Literature DB >> 22743979

Antibody-enabled small-molecule drug discovery.

Alastair D G Lawson1.   

Abstract

Although antibody-based therapeutics have become firmly established as medicines for serious diseases, the value of antibodies as tools in the early stages of small-molecule drug discovery is only beginning to be realized. In particular, antibodies may provide information to reduce risk in small-molecule drug discovery by enabling the validation of targets and by providing insights into the design of small-molecule screening assays. Moreover, antibodies can act as guides in the quest for small molecules that have the ability to modulate protein-protein interactions, which have traditionally only been considered to be tractable targets for biological drugs. The development of small molecules that have similar therapeutic effects to current biologics has the potential to benefit a broader range of patients at earlier stages of disease.

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Year:  2012        PMID: 22743979     DOI: 10.1038/nrd3756

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN: 1474-1776            Impact factor:   84.694


  64 in total

Review 1.  Small-molecule inhibitors of protein-protein interactions: progressing towards the dream.

Authors:  Michelle R Arkin; James A Wells
Journal:  Nat Rev Drug Discov       Date:  2004-04       Impact factor: 84.694

Review 2.  Structural and mechanistic insight into how antibodies inhibit serine proteases.

Authors:  Rajkumar Ganesan; Charles Eigenbrot; Daniel Kirchhofer
Journal:  Biochem J       Date:  2010-09-01       Impact factor: 3.857

Review 3.  Targeting protein-protein interactions with small molecules: challenges and perspectives for computational binding epitope detection and ligand finding.

Authors:  Domingo González-Ruiz; Holger Gohlke
Journal:  Curr Med Chem       Date:  2006       Impact factor: 4.530

4.  Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis.

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Journal:  J Am Chem Soc       Date:  2011-02-15       Impact factor: 15.419

5.  Recombinant anti-sialidase single-chain variable fragment antibody. Characterization, formation of dimer and higher-molecular-mass multimers and the solution of the crystal structure of the single-chain variable fragment/sialidase complex.

Authors:  A A Kortt; R L Malby; J B Caldwell; L C Gruen; N Ivancic; M C Lawrence; G J Howlett; R G Webster; P J Hudson; P M Colman
Journal:  Eur J Biochem       Date:  1994-04-01

6.  The development of activating and inhibiting camelid VHH domains against human protein kinase C epsilon.

Authors:  Milla M I Paalanen; Elina Ekokoski; Mohamed El Khattabi; Raimo K Tuominen; C Theo Verrips; Johannes Boonstra; Christophe Blanchetot
Journal:  Eur J Pharm Sci       Date:  2011-01-08       Impact factor: 4.384

7.  Unraveling the allosteric mechanism of serine protease inhibition by an antibody.

Authors:  Rajkumar Ganesan; Charles Eigenbrot; Yan Wu; Wei-Ching Liang; Steven Shia; Michael T Lipari; Daniel Kirchhofer
Journal:  Structure       Date:  2009-12-09       Impact factor: 5.006

8.  Mutations in PCSK9 cause autosomal dominant hypercholesterolemia.

Authors:  Marianne Abifadel; Mathilde Varret; Jean-Pierre Rabès; Delphine Allard; Khadija Ouguerram; Martine Devillers; Corinne Cruaud; Suzanne Benjannet; Louise Wickham; Danièle Erlich; Aurélie Derré; Ludovic Villéger; Michel Farnier; Isabel Beucler; Eric Bruckert; Jean Chambaz; Bernard Chanu; Jean-Michel Lecerf; Gerald Luc; Philippe Moulin; Jean Weissenbach; Annick Prat; Michel Krempf; Claudine Junien; Nabil G Seidah; Catherine Boileau
Journal:  Nat Genet       Date:  2003-06       Impact factor: 38.330

9.  Nanobody-aided structure determination of the EpsI:EpsJ pseudopilin heterodimer from Vibrio vulnificus.

Authors:  Anita Y Lam; Els Pardon; Konstantin V Korotkov; Wim G J Hol; Jan Steyaert
Journal:  J Struct Biol       Date:  2008-12-10       Impact factor: 2.867

