MBRS-SCORE Program at Hampton University

描述（由申请人提供）：最近资助的MBRS-SCORE（1S0-GM66093 - 01）被设想为汉普顿大学校园内的生物医学研究恢复活力的工具。该计划的根本目标是一个充满活力和可持续的生物医学研究计划的肆无忌惮的发展。预计该MBRS-SCORE计划将有助于在汉普顿大学建立生物医学研究科学家的"临界质量"，使该机构能够更好地成功参与公开的研究资助竞争。拟议方案的另一个基本目标是培训少数民族教师和学生进行生物医学研究。将组织和推广一系列"尖端"研讨会和讲习班，使整个汉普顿大学的研究界都能参与。据预计，这MBRS-SCORE研究补充的收购将进一步加强药学院的研究基础设施，它无疑将沉淀在汉普顿大学的研究基础设施的巨大改善。目前的研究补充的主要推力是开发一个特定的竞争性抑制剂的聚（ADP-核糖）糖水解酶（PARG），这可以想象提高抗癌药物的疗效。为此，提出了ADP-（羟甲基）吡咯烷酮（ADP-HPD）的内酰胺类似物，其类似于糖水解酶催化反应的过渡态。因此，本研究补充的目的有两个：1）合成ADP-HPD的内酰胺类似物和2）测定其体外对PARG的抑制活性。据推测，从这些研究中获得的结果可能会导致癌症治疗中有用的化学和放射增敏剂的发展。这一补充肯定有助于实现MBRS-SCORE原始提案中概述的目标和目的。

DESCRIPTION (provided by applicant): The recently funded MBRS-SCORE (1S0-GM66093-01) is envisioned to be the vehicle by which biomedical research on the campus of Hampton University is rejuvenated. The underlying goal of this program is the unbridled development of a vigorous and sustainable biomedical research program. It is anticipated that this MBRS-SCORE Program will serve to create a "critical mass" of biomedical research scientist at Hampton University, such that the institution will be better poised to successfully participate in open competition for research grants. Another underlying objective of the proposed program is the training of minority faculty and students in biomedical research. A series of "cutting-edge" seminars and workshops will be organized and promoted, so that the entire Hampton University research community can participate. It is anticipated that the acquisition of this MBRS-SCORE Research Supplement will further enhance the research infrastructure in the School of Pharmacy, and it will undoubtedly precipitate a monumental improvement in the research infrastructure at Hampton University. The main thrust of the current research supplement is to develop a specific competitive inhibitor of poly (ADP-ribose) glycohydrolase (PARG), which can conceivably enhance the efficacy of anticancer agents. To this end, a lactam analog of ADP-(hydroxymethyl) pyrrolidinediol (ADP-HPD) that is similar to the transition state of the glycohydrolase catalyzed reaction is proposed. Therefore, the objectives of this research supplement are two fold: 1) to synthesize the lactam analog of ADP-HPD and 2) to determine its inhibitory activity toward PARG in vitro. It is postulated that the results garnered from these studies may lead to the development of useful chemo- and radiosensitizers in cancer therapy. This supplement will definitely facilitate the realizations of the goals and objectives outlined in the original MBRS-SCORE proposal.