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1

Inhibitors to overcome secondary mutations in the stem cell factor receptor KIT

Kaitsiotou, Helena, Keul, Marina, Hardick, Julia, Mühlenberg, Thomas, Ketzer, Julia, Ehrt, Christiane, Krüll, Jasmin, Medda, Federico, Koch, Oliver, Giordanetto, Fabrizio, Bauer, Sebastian, Rauh, Dani

Journal:

Journal of Medicinal Chemistry

Year:

2017

Language:

english

File:

PDF, 3.29 MB

english, 2017

2

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Solid-State Properties

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 441 KB

english, 2018

3

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Early Phase API Process Development Overview

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 459 KB

english, 2018

4

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Addressing Genotoxicity Risk in Lead Optimization: A PDE10A Inhibitor Case Study

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 2.47 MB

english, 2018

5

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Active Pharmaceutical Ingredient Cost of Goods: Discovery to Early Development

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 675 KB

english, 2018

6

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Nonclinical Safety Pharmacology

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 219 KB

english, 2018

7

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Intellectual Property: The Patent Landscape Viewed from Generic and Originator Perspectives

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 360 KB

english, 2018

8

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Patent Law Relevant to Early Drug Development

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 156 KB

english, 2018

9

Optimization of ketone-based P2Y12 receptor antagonists as antithrombotic agents: Pharmacodynamics and receptor kinetics considerations

Giordanetto, Fabrizio, Bach, Peter, Zetterberg, Fredrik, Antonsson, Thomas, Bylund, Ruth, Johansson, Johan, Sellén, Mikael, Brown, David, Hideståhl, Lotta, Berntsson, Pia, Hovdal, Daniel, Zachrisson,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.54 MB

english, 2014

10

Lead Optimization of Ethyl 6-Aminonicotinate Acyl Sulfonamides as Antagonists of the P2Y 12 Receptor. Separation of the Antithrombotic Effect and Bleeding for Candidate Drug AZD1283

Bach, Peter, Antonsson, Thomas, Bylund, Ruth, Björkman, Jan-Arne, Österlund, Krister, Giordanetto, Fabrizio, van Giezen, J. J. J., Andersen, Søren M., Zachrisson, Helen, Zetterberg, Fredrik

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 948 KB

english, 2013

11

Small molecule inhibitors of ebola virus infection

Picazo, Edwige, Giordanetto, Fabrizio

Journal:

Drug Discovery Today

Year:

2015

Language:

english

File:

PDF, 856 KB

english, 2015

12

DYRK1A inhibition as potential treatment for Alzheimer’s disease

Stotani, Silvia, Giordanetto, Fabrizio, Medda, Federico

Journal:

Future Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.02 MB

english, 2016

13

Surgical correction of mandibular hypoplasia in hemifacial microsomia: A retrospective study in 39 patients

Bertin, H., Mercier, J., Cohen, A., Giordanetto, J., Cohen, N., Lee, S.H., Perrin, J.P., Corre, P.

Journal:

Journal of Cranio-Maxillofacial Surgery

Year:

2017

Language:

english

File:

PDF, 2.22 MB

english, 2017

14

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Particle Size Reduction: From Microsizing to Nanosizing

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 538 KB

english, 2018

15

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Informing Decisions in Discovery and Early Development Research Through Quantitative and Translational Modeling

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 931 KB

english, 2018

16

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || The Discovery/Development Transition

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 425 KB

english, 2018

17

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Translational Modeling and Simulation for Molecularly Targeted Small Molecule Anticancer Agents: Case Studies of Multiple Tyrosine Kinase Inhibitors, Crizotinib and Lorlatinib

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 1.15 MB

english, 2018

18

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Patent Considerations in Collaborative Drug Development

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 322 KB

english, 2018

19

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Early Drug Development: From a Drug Candidate to the Clinic

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 681 KB

english, 2018

20

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || From TRAIL to ONC201: Case Study on the Safety Benefit of Developing Targeted Agents Against Cancer-selective Pathways

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 280 KB

english, 2018

21

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Vortioxetine and Early Drug Development Considerations at the Interface of R&D

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 696 KB

english, 2018

22

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Salt and Cocrystal Screening

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 2.51 MB

english, 2018

23

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Solubility, Permeability, and Their Interplay

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 589 KB

english, 2018

24

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Preclinical Toxicology Evaluation

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 263 KB

english, 2018

25

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || New Technologies in Process Development

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 1.74 MB

english, 2018

26

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Prediction of Human Pharmacokinetics and Pharmacodynamics

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 801 KB

english, 2018

27

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Integration of Pharmacokinetic and Pharmacodynamic Reasoning and Its Importance in Drug Discovery

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 1.05 MB

english, 2018

28

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Patent Protection Strategy

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 171 KB

english, 2018

29

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Early Drug Development: Progressing a Candidate Compound to the Clinics

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 101 KB

english, 2018

30

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Early Drug Development

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 232 KB

english, 2018

31

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Development of a Practical Synthesis of 4′-Azido-2′β-Methyl-2′-Desoxycytosine and Its Prodrugs as HCV Chemotherapeutic Agents

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 587 KB

english, 2018

32

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Front Matter

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 180 KB

english, 2018

33

[Methods and Principles in Medicinal Chemistry] Early Drug Development (Bringing a Preclinical Candidate to the Clinic) || Index

Giordanetto, Fabrizio Giordanetto

Year:

2018

Language:

english

File:

PDF, 126 KB

english, 2018

34

Structural basis for selective PDE 3 inhibition: a docking study

Paola Fossa, Fabrizio Giordanetto, Giulia Menozzi, Luisa Mosti

Journal:

Molecular Informatics

Year:

2002

Language:

english

File:

PDF, 275 KB

english, 2002

35

Novel Scoring Functions Comprising QXP, SASA, and Protein Side-Chain Entropy Terms.

