Zobrazeno 1 - 10
of 352
pro vyhledávání: '"Penetrant (biochemical)"'
Autor:
Ann Vos, Frederik Jan Rita Rombouts, Andrés A. Trabanco, Daniel Oehlrich, Harrie J.M. Gijsen, Diederik Moechars, Sven Franciscus Anna Van Brandt, Aldo Peschiulli, Gregor James Macdonald, Michel Surkyn, Gary Tresadern, Michiel Van Gool, Nigel E. Austin, Michel Anna Jozef De Cleyn
Publikováno v:
ACS Med Chem Lett
[Image: see text] We recently disclosed a set of heteroaryl-fused piperazine inhibitors of BACE1 that combined nanomolar potency with good intrinsic permeability and low Pgp-mediated efflux. Herein we describe further work on two prototypes of this f
Publikováno v:
ACS Med Chem Lett
[Image: see text] An indazole/aza-indazole scaffold was developed as a novel chemotype for JNK3 inhibition. Extensive structure activity relationship (SAR) studies utilizing various in vitro and in vivo assays led to potent and highly selective JNK3
Publikováno v:
Organic Process Research & Development. 25:2288-2299
Autor:
Konstantinos I. Tsamis, Alexandros Giannakis, Ioannis Sarmas, Ilias P. Nikas, Georgia Xiromerisiou, Spiridon Konitsiotis
Publikováno v:
Laboratory Medicine. 53:210-214
The advent of next generation sequencing has revolutionized diagnostic approaches to hereditary polyneuropathies. Recently, mutations on the membrane metallo-endopeptidase (MME) gene, encoding neprilysin, have been related to the development of late-
Potential Landscape of a Probe Penetrant Particle for Fast Estimating of Silica Diffusion Properties
Autor:
Sergey V. Kukhtetskiy
Publikováno v:
Journal of Siberian Federal University. Chemistry. 14:406-417
Successful search for optimal molecular structures of membrane materials requires efficient algorithms for assessing their diffusion properties. It is shown in this work that the potential landscape of a probe penetrating particle, a component that p
Autor:
Wylie Burke
Publikováno v:
Annual Review of Genomics and Human Genetics. 22:1-24
Genomic information is poised to play an increasing role in clinical care, extending beyond highly penetrant genetic conditions to less penetrant genotypes and common disorders. But with this shift, the question of clinical utility becomes a major ch
Autor:
Michael Derks, Christoph Wandel, Sian Lennon-Chrimes, Axel Paehler, Piotr Szczesny, Heidemarie Kletzl, Lisa Squassante, Andreas Guenther
Publikováno v:
Expert Opinion on Investigational Drugs. 30:893-901
Balovaptan is a potent, selective vasopressin 1a receptor antagonist. The early-phase pharmacokinetics (PK) of balovaptan are reported.Two Phase 1 studies (overallAbsolute balovaptan bioavailability was high (103-116%). Steady-state (Day 14) balovapt
Autor:
Elana Raaphorst, Donald F. Weaver, Darapaneni Chandra Mohan, Alexander Kreft, Paolo Schiavini, Jagadeesh P. Pasangulapati, Ramana Reddy Mittapalli, Fan Wu, Laura Villar, Eric C. Keske, Kurt R. Stover, Paul M. Stafford, Kiersten Thomas, Shea L. Johnson, Mark A. Reed, Siva R. Alla, Irina Sagamanova, Mayuri Gupta, Yong Zheng, Simmi Sharma
Publikováno v:
ChemMedChem. 16:2195-2205
Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising therapeutic target in cancer immunotherapy and neurological disease. Thus, searching for highly active inhibitors for use in human cancers is now a focus of widespread research and development effor
Publikováno v:
Cement Science and Concrete Technology. 74:302-309
Publikováno v:
Cement Science and Concrete Technology. 74:318-324