是小分子探针的可用性和有效递送,以了解基本生物学。提供这些探针将允许药物靶点的临床前验证,并减少整个制药行业的重复工作。在后期临床试验中,潜在药物分子的失败给相关公司和整个制药行业带来了巨大的成本,也使无数患者的希望破灭。对疾病机制,特别是人类疾病机制的了解相对较差,使药物发现过程变得混乱,并代表了生物学研究的关键领域。强效、选择性和细胞渗透性的化学探针在基础和应用生物学研究中都是有价值的试剂,它们在学术和工业实验室的临床前靶标验证中是必不可少的。学术合成化学家、分子建模师和结构生物学家与工业终端用户的战略结盟将为提供开放获取化学探针提供蓝图,以支持英国的临床验证和药物发现工作。
英文摘要
This programme will establish an Academia-Users Network in Chemical Biology to initiate, establish and nurture collaborative projects for the advancement of the drug discovery process. It aims to expand the capability of UK drug discovery, with new drug targets, new tools to validate targets and new multidisciplinary partnerships to explore the platforms, tools and targets of the future.In the post-genomic age opportunities for the development of new clinically validated targets for drug discovery and ultimately medicines are considerable. Drug discovery resources in academia and industry are not used efficiently, to the detriment of industry and society. Duplication could be reduced, and productivity could be increased, by performing basic biology and clinical proofs of concept within open access industry-academia partnerships.The major obstacle to clinical validation of new drug targets and the invention of new medicines is the availability and efficient delivery of small-molecules probes in order to understand the basic biology. Provision of these probes will allow for pre-clinical validation of drug targets and reduce the duplication of efforts across the pharmaceutical industry. Failures of potential drug molecules in late stage clinical trials result in enormous cost to the companies involved, the pharmaceutical industry in general and also dashes the hopes of countless patients.A relatively poor understanding of disease mechanisms, particularly in humans, confounds the drug discovery process and represents a pivotal area of biological research. Potent, selective and cell-permeable chemical probes are valued reagents in both fundamental and applied biological research, and they are essential for preclinical target validation in academic and industrial laboratories.Strategic alignment of academic synthetic chemists, molecular modellers and structural biologists with industrial end users will provide a blueprint for the provision of open access chemical probes to support clinical validation and drug discovery efforts within the UK.
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DOI:
10.1021/jm401399c
发表时间:
2013-11-27
期刊:
Journal of medicinal chemistry
影响因子:
7.3
作者:
[Baek DJ, MacRitchie N, Anthony NG, Mackay SP, Pyne S, Pyne NJ, Bittman R]
通讯作者:
Bittman R
Microwave-Assisted Bohlmann-Rahtz Synthesis of Highly Substituted 2-Aminonicotinates
微波辅助 Bohlmann-Rahtz 合成高度取代的 2-氨基烟酸酯
DOI:
10.1055/s-0035-1561941
发表时间:
2016
期刊:
Synlett
影响因子:
2
作者:
[Bagley M]
通讯作者:
Bagley M
DOI:
10.1016/j.tet.2013.07.055
发表时间:
2013-09-30
期刊:
TETRAHEDRON
影响因子:
2.1
作者:
[Bagley, Mark C., Baashen, Mohammed, Davis, Terence]
通讯作者:
Davis, Terence
DOI:
10.3390/ph8020257
发表时间:
2015-06-03
期刊:
Pharmaceuticals (Basel, Switzerland)
影响因子:
--
作者:
[Bagley MC, Baashen M, Chuckowree I, Dwyer JE, Kipling D, Davis T]
通讯作者:
Davis T
DOI:
10.1039/c5ob00819k
发表时间:
2015-06
期刊:
Organic & biomolecular chemistry
影响因子:
3.2
作者:
[M. Bagley;J. Dwyer;M. D. Molina;A. W. Rand;H. Rand;N. Tomkinson]
通讯作者:
M. Bagley;J. Dwyer;M. D. Molina;A. W. Rand;H. Rand;N. Tomkinson
Delivering the impossible - novel fatty acid delivery reagents to enable in vivo research and discovery
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批准号:BB/W000199/1
-
项目类别:Research Grant
-
资助金额:$26.82万
-
财政年份:2022
-
负责人:Nicholas Tomkinson
-
依托单位:
Innovative targets for circadian drug discovery: REV-ERBalpha and RORalpha
-
批准号:EP/H031111/2
-
项目类别:Research Grant
-
资助金额:$154.21万
-
财政年份:2011
-
负责人:Nicholas Tomkinson
-
依托单位:
Innovative targets for circadian drug discovery: REV-ERBalpha and RORalpha
-
批准号:EP/H031111/1
-
项目类别:Research Grant
-
资助金额:$174.1万
-
财政年份:2011
-
负责人:Nicholas Tomkinson
-
依托单位:
Direct methods for the preparation of heterocycles and bis-heteroaromatics
-
批准号:EP/E020607/1
-
项目类别:Research Grant
-
资助金额:$28.86万
-
财政年份:2007
-
负责人:Nicholas Tomkinson
-
依托单位:
国内基金
海外基金
新型滤波器综合技术-直接综合技术(Direct synthesis Technique)的研究及应用
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批准号:61671111
-
项目类别:面上项目
-
资助金额:58.0万元
-
批准年份:2016
-
负责人:肖飞
-
依托单位: