MBRS-SCORE Program at Hampton University

描述(申请人提供)：最近资助的MBRS-SCORE(1S0-GM66093-01)被设想为振兴汉普顿大学校园生物医学研究的载体。该计划的基本目标是不受限制地发展一个充满活力和可持续的生物医学研究计划。预计这个MBRS-SCORE计划将有助于在汉普顿大学培养一批生物医学研究科学家，这样该机构将更好地做好准备，成功地参与研究拨款的公开竞争。拟议计划的另一个基本目标是培训少数族裔教职员工和学生进行生物医学研究。将组织和推动一系列“前沿”研讨会和研讨会，让整个汉普顿大学研究界都能参与进来。预计收购MBRS-SCORE研究副刊将进一步加强药学院的研究基础设施，它无疑将极大地改善汉普顿大学的研究基础设施。目前研究补充的主要目的是开发一种特异性的竞争抑制聚(ADP-核糖)糖水解酶(PARG)，可以想见地增强抗癌药物的疗效。为此，提出了一种类似于糖水解酶催化反应过渡态的ADP-(羟甲基)吡咯烷二醇的内酰胺类似物(ADP-HPD)。因此，本补充研究的目的有两个：1)合成ADP-HPD的内酰胺类似物；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在癌症治疗中开发有用的化学和放射增敏剂。这一补编肯定有助于实现最初的MBRS-SCORE提案中概述的各项目标和目的。

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.