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375 Newest Publications in drug development research

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Assessment of the antinociceptive and ulcerogenic activity of the tapentadol–diclofenac combination in rodents

04-Jan-2018 | Juan R. Zapata‐Morales, Ángel J. Alonso‐Castro, Vinicio Granado‐Soto, Sergio Sánchez‐Enriquez, Mario A. Isiordia‐Esp ..., Drug Development Research, 2018

Abstract The objective of the present study was to evaluate the tapentadol–diclofenac combination in three dose‐ratios in the mouse acetic acid‐induced visceral pain and their ulcerogenic activity on the stomachal mucous. Dose‐response curves were generated for tapentadol, ...

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Computational and experimental exploration of the structure–activity relationships of flavonoids as potent glyoxalase‐I inhibitors

29-Dec-2017 | Qosay A. Al‐Balas, Mohammad A. Hassan, Nizar A. Al‐Shar'i, Tamam El‐Elimat, Ammar M. Almaaytah, Drug Development Research, 2017

Abstract Glyoxalase‐I (Glo‐I) enzyme has emerged as a potential target for cancer treatment. Several classes of natural products including coumarins and flavonoids have shown remarkable Glo‐I inhibitory activity. In the present study, computational and experimental approaches were ...

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Limiting Assumptions in the Design of Peptidomimetics

06-Sep-2017 | Garland R. Marshall, Flavio Ballante, Drug Development Research, 2017

ABSTRACT Limiting the flexibility of organic compounds to enhance their affinity and selectivity for targeting a macromolecule involved in molecular recognition has become a well‐developed paradigm in medicinal chemistry. While the role of reverse‐turn motifs as peptidomimetics ...

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Ultra‐Low Doses of Naltrexone Enhance the Antiallodynic Effect of Pregabalin or Gabapentin in Neuropathic Rats

04-Sep-2017 | Jorge B. Pineda‐Farias, Nadia L. Caram‐Salas, Ana B. Salinas‐Abarca, Jorge Ocampo, Vinicio Granados‐Soto, Drug Development Research, 2017

ABSTRACT Treatment of neuropathic pain is an area of largely unmet medical need. Pregabalin and gabapentin are anticonvulsants widely used for the treatment of neuropathic pain. Unfortunately, these drugs are only effective in 50–60% of the treated patients. In addition, both ...

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Peptide Mimetic Drugs for Modulating Thrombosis and Hemostasis

17-Aug-2017 | Kimberly Nellenbach, Ashley C. Brown, Drug Development Research, 2017

ABSTRACT Hemostasis is the complex physiological process that stems bleeding at an injury site while simultaneously maintaining unobstructed circulation in other areas of the body. This system is kept in balance with finely tuned regulation by pro‐ and antithrombotic agents. When ...

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RGD Peptide‐Based Target Drug Delivery of Doxorubicin Nanomedicine

17-Aug-2017 | Yuan Sun, Chen Kang, Fei Liu, You Zhou, Lei Luo, Hongzhi Qiao, Drug Development Research, 2017

ABSTRACT Doxorubicin (DOX) is commonly used for the treatment of breast cancer and lymphoma. However, its clinical use has been severely limited due to cardiotoxicity, requiring the development of safer and more efficient pharmaceutical formulations of DOX. Advances in ...

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On BH3 Mimetics and Ca2+ Signaling

14-Aug-2017 | Pawel E. Ferdek, Monika A. Jakubowska, Drug Development Research, 2017

ABSTRACT BH3 mimetics are anticancer agents that reproduce the spatial arrangement of the BH3 domain of Bcl‐2 family proteins. Just like the BH3‐only proteins, these compounds bind to the hydrophobic cleft of the pro‐survival Bcl‐2 members such as Bcl‐2 or Bcl‐xL, and disrupt ...

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On BH3 Mimetics and Ca2+ Signaling

14-Aug-2017 | Pawel E. Ferdek, Monika A. Jakubowska, Drug Development Research, 2017

ABSTRACT BH3 mimetics are anticancer agents that reproduce the spatial arrangement of the BH3 domain of Bcl‐2 family proteins. Just like the BH3‐only proteins, these compounds bind to the hydrophobic cleft of the pro‐survival Bcl‐2 members such as Bcl‐2 or Bcl‐xL, and disrupt ...

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Small Scaffolds, Big Potential: Developing Miniature Proteins as Therapeutic Agents

11-Aug-2017 | Justin M. Holub, Drug Development Research, 2017

ABSTRACT Miniature proteins are a class of oligopeptide characterized by their short sequence lengths and ability to adopt well‐folded, three‐dimensional structures. Because of their biomimetic nature and synthetic tractability, miniature proteins have been used to study a range ...

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Recent Advances on Bioactive Constituents in Ferula

08-Aug-2017 | Yueting Zhou, Fang Xin, Guoqiang Zhang, Hexiang Qu, Desong Yang, Xiaoqiang Han, Drug Development Research, 2017

ABSTRACT The genus Ferula (Umbelliferea) is widely distributed across Central Asia and the Mediterranean. Some plants of the genus Ferula have been used as sources of pharmaceuticals for centuries. Ferula is a rich source of biologically active compounds, including coumarin ...

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