MolSnapper: Conditioning Diffusion for Structure-Based Drug Design

被引:4
作者
Ziv, Yael [1 ]
Imrie, Fergus [1 ]
Marsden, Brian [2 ]
Deane, Charlotte M. [1 ]
机构
[1] Univ Oxford, Dept Stat, Oxford OX1 3LB, England
[2] Univ Oxford, Nuffield Dept Med, Oxford OX3 7BN, England
关键词
SCREENING LIBRARIES; INHIBITORS; DISCOVERY;
D O I
10.1021/acs.jcim.4c02008
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Generative models have emerged as potentially powerful methods for molecular design, yet challenges persist in generating molecules that effectively bind to the intended target. The ability to control the design process and incorporate prior knowledge would be highly beneficial for better tailoring molecules to fit specific binding sites. In this paper, we introduce MolSnapper, a novel tool that is able to condition diffusion models for structure-based drug design by seamlessly integrating expert knowledge in the form of 3D pharmacophores. We demonstrate through comprehensive testing on both the CrossDocked and Binding MOAD data sets that our method generates molecules better tailored to fit a given binding site, achieving high structural and chemical similarity to the original molecules. Additionally, MolSