Overview of Protein-Protein Interactions and Small-Molecule Inhibitors Under Clinical Development

No abstract is available for this paper.

• Publication year

  2018

• Venue

  Unknown venue

• Publication date

  Unknown publication date

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1007/978-981-13-0773-7_1
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

• From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

  2017cited by this paper
• BCL-2: Long and winding path from discovery to therapeutic target.

  2017cited by this paper
• Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.

  2016cited by this paper
• The BCL2 selective inhibitor venetoclax induces rapid onset apoptosis of CLL cells in patients via a TP53-independent mechanism.

  2016cited by this paper
• Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease.

  2016cited by this paper
• Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

  2016cited by this paper
• Therapeutic Small Molecules Target Inhibitor of Apoptosis Proteins in Cancers with Deregulation of Extrinsic and Intrinsic Cell Death Pathways

  2016cited by this paper
• Stabilization of protein-protein interaction complexes through small molecules.

  2016cited by this paper
• A distinct p53 target gene set predicts for response to the selective p53–HDM2 inhibitor NVP-CGM097

  2015cited by this paper
• Design, Virtual Screening, and Synthesis of Antagonists of αIIbβ3 as Antiplatelet Agents.

  2015cited by this paper
• Stabilizer-Guided Inhibition of Protein-Protein Interactions.

  2015cited by this paper
• Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia

  2015cited by this paper
• Flexibility and small pockets at protein–protein interfaces: New insights into druggability

  2015cited by this paper
• State-of-the-art strategies for targeting protein-protein interactions by small-molecule inhibitors.

  2015cited by this paper
• The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

  2015cited by this paper
• Small Macrocycles As Highly Active Integrin α2β1 Antagonists.

  2014cited by this paper
• Modulators of protein-protein interactions.

  2014cited by this paper
• Small-molecule inhibitors of protein-protein interactions: progressing toward the reality.

  2014cited by this paper
• Oncogenic protein interfaces: small molecules, big challenges

  2014cited by this paper
• Small molecule modulators of protein-protein interactions: selected case studies.

  2014cited by this paper
• Drug-Like Protein–Protein Interaction Modulators: Challenges and Opportunities for Drug Discovery and Chemical Biology

  2014cited by this paper
• SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression.

  2014cited by this paper
• Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.

  2014cited by this paper
• Hot spot-based design of small-molecule inhibitors for protein-protein interactions.

  2014cited by this paper
• Birinapant (TL32711), a Bivalent SMAC Mimetic, Targets TRAF2-Associated cIAPs, Abrogates TNF-Induced NF-κB Activation, and Is Active in Patient-Derived Xenograft Models

  2014cited by this paper
• Targeting protein-protein interaction by small molecules.

  2014cited by this paper
• MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.

  2013cited by this paper
• Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.

  2013cited by this paper
• Learning and Confirming with Preclinical Studies: Modeling and Simulation in the Discovery of GDC-0917, an Inhibitor of Apoptosis Proteins Antagonist

  2013cited by this paper
• Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice.

  2013cited by this paper
• Inhibition of α-helix-mediated protein-protein interactions using designed molecules.

  2013cited by this paper
• Targeting protein-protein interactions as an anticancer strategy.

  2013cited by this paper
• Protein-protein interactions as druggable targets: recent technological advances.

  2013cited by this paper
• Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.

  2013cited by this paper
• Druggable protein-protein interactions--from hot spots to hot segments.

  2013cited by this paper
• ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

  2013cited by this paper
• Protein–protein interaction inhibitors get into the groove

  2012cited by this paper
• Small-molecule stabilization of protein-protein interactions: an underestimated concept in drug discovery?

  2012cited by this paper
• Features of protein–protein interactions that translate into potent inhibitors: topology, surface area and affinity

  2012cited by this paper
• Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

  2012cited by this paper
• Targeting protein-protein interactions and fragment-based drug discovery.

  2012cited by this paper
• Structural biology and drug discovery for protein-protein interactions.

  2012cited by this paper
• Laparoscopic and gasless laparoscopic sigmoid colon vaginoplasty in women with vaginal agenesis.

  2012cited by this paper
• Minimal ensembles of side chain conformers for modeling protein–protein interactions

  2012cited by this paper
• A leap into the chemical space of protein-protein interaction inhibitors.

  2012cited by this paper
• Phase II Study of Single-Agent Navitoclax (ABT-263) and Biomarker Correlates in Patients with Relapsed Small Cell Lung Cancer

  2012cited by this paper
• Druggability assessment of protein-protein interfaces.

  2011cited by this paper
• A Phase I First-in-Human Pharmacokinetic and Pharmacodynamic Study of Serdemetan in Patients with Advanced Solid Tumors

  2011cited by this paper
• The neuroprotective effect of propofol against brain ischemia mediated by the glutamatergic signaling pathway in rats

  2011cited by this paper
• Discovery of modulators of protein-protein interactions: current approaches and limitations.

  2011cited by this paper
• Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.

  2011cited by this paper
• Hydrophobic Binding Hot Spots of Bcl-xL Protein-Protein Interfaces by Cosolvent Molecular Dynamics Simulation.

  2011cited by this paper
• Structural conservation of druggable hot spots in protein–protein interfaces

  2011cited by this paper
• Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

  2010cited by this paper
• RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo.

  2010cited by this paper
• Small‐molecule protein–protein interaction inhibitors: Therapeutic potential in light of molecular size, chemical space, and ligand binding efficiency considerations

  2010cited by this paper
• Suppression of inflammation by a synthetic histone mimic

  2010cited by this paper
• Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.

  2010cited by this paper
• Targeting protein-protein interactions for therapeutic intervention: a challenge for the future.

  2009cited by this paper
• Long-timescale molecular dynamics simulations of protein structure and function.

  2009cited by this paper
• What induces pocket openings on protein surface patches involved in protein–protein interactions?

  2009cited by this paper
• Predicting druggable binding sites at the protein-protein interface.

  2009cited by this paper
• Principles of protein-protein interactions: what are the preferred ways for proteins to interact?

  2008cited by this paper
• Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax).

  2008cited by this paper
• Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

  2008cited by this paper
• In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics.

  2008cited by this paper
• Estimating the size of the human interactome

  2008cited by this paper
• An empirical framework for binary interactome mapping

  2008cited by this paper
• ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

  2008cited by this paper
• Small-molecule inhibitors of protein-protein interactions.

  2008cited by this paper
• Drug-like inhibitors of protein-protein interactions: a structural examination of effective protein mimicry.

  2008cited by this paper
• Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

  2007cited by this paper
• Reaching for high-hanging fruit in drug discovery at protein–protein interfaces

  2007cited by this paper
• Structure-based maximal affinity model predicts small-molecule druggability

  2007cited by this paper
• Transient pockets on protein surfaces involved in protein-protein interaction.

  2007cited by this paper
• Alpha4-integrin antagonism--an effective approach for the treatment of inflammatory diseases?

  2007cited by this paper
• Hot spots—A review of the protein–protein interface determinant amino‐acid residues

  2007cited by this paper
• Design, synthesis, and computational studies of inhibitors of Bcl-XL.

  2006cited by this paper
• Drugs Targeting Protein–Protein Interactions

  2006cited by this paper
• Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.

  2006cited by this paper
• Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis.

  2006cited by this paper
• Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

  2006cited by this paper
• An inhibitor of Bcl-2 family proteins induces regression of solid tumours

  2005cited by this paper
• Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

  2005cited by this paper
• Small-molecule inhibitors of protein–protein interactions: progressing towards the dream

  2004cited by this paper
• Therapeutics of Platelet Glycoprotein IIb/IIIa Receptor Antagonism

  2004cited by this paper
• Crystal Structure of the E2 Transactivation Domain of Human Papillomavirus Type 11 Bound to a Protein Interaction Inhibitor*

  2004cited by this paper
• Binding of small molecules to an adaptive protein–protein interface

  2003cited by this paper
• Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist.

  2002cited by this paper
• Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule.

  2002cited by this paper
• Convergent solutions to binding at a protein-protein interface.

  2000cited by this paper
• Protein-Protein Interactions in Receptor Activation and Intracellular Signalling

  2000cited by this paper
• The atomic structure of protein-protein recognition sites.

  1999cited by this paper
• Anatomy of hot spots in protein interfaces.

  1998cited by this paper
• The Bcl-2 protein family: arbiters of cell survival.

  1998cited by this paper
• Structural plasticity in a remodeled protein-protein interface.

  1997cited by this paper
• Structure of Bcl-xL-Bak Peptide Complex: Recognition Between Regulators of Apoptosis

  1997cited by this paper
• Principles of protein-protein interactions.

  1996cited by this paper
• Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.

  1995cited by this paper
• A hot spot of binding energy in a hormone-receptor interface

  1995cited by this paper

• Development of small-molecule Tau-SH3 interaction inhibitors that prevent amyloid-β toxicity and network hyperexcitability

  2023cites this paper