Search Results - "Tomczuk, B E"

Antagonists that demonstrate species differences in neurokinin-1 receptors by Appell, K C, Fragale, B J, Loscig, J, Singh, S, Tomczuk, B E

“…125I-Bolton-Hunter-substance P (125I-BH-SP) binding properties of three novel classes of neurokinin-1 (NK-1) receptor antagonists were investigated in tissues…”
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Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor by TIANBAO LU, SOLL, R. M, ILLIG, C. R, BONE, R, MURPHY, L, SPURLINO, J, SALEMME, F. R, TOMCZUK, B. E

“…The structure activity relationships of a novel series of non-amide-based thrombin inhibitors are described. Exploration of the P2 and the aryl binding region…”
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Synthesis and substance P antagonist activity of naphthimidazolium derivatives by Lawrence, Kristine B, Venepalli, Bhaskar R, Appell, Kenneth C, Goswami, Ramanuj, Logan, Margaret E, Tomczuk, Bruce E, Yanni, John M

“…The synthesis of unsymmetrical naphth[2,3-d]imidazolium and bridged naphth[2,3-d]imidazolium derivatives and their substance P (SP) antagonist activity are…”
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Inhibition of Matrix Metalloproteinases by Hydroxamates Containing Heteroatom-Based Modifications of the P1' Group by Gowravaram, Madhusudhan R, Johnson, Jeffrey S, Delecki, Daniel, Cook, Ewell R, Tomczuk, Bruce E, Ghose, Arup K, Mathiowetz, Alan M, Spurlino, John C, Rubin, Byron, Smith, Douglas L, Pulvino, Tricia, Wahl, Robert C

“…In this study, structure-based drug design of matrix metalloproteinase inhibitors [human fibroblast collagenase (HFC), human fibroblast stromelysin (HFS), and…”
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Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists by Appell, Kenneth C, Babb, Bruce E, Goswami, Ramanuj, Hall, Patricia L, Lawrence Kristine B, Logan, Margaret E, Przyklek-Elling, Rose, Tomczuk, Bruce E, Venepalli, Bhaskar R, Yanni, John M

“…Substance P (SP) is an undecapeptide neuromodulator that belongs to the neurokinin (NK) family, which includes the structurally related neurokinin A (NKA) and…”
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2-phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics by TOMCZUK, B. E, TAYLOR, C. R, MOSES, L. M, SUTHERLAND, D. B, LO, Y. S, JOHNSON, D. N, KINNIER, W. B, KILPATRICK, B. F

“…A series of 2-phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides were designed and synthesized as non-benzodiazepine anxiolytics based on a molecular disconnection…”
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Measurement of tachykinin-induced salivation in conscious rats by Wagner, L E, Tomczuk, B E, Yanni, J M

“…A method of quantitatively measuring tachykinin-induced salivation in conscious, male, Sprague-Dawley rats is described. Salivation is quantified by…”
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Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles by Venepalli, Bhaskar R, Aimone, Lisa D, Appell, Kenneth C, Bell, Malcolm R, Dority, John A, Goswami, Ramanuj, Hall, Patricia L, Kumar, Virendra, Lawrence, Kristine B

“…Several heterosteroids containing a dihydroethisterone skeleton were prepared and shown to displace substance P in a receptor binding assay. Further…”
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Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells by Grasberger, Bruce L, Lu, Tianbao, Schubert, Carsten, Parks, Daniel J, Carver, Theodore E, Koblish, Holly K, Cummings, Maxwell D, LaFrance, Louis V, Milkiewicz, Karen L, Calvo, Raul R, Maguire, Diane, Lattanze, Jennifer, Franks, Carol F, Zhao, Shuyuan, Ramachandren, Kannan, Bylebyl, Gwendolyn R, Zhang, Marie, Manthey, Carl L, Petrella, Eugene C, Pantoliano, Michael W, Deckman, Ingrid C, Spurlino, John C, Maroney, Anna C, Tomczuk, Bruce E, Molloy, Christopher J, Bone, Roger F

“…HDM2 binds to an α-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to…”
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Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors by Qiao, Lei, Baumann, Christian A., Crysler, Carl S., Ninan, Nisha S., Abad, Marta C., Spurlino, John C., DesJarlais, Renee L., Kervinen, Jukka, Neeper, Mike P., Bayoumy, Shariff S., Williams, Robyn, Deckman, Ingrid C., Dasgupta, Malini, Reed, Rolanda L., Huebert, Norman D., Tomczuk, Bruce E., Moriarty, Kevin J.

“…The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of…”
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A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s by Subasinghe, Nalin L., Travins, Jeremy M., Ali, Farah, Huang, Hui, Ballentine, Shelley K., Marugán, Juan José, Khalil, Ehab, Hufnagel, Heather R., Bone, Roger F., DesJarlais, Renee L., Crysler, Carl S., Ninan, Nisha, Cummings, Maxwell D., Molloy, Christopher J., Tomczuk, Bruce E.

“…Inhibiting the classical pathway of complement activation by attenuating the proteolytic activity of the serine protease C1s is a potential strategy for the…”
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Determination of Pharmacophoric Geometry for Collagenase Inhibitors Using a Novel Computational Method and Its Verification Using Molecular Dynamics, NMR, and X-ray Crystallography by Ghose, Arup K, Logan, Margaret E, Treasurywala, Adi M, Wang, Hsin, Wahl, Robert C, Tomczuk, Bruce E, Gowravaram, Madhusudhan R, Jaeger, Edward P, Wendoloski, John J

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2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as nonbenzodiazepine anticonvulsants and anxiolytics by Tomczuk, Bruce E, Taylor, C. R, Moses, L. Meredith, Sutherland, Deborah B, Lo, Young S, Johnson, David N, Kinnier, William B, Kilpatrick, Brian F

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Hydroxamate inhibitors of human gelatinase B (92 kDa) by Wahl, Robert C., Pulvino, Tricia A., Mathiowetz, Alan M., Ghose, Arup K., Johnson, Jeffrey S., Delecki, Daniel, Cook, Ewell R., Gainor, James A., Gowravaram, Madhusudhan R., Tomczuk, Bruce E.

“…Gelatinase B is potently inhibited by peptide hydroxamates, including molecules that have a R 1′ group which is larger than the side chains of the natural…”
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Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P 1′ heteroatom based modifications by Tomczuk, Bruce E., Gowravaram, Madhusudhan R., Johnson, Jeffrey S., Delecki, Daniel, Cook, Ewell R., Ghose, Arup K., Mathiowetz, Alan M., Spurlino, John C., Rubin, Byron, Smith, Douglas L., Pulvino, Tricia, Wahl, Robert C.

“…Structure-based drug design (SBDD) and traditional SAR have guided the development of potent and selective hydroxamate inhibitors which contain…”
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