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Full-Text Articles in Medicinal and Pharmaceutical Chemistry
Am 6545: A Novel Peripheral Cb1 Antagonist, Seth Hosmer
Am 6545: A Novel Peripheral Cb1 Antagonist, Seth Hosmer
Honors Scholar Theses
Obesity and other related metabolic disorders are a common problem in the United States. Consequently, several drug therapies have been developed in an attempt to address this problem. Many older appetite suppressants, such as amphetamines, were dangerous and potentially addictive. For the last few years, the endocannabinoid system was investigated as a potential target for appetite suppression. Unfortunately, early cannabinoid CB1 antagonists came with an unacceptable side effect profile of their own, which is largely due to central actions of these drugs. In an attempt to reduce the side effect profile, researchers are investigating peripherally acting cannabinoid antagonists, which do …
The Proteolytic Stability And Cytotoxicity Studies Of L‐Aspartic Acid And L‐Diaminopropionic Acid Derived Β‐Peptides And A Mixed Α/Β‐Peptide, Sahar Ahmed, Kamaljit Kaur
The Proteolytic Stability And Cytotoxicity Studies Of L‐Aspartic Acid And L‐Diaminopropionic Acid Derived Β‐Peptides And A Mixed Α/Β‐Peptide, Sahar Ahmed, Kamaljit Kaur
Pharmacy Faculty Articles and Research
The use of peptides as drugs in pharmaceutical applications is hindered by their susceptibility to proteolysis and therefore low bioavailability. β‐Peptides that contain an additional methylene group in the backbone, are gaining recognition from a pharmaceutical stand point as they are considerably more resilient to proteolysis and metabolism. Recently, we reported two new classes of β‐peptides, β3‐ and β2‐peptides derived from l‐aspartic acid and l‐diaminopropionic acid, respectively. Here, we report the proteolytic stability of these β‐peptidic compounds and a mixed α /β‐peptide against three enzymes (pronase, trypsin and elastase), as well as, human serum. The …
New Dosing Schedules Of Dasatinib For Cml And Adverse Event Management, Siu Fun Wong
New Dosing Schedules Of Dasatinib For Cml And Adverse Event Management, Siu Fun Wong
Pharmacy Faculty Articles and Research
Resistance to imatinib in patients with chronic myelogenous leukemia (CML) or Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) has emerged as a significant clinical issue. Dasatinib is a tyrosine kinase inhibitor that has 325-fold greater in vitro activity against native BCR-ABL (breakpoint cluster region-Abelson leukemia virus) compared with imatinib and can overcome primary (intrinsic) and secondary (acquired) imatinib resistance. Here, we review the clinical profile of dasatinib in imatinib-resistant and -intolerant patients and share clinical approaches for managing adverse events (AEs) to ensure maximum patient benefit. References were obtained through literature searches on PubMed as well as from the Proceedings …