T
Tadas S. Vasaitis
Researcher at University of Maryland Eastern Shore
Publications - 24
Citations - 1286
Tadas S. Vasaitis is an academic researcher from University of Maryland Eastern Shore. The author has contributed to research in topics: Prostate cancer & Androgen receptor. The author has an hindex of 17, co-authored 23 publications receiving 1180 citations. Previous affiliations of Tadas S. Vasaitis include University of Maryland Marlene and Stewart Greenebaum Cancer Center & University of Maryland, Baltimore.
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Journal ArticleDOI
Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens: Synthesis, in Vitro Biological Activity, Pharmacokinetics, and Antitumor Activity in the LAPC4 Human Prostate Cancer Xenograft Model
Venkatesh D. Handratta,Tadas S. Vasaitis,Vincent C. O. Njar,Lalji K. Gediya,Ritesh Kataria,Pankaj Chopra,Donnell Newman,Rena Farquhar,Zhiyong Guo,Yun Qiu,Angela Brodie +10 more
TL;DR: To the authors' knowledge, this is the first example of an antihormonal agent (an inhibitor of androgen synthesis (CYP17 inhibitor)/antiandrogen) that is significantly more effective than castration in suppression of androgens-dependent prostate tumor growth.
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CYP17 inhibitors for prostate cancer therapy
TL;DR: The role of androgen biosynthesis in the progression of prostate cancer and the impact of CYP17 inhibitors, such as ketoconazole, abiraterone acetate, VN/124-1 (TOK-001) and TAK-700 in the clinic and in clinical development are highlighted.
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Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases.
Vincent C. O. Njar,Lalji K. Gediya,Lalji K. Gediya,Puranik Purushottamachar,Puranik Purushottamachar,Pankaj Chopra,Pankaj Chopra,Tadas S. Vasaitis,Tadas S. Vasaitis,Aakanksha Khandelwal,Aakanksha Khandelwal,Jhalak Mehta,Jhalak Mehta,Carlic Huynh,Carlic Huynh,Aashvini Belosay,Aashvini Belosay,Jyoti Patel,Jyoti Patel +18 more
TL;DR: A novel strategy to overcome the limitation associated with exogenous ATRA therapy has been to modulate and/or increase the levels of endogenous ATRA by inhibiting the cytochrome P450-dependent ATRA-4-hydroxylase enzymes (particularly CYP26s) responsible for ATRA metabolism.
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Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.
Puranik Purushottamachar,Abhijit M. Godbole,Lalji K. Gediya,Marlena S. Martin,Tadas S. Vasaitis,Tadas S. Vasaitis,Andrew K. Kwegyir-Afful,Senthilmurugan Ramalingam,Zeynep Ates-Alagoz,Zeynep Ates-Alagoz,Vincent C. O. Njar +10 more
TL;DR: It is discovered that compounds prepared, including 5, 36, 43, and 47, could degrade both full-length and truncated ARs in CWR22rv1 human prostate cancer cells and have potential for development as new drugs for the treatment of all forms of prostate cancer.
Journal ArticleDOI
Three Dimensional Pharmacophore Modeling of Human CYP17 Inhibitors. Potential Agents for Prostate Cancer Therapy
Omoshile O. Clement,Clive M. Freeman,Rolf W Hartmann,Venkatesh D. Handratta,Tadas S. Vasaitis,Angela Brodie,Vincent C. O. Njar +6 more
TL;DR: Using the pharmacophore model derived for azole-steroidal inhibitors as a 3D search query against several 3D multiconformational Catalyst formatted databases, several steroidal compounds with potential inhibition of this enzyme are identified.