Tutorial on Drug Development for Central Nervous System

Docking and scoring in virtual screening for drug discovery: methods and applications

Kitchen, D. B., Decornez, H. Y., Furr, J. R., & Bajorath, J. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1549 · Cited by 4,245 · see citing works

Can the pharmaceutical industry reduce attrition rates?

Kola, I., & Landis, J. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1470 · Cited by 4,167 · see citing works

The Blood-Brain Barrier in Health and Chronic Neurodegenerative Disorders

Zlokovic, B. V. (2008) · Neuron · doi:10.1016/j.neuron.2008.01.003 · Cited by 3,280 · see citing works

A "Silent" Polymorphism in the <i>MDR</i> 1 Gene Changes Substrate Specificity

Kimchi-Sarfaty, C., Oh, J. M., Kim, I.-W., Sauna, Z. E., Calcagno, A. M., Ambudkar, S. V., & Gottesman, M. M. (2007) · Science · doi:10.1126/science.1135308 · Cited by 2,416 · see citing works

Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs

Schinkel, A. H., Smit, J., van Tellingen, O., Beijnen, J. H., Wagenaar, E., van Deemter, L., Mol, C. A. A. M., van der Valk, M. A., Robanus-Maandag, E. C., Riele, H. T., et al. (1994) · Cell · doi:10.1016/0092-8674(94)90212-7 · Cited by 2,284 · see citing works

Cyclodextrin-based pharmaceutics: past, present and future

Davis, M. E., & Brewster, M. E. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1576 · Cited by 2,002 · see citing works

Metabonomics: a platform for studying drug toxicity and gene function

Nicholson, J. K., Connelly, J. C., Lindon, J. C., & Holmes, E. C. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd728 · Cited by 1,915 · see citing works

Protein Therapeutics: A Summary and Pharmacological Classification

Leader, B., Baca, Q. J., & Golan, D. E. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2399 · Cited by 1,913 · see citing works

Virtual screening of chemical libraries

Shoichet, B. K. (2004) · Nature · doi:10.1038/nature03197 · Cited by 1,425 · see citing works

A ‘Rule of Three’ for fragment-based lead discovery?

Congreve, M., Carr, R. A. E., Murray, C. W., & Jhoti, H. (2003) · Drug Discovery Today · doi:10.1016/s1359-6446(03)02831-9 · Cited by 1,365 · see citing works

Multi-target therapeutics: when the whole is greater than the sum of the parts

Zimmermann, G. R., Lehár, J., & Keith, C. T. (2007) · Drug Discovery Today · doi:10.1016/j.drudis.2006.11.008 · Cited by 1,105 · see citing works

Hit and lead generation: beyond high-throughput screening

Bleicher, K., Böhm, H., Müller, K., & Alanine, A. I. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1086 · Cited by 1,054 · see citing works

Navigating chemical space for biology and medicine

Lipinski, C. A., & Hopkins, A. L. (2004) · Nature · doi:10.1038/nature03193 · Cited by 1,008 · see citing works

Global mapping of pharmacological space

Paolini, G. V., Shapland, R. H. B., van Hoorn, W. P., Mason, J. S., & Hopkins, A. L. (2006) · Nature Biotechnology · doi:10.1038/nbt1228 · Cited by 812 · see citing works

Approaches to transport therapeutic drugs across the blood–brain barrier to treat brain diseases

Gabathuler, R. (2009) · Neurobiology of Disease · doi:10.1016/j.nbd.2009.07.028 · Cited by 804 · see citing works

Fragment-based lead discovery

Rees, D. C., Congreve, M., Murray, C. W., & Carr, R. A. E. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1467 · Cited by 797 · see citing works

Characteristics of Compounds that Cross the Blood-Brain Barrier

Banks, W. A. (2009) · BMC Neurology · doi:10.1186/1471-2377-9-s1-s3 · Cited by 710 · see citing works

Modelling of the blood–brain barrier in drug discovery and development

Cecchelli, R., Bérézowski, V., Lundquist, S., Culot, M., Renftel, M., Dehouck, M., & Fénart, L. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2368 · Cited by 622 · see citing works

Synthesis at the molecular frontier

Wender, P. A., & Miller, B. L. (2009) · Nature · doi:10.1038/460197a · Cited by 580 · see citing works

Target-based drug discovery: is something wrong?

Sams‐Dodd, F. (2005) · Drug Discovery Today · doi:10.1016/s1359-6446(04)03316-1 · Cited by 522 · see citing works

Can we rationally design promiscuous drugs?

HOPKINS, A., MASON, J., & OVERINGTON, J. (2006) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2006.01.013 · Cited by 469 · see citing works

The role of the medicinal chemist in drug discovery — then and now

Lombardino, J. G., & Lowe, J. A., III (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1523 · Cited by 455 · see citing works

Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents

Massa, S. M., Yang, T., Xie, Y., Shi, J., Bilgen, M., Joyce, J. N., Nehama, D., Rajadas, J., & Longo, F. M. (2010) · Journal of Clinical Investigation · doi:10.1172/jci41356 · Cited by 406 · see citing works

Knockouts model the 100 best-selling drugs—will they model the next 100?

