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Batman A.M.,University of Richmond | Batman A.M.,Melior Discovery, Inc. | Miles M.F.,Virginia Commonwealth University
Alcohol Research: Current Reviews | Year: 2015

Alcohol use disorder (AUD) and its sequelae impose a major burden on the public health of the United States, and adequate long-term control of this disorder has not been achieved. Molecular and behavioral basic science research findings are providing the groundwork for understanding the mechanisms underlying AUD and have identified multiple candidate targets for ongoing clinical trials. However, the translation of basic research or clinical findings into improved therapeutic approaches for AUD must become more efficient. Translational research is a multistage process of streamlining the movement of basic biomedical research findings into clinical research and then to the clinical target populations. This process demands efficient bidirectional communication across basic, applied, and clinical science as well as with clinical practitioners. Ongoing work suggests rapid progress is being made with an evolving translational framework within the alcohol research field. This is helped by multiple interdisciplinary collaborative research structures that have been developed to advance translational work on AUD. Moreover, the integration of systems biology approaches with collaborative clinical studies may yield novel insights for future translational success. Finally, appreciation of genetic variation in pharmacological or behavioral treatment responses and optimal communication from bench to bedside and back may strengthen the success of translational research applications to AUD. © 2015, National Institute on Alcohol Abuse and Alcoholism (NIAAA). All rights reserved.

Reaume A.G.,Melior Discovery, Inc.
Drug Discovery Today: Therapeutic Strategies | Year: 2012

The tremendous biological complexity associated with living systems results in significant limitations on the reductionist or target-based drug discovery approach. Increasingly it is being recognized that allowing for more serendipity to enter drug discovery vis-a'-vis phenotypic screening provides for more cost-effective drug discovery with higher productivity. Several compelling studies and examples help establish this point of view. © 2011 Elsevier Ltd. All rights reserved.

Lipinski C.A.,Melior Discovery, Inc.
Topics in Medicinal Chemistry | Year: 2010

A medicinal chemist combines organic synthesis expertise and the ability to optimize chemistry structure-activity relationships (SAR) based on relevant biomedical information so as to achieve project goals. The ability to optimize chemistry SAR consists of both the easier to explain logical stepwise structural modification that is often described by quantitative structure-activity relationships (QSAR) and the more difficult to explain exercise of high-order pattern recognition. Optimizing SAR is full of traps for the unwary. What are the pros and cons of various types of screens? Should one believe the screening data? How does one optimize against multiple sometimes conflicting properties? What types of compounds are worth screening? How does one judge the quality of a screening hit? Very importantly, drug discovery is a team exercise in which the medicinal chemist plays a key facilitating role. Given good interpersonal skills, the medicinal chemist's training is broad enough to enable cooperative interactions across the whole discovery team. Chemistry pattern recognition is the unique skill that the medicinal chemist contributes to drug discovery. The ability to relate chemistry structure to biological activity and to change chemistry structure so as to change a variety of biomedical parameters in a desired direction leads to the successful "drug hunter." © 2009 Springer-Verlag London.

Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase I | Award Amount: 224.98K | Year: 2014

DESCRIPTION (provided by applicant): The goals of this project are to develop a biomarker for MLR-1023 in order to validate Lyn kinase as a molecular target for treatment of Type II diabetes (T2D) and use the biomarker to understand the pharmacokinetic/pharmacodynamic (PK/PD) disconnect in order to optimize a dosing regimen in clinical trials. These goals will be accomplished by showing MLR-1023 target engagement and kinetics of that engagement in cells and in a translatable rodent model of T2D. Results will be translated to human clinical studies. T2D is an epidemic in the U.S. that is worsening every year. The disease affects 8.3% of Americans, a rate that some expect to double by 2025. T2D was the seventh leading cause of death in 2007 and is a leading cause of a host of other disorders, including blindness and amputations. The disease takes a massive toll on the healthcare system, having caused about 174 billion in healthcare costs in 2007 alone. Although a host of therapies have been approved by FD

Melior Discovery, Inc. | Date: 2015-05-01

The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.

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