Fabrizio Giordanetto, Simona Cotesta, Cornel Catana, Jean-Yves Trosset, Anna Vulpetti, Pieter F. W. Stouten, Romano T. Kroemer

Journal:

Year:

2004

File:

PDF, 82 KB

2004

36

Assessment of Docking Poses: Interactions-Based Accuracy Classification (IBAC) versus Crystal Structure Deviations.

Romano T. Kroemer, Anna Vulpetti, Joseph J. McDonald, Douglas C. Rohrer, Jean-Yves Trosset, Fabrizio Giordanetto, Simona Cotesta, Colin McMartin, Mats Kihlen, Pieter F. W. Stouten

Journal:

Year:

2004

File:

PDF, 82 KB

2004

37

Structure-Based Discovery of Allosteric Modulators of Two Related Class B G-Protein-Coupled Receptors

Dr. Chris de Graaf, Dr. Chantal Rein, Dr. David Piwnica, Dr. Fabrizio Giordanetto, Dr. Didier Rognan

Journal:

Year:

2011

Language:

english

File:

PDF, 1.40 MB

english, 2011

38

Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities

Susanne Berglund, Bryan J. Egner, Henrik Gradén, Joakim Gradén, David G.A. Morgan, Tord Inghardt, Fabrizio Giordanetto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 2.22 MB

english, 2009

39

Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition

Susanne Berglund, Bryan J. Egner, Henrik Gradén, Joakim Gradén, David G.A. Morgan, Tord Inghardt, Fabrizio Giordanetto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 2.40 MB

english, 2009

40

Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists

Fabrizio Giordanetto, Olle Karlsson, Jan Lindberg, Lars-Olof Larsson, Anna Linusson, Emma Evertsson, David G.A. Morgan, Tord Inghardt

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2007

Language:

english

File:

PDF, 343 KB

english, 2007

41

Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent Melanin-Concentrating Hormone Receptor 1 (MCH-R1) antagonists

Susanne Berglund, Bryan J. Egner, Henrik Gradén, Joakim Gradén, David G.A. Morgan, Tord Inghardt, Fabrizio Giordanetto

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 277 KB

english, 2008

42

Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening

Fabrizio Giordanetto, Bengt Kull, Anita Dellsén

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 1002 KB

english, 2011

43

Virtual screening to enrich a compound collection with CDK2 inhibitors using docking, scoring, and composite scoring models

Simona Cotesta, Fabrizio Giordanetto, Jean-Yves Trosset, Patrizia Crivori, Romano T. Kroemer, Pieter F.W. Stouten, Anna Vulpetti

Journal:

Proteins: Structure, Function, and Bioinformatics

Year:

2005

Language:

english

File:

PDF, 901 KB

english, 2005

44

Ticagrelor binds to human P2Y12 independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation

J. J. J. VAN GIEZEN, L. NILSSON, P. BERNTSSON, B.-M. WISSING, F. GIORDANETTO, W. TOMLINSON, P. J. GREASLEY

Journal:

Journal of Thrombosis and Haemostasis

Year:

2009

Language:

english

File:

PDF, 463 KB

english, 2009

45

A human mitochondriopathy caused by AIF mutation

Modjtahedi, N, Giordanetto, F, Kroemer, G

Journal:

Cell Death & Differentiation

Year:

2010

Language:

english

File:

PDF, 272 KB

english, 2010

46

Re-examining the role of cytochrome c in cell death

Solary, Eric, Giordanetto, Fabrizio, Kroemer, Guido

Journal:

Nature Genetics

Year:

2008

Language:

english

File:

PDF, 334 KB

english, 2008

47

AIF and cyclophilin A cooperate in apoptosis-associated chromatinolysis

Candé, Céline, Vahsen, Nicola, Kouranti, Ilektra, Schmitt, Elise, Daugas, Eric, Spahr, Chris, Luban, Jeremy, Kroemer, Romano T, Giordanetto, Fabrizio, Garrido, Carmen

Journal:

Year:

2004

Language:

english

File:

PDF, 341 KB

english, 2004

48

Physical interaction of apoptosis-inducing factor with DNA and RNA

Vahsen, N, Candé, C, Dupaigne, P, Giordanetto, F, Kroemer, R T, Herker, E, Scholz, S, Modjtahedi, N, Madeo, F, Le Cam, E

Journal:

Year:

2005

Language:

english

File:

PDF, 836 KB

english, 2005

49

Structure–function analysis of the interaction between Bax and the cytomegalovirus-encoded protein vMIA

Pauleau, A-L, Larochette, N, Giordanetto, F, Scholz, S R, Poncet, D, Zamzami, N, Goldmacher, V S, Kroemer, G

Journal:

Year:

2007

Language:

english

File:

PDF, 488 KB

english, 2007

50

Discovery of N-(1-adamantyl)-2-(4-alkylpiperazin-1-yl)acetamide derivatives as T-type calcium channel (Cav3.2) inhibitors

Fabrizio Giordanetto, Laurent Knerr, Nidhal Selmi, Antonio Llinàs, Anders Lindqvist, Qing-Dong Wang, Pernilla Ståhlberg, Fredrik Thorstensson, Victoria Ullah, Kristina Nilsson, Gavin O’Mahony, Ågot Hö

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 851 KB

english, 2011

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