10.  Allosteric control of ligand-binding affinity using engineered conformation-specific effector proteins.

Authors:  Shahir S Rizk; Marcin Paduch; John H Heithaus; Erica M Duguid; Andrew Sandstrom; Anthony A Kossiakoff
Journal:  Nat Struct Mol Biol       Date:  2011-03-06       Impact factor: 15.369

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  24 in total

1.  New Chemical Modalities and Strategic Thinking in Early Drug Discovery.

Authors:  Maria-Jesus Blanco; Kevin M Gardinier
Journal:  ACS Med Chem Lett       Date:  2020-01-14       Impact factor: 4.345

2.  Exploring the structural origins of cryptic sites on proteins.

Authors:  Dmitri Beglov; David R Hall; Amanda E Wakefield; Lingqi Luo; Karen N Allen; Dima Kozakov; Adrian Whitty; Sandor Vajda
Journal:  Proc Natl Acad Sci U S A       Date:  2018-03-26       Impact factor: 11.205

3.  Multiplex Three-Dimensional Mapping of Macromolecular Drug Distribution in the Tumor Microenvironment.

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Journal:  Mol Cancer Ther       Date:  2018-10-15       Impact factor: 6.261

4.  A general protocol for the generation of Nanobodies for structural biology.

Authors:  Els Pardon; Toon Laeremans; Sarah Triest; Søren G F Rasmussen; Alexandre Wohlkönig; Armin Ruf; Serge Muyldermans; Wim G J Hol; Brian K Kobilka; Jan Steyaert
Journal:  Nat Protoc       Date:  2014-02-27       Impact factor: 13.491

5.  Uncommon structural motifs dominate the antigen binding site in human autoantibodies reactive with basement membrane collagen.

Authors:  Mary H Foster; Elizabeth S Buckley; Benny J Chen; Kwan-Ki Hwang; Amy G Clark
Journal:  Mol Immunol       Date:  2016-07-20       Impact factor: 4.407

6.  Bioactive Macrocyclic Inhibitors of the PD-1/PD-L1 Immune Checkpoint.

Authors:  Katarzyna Magiera-Mularz; Lukasz Skalniak; Krzysztof M Zak; Bogdan Musielak; Ewa Rudzinska-Szostak; Łukasz Berlicki; Justyna Kocik; Przemyslaw Grudnik; Dominik Sala; Tryfon Zarganes-Tzitzikas; Shabnam Shaabani; Alexander Dömling; Grzegorz Dubin; Tad A Holak
Journal:  Angew Chem Int Ed Engl       Date:  2017-09-26       Impact factor: 15.336

Review 7.  Nanobodies to Study G Protein-Coupled Receptor Structure and Function.

Authors:  Aashish Manglik; Brian K Kobilka; Jan Steyaert
Journal:  Annu Rev Pharmacol Toxicol       Date:  2016-12-07       Impact factor: 13.820

8.  AbPredict 2: a server for accurate and unstrained structure prediction of antibody variable domains.

Authors:  Gideon Lapidoth; Jake Parker; Jaime Prilusky; Sarel J Fleishman
Journal:  Bioinformatics       Date:  2019-05-01       Impact factor: 6.937

9.  Dynamic design: manipulation of millisecond timescale motions on the energy landscape of cyclophilin A.

Authors:  Jordi Juárez-Jiménez; Arun A Gupta; Gogulan Karunanithy; Antonia S J S Mey; Charis Georgiou; Harris Ioannidis; Alessio De Simone; Paul N Barlow; Alison N Hulme; Malcolm D Walkinshaw; Andrew J Baldwin; Julien Michel
Journal:  Chem Sci       Date:  2020-01-15       Impact factor: 9.825

10.  Structure of a Potential Therapeutic Antibody Bound to Interleukin-16 (IL-16): MECHANISTIC INSIGHTS AND NEW THERAPEUTIC OPPORTUNITIES.

Authors:  Gareth Hall; Eilish Cullen; Kovilen Sawmynaden; Joanne Arnold; Simon Fox; Richard Cowan; Frederick W Muskett; David Matthews; Andrew Merritt; Catherine Kettleborough; William Cruikshank; Debra Taylor; Richard Bayliss; Mark D Carr
Journal:  J Biol Chem       Date:  2016-05-26       Impact factor: 5.157

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