Zambrowicz, B., & Sands, A. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd987 · Cited by 393 · see citing works

The application of discovery toxicology and pathology towards the design of safer pharmaceutical lead candidates

Kramer, J. A., Sagartz, J. E., & Morris, D. L. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2378 · Cited by 370 · see citing works

Preclinical safety evaluation of biotechnology-derived pharmaceuticals

Cavagnaro, J. A. (2002) · Nature Reviews Drug Discovery · doi:10.1038/nrd822 · Cited by 340 · see citing works

Targeting protein kinases in central nervous system disorders

Chico, L. K., Eldik, L. J. V., & Watterson, D. M. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2999 · Cited by 292 · see citing works

Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds

Feng, Y., Mitchison, T. J., Bender, A., Young, D. W., & Tallarico, J. A. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2876 · Cited by 278 · see citing works

Molecular Trojan horses for blood–brain barrier drug delivery

Pardridge, W. M. (2006) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2006.06.001 · Cited by 259 · see citing works

Structure-based virtual screening of chemical libraries for drug discovery

Ghosh, S., Nie, A., An, J., & Huang, Z. (2006) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2006.04.002 · Cited by 246 · see citing works

Target selection in drug discovery

Knowles, J., & Gromo, G. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd986 · Cited by 216 · see citing works

The p75 Neurotrophin Receptor Promotes Amyloid-β(1-42)-Induced Neuritic Dystrophy<i>In Vitro</i>and<i>In Vivo</i>

Knowles, J. K., Rajadas, J., Nguyen, T.-V. V., Yang, T., LeMieux, M. C., Vander Griend, L., Ishikawa, C., Massa, S. M., Wyss-Coray, T., & Longo, F. M. (2009) · The Journal of Neuroscience · doi:10.1523/jneurosci.0620-09.2009 · Cited by 184 · see citing works

Human stem cells and drug screening: opportunities and challenges

Ebert, A., & Svendsen, C. (2010) · Nature reviews. Drug discovery · doi:10.1038/nrd3000 · Cited by 178 · see citing works

The basics of preclinical drug development for neurodegenerative disease indications

Steinmetz, K. L., & Spack, E. G. (2009) · BMC Neurology · doi:10.1186/1471-2377-9-s1-s2 · Cited by 155 · see citing works

Stem Cells and Drug Discovery: The Beginning of a New Era?

Rubin, L. L. (2008) · Cell · doi:10.1016/j.cell.2008.02.010 · Cited by 145 · see citing works

Challenges and opportunities in CNS delivery of therapeutics for neurodegenerative diseases

Barchet, T. M., & Amiji, M. M. (2009) · Expert Opinion on Drug Delivery · doi:10.1517/17425240902758188 · Cited by 145 · see citing works

ADDME – Avoiding Drug Development Mistakes Early: central nervous system drug discovery perspective

Tsaioun, K., Bottlaender, M., & Mabondzo, A. M. (2009) · BMC Neurology · doi:10.1186/1471-2377-9-s1-s1 · Cited by 107 · see citing works

Predicting therapeutic value in the lead optimization phase of drug discovery

Kenakin, T. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1110 · Cited by 104 · see citing works

Back to the future: the 'old-fashioned' way to new medications for neurodegeneration

Lansbury, P. T. (2004) · Nature Medicine · doi:10.1038/nrn1435 · Cited by 86 · see citing works

New approaches to drug safety: a pharmacovigilance tool kit

Wise, L., Parkinson, J. A., Raine, J. M., et al. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd3002 · Cited by 79 · see citing works

Developing drugs that can cross the blood-brain barrier: applications to Alzheimer's disease

Banks, W. A. (2008) · BMC Neuroscience · doi:10.1186/1471-2202-9-s3-s2 · Cited by 51 · see citing works

Quantifying Biological Activity in Chemical Terms: A Pharmacology Primer To Describe Drug Effect

Kenakin, T. (2009) · ACS Chemical Biology · doi:10.1021/cb800299s · Cited by 46 · see citing works

Modern Molecular Approaches to Drug Design and Discovery

Ojima, I. (2008) · Accounts of Chemical Research · doi:10.1021/ar700158c · Cited by 33 · see citing works

Molecular Properties and CYP2D6 Substrates: Central Nervous System Therapeutics Case Study and Pattern Analysis of a Substrate Database

Chico, L. K., Behanna, H. A., Hu, W., Zhong, G., Roy, S. M., & Watterson, D. M. (2009) · Drug Metabolism and Disposition · doi:10.1124/dmd.109.028134 · Cited by 20 · see citing works

Meeting the unique challenges of drug discovery for neurodegenerative diseases

Shineman, D. W., & Fillit, H. M. (2009) · BMC Neurology · doi:10.1186/1471-2377-9-s1-i1 · Cited by 9 · see citing works

People's Drug Guide to Deadly Drug Interactions Focuses on Drug/Drug, Drug/Food, and Drug/Vitamin Interactions

(1998) · Gastroenterology Nursing · doi:10.1097/00001610-199805000-00012

Me-too drug,me-better drug and me-new drug in drug R&D

Bao-quan, Z. (2009) · Zhongguo xin yao zazhi

Delay Between Drug Action, Drug Effect and Final Drug Exposure

Talevi, A. (2022) · Springer eBooks · doi:10.1007/978-3-030-84860-6_300086

The People's Guide to Deadly Drug Interactions: How to Protect Yourself from Life-Threatening Drug/Drug, Drug/Food, Drug/Vitamin Combinations

Adams, S. (1996) · Europe PMC (PubMed Central) · Cited by 1 · see citing works

Drug–Drug, Drug–Dietary Supplement, Drug–Citrus Fruit, and Other Food Interactions—Labeling Implications

Huang, S., Lesko, L. J., & Temple, R. (2006) · CRC Press eBooks · doi:10.1201/9780849355530-13