Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Jennifer Lattanze"'
Autor:
Juan Jose Marugan, Wenxi Pan, Carl Crysler, Carl L. Manthey, Margery A. Chaikin, Bruce E. Tomczuk, Kristi A. Leonard, Jennifer Lattanze, Pierre Raboisson
Publikováno v:
European Journal of Medicinal Chemistry. 41:847-861
The binding of lead compounds and drugs to human serum albumin (HSA) is a ubiquitous problem in drug discovery since it modulates the availability of the leads and drugs to their intended target, which is linked to biological efficacy. In our continu
Autor:
Maxwell D. Cummings, Tianbao Lu, Jennifer Lattanze, Juan J. Marugan, Carsten Schubert, Joan Gushue, Holly K. Koblish, Shuyuan Zhao, Kristi A. Leonard, Mark R. Player, Anna C. Maroney, Pierre Raboisson, Raul R. Calvo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3115-3120
The 1,4-benzodiazepine-2,5-dione is a suitable template to disrupt the interaction between p53 and Hdm2. The development of an enantioselective synthesis disclosed the stereochemistry of the active enantiomer. An in vitro p53 peptide displacement ass
Autor:
Jennifer Lattanze, Tianbao Lu, Karen L. Milkiewicz, Bruce L. Grasberger, Theodore E. Carver, Louis V. LaFrance, Daniel J. Parks, Kannan Ramachandren, Varsha Gupta, Raul R. Calvo, Diane M. Maguire, Eugene C. Petrella, Maxwell D. Cummings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:765-770
A library of 1,4-benzodiazepine-2,5-diones was screened for binding to the p53-binding domain of HDM2 using Thermofluor ® , a miniaturized thermal denaturation assay. The hits obtained were shown to bind to HDM2 in the p53-binding pocket using a flu
Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells
Autor:
Tianbao Lu, Jennifer Lattanze, Ingrid Deckman, Marie Zhang, Bruce L. Grasberger, Carl L. Manthey, and Christopher J. Molloy, John C. Spurlino, Diane M. Maguire, Eugene C. Petrella, Kannan Ramachandren, Holly K. Koblish, Shuyuan Zhao, Bruce E. Tomczuk, Gwendolyn R. Bylebyl, Louis V. LaFrance, Carsten Schubert, Daniel J. Parks, Karen L. Milkiewicz, Carol F. Franks, Theodore E. Carver, Roger F. Bone, Anna C. Maroney, Maxwell D. Cummings, Raul R. Calvo, W. Michael Avondale Pantoliano
Publikováno v:
Journal of Medicinal Chemistry. 48:909-912
HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepined
Autor:
Pierre Raboisson, Jennifer Lattanze, Margery A. Chaikin, Carl Crysler, Juan Jose Marugan, Bruce E. Tomczuk, Kristi A. Leonard, Carl L. Manthey, Wenxi Pan
Publikováno v:
ChemInform. 37
The binding of lead compounds and drugs to human serum albumin (HSA) is a ubiquitous problem in drug discovery since it modulates the availability of the leads and drugs to their intended target, which is linked to biological efficacy. In our continu
Autor:
Carl L. Manthey, Renee L. DesJarlais, Rolanda Reed, Margery Chaikin, Jennifer Lattanze, B. Tomczuk, Juan Jose Marugan, Pierre Raboisson
Publikováno v:
European journal of medicinal chemistry. 42(3)
The vitronectin receptor alpha(v)beta(3) has been identified as a promising potential target for the treatment of osteoporosis, diabetic retinopathy and cancer. We have recently reported 5-substituted indoles 3-[5-[2-(5,6,7,8-tetrahydro[1,8]naphthyri
Autor:
Karen L. Milkiewicz, Tianbao Lu, Maxwell D. Cummings, Louis V. LaFrance, Jennifer Lattanze, Carsten Schubert, Daniel J. Parks, Raul R. Calvo
Publikováno v:
Chemical biologydrug design. 67(3)
Small molecule antagonists of protein-protein interactions represent a particular challenge for pharmaceutical discovery. One approach to finding molecules that can disrupt these interactions is to seek mimics of common protein structure motifs. We p
Autor:
Pierre, Raboisson, Carl L, Manthey, Margery, Chaikin, Jennifer, Lattanze, Carl, Crysler, Kristi, Leonard, Wenxi, Pan, Bruce E, Tomczuk, Juan José, Marugán
Publikováno v:
European journal of medicinal chemistry. 41(7)
The binding of lead compounds and drugs to human serum albumin (HSA) is a ubiquitous problem in drug discovery since it modulates the availability of the leads and drugs to their intended target, which is linked to biological efficacy. In our continu
Autor:
Raymond J. Patch, Baumann Christian Andrew, Mark R. Player, Jian Liu, Heidi Ott, Alan C. Gibbs, Jennifer Lattanze
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(12)
A series of 2-acylaminothiophene-3-carboxamides has been identified which exhibit potent inhibitory activity against the FLT3 tyrosine kinase. Compound 44 inhibits the isolated enzyme (IC50 = 0.027 microM) and blocks the proliferation of MV4-11 cells
Autor:
Tianbao Lu, Anna C. Maroney, Jennifer Lattanze, Joan Gushue, Pierre Raboisson, Juan J. Marugan, Raul R. Calvo, Maxwell D. Cummings, Shuyuan Zhao, Holly K. Koblish, Kristi A. Leonard, Mark R. Player
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(13)
The disruption of the p53-Hdm2 protein-protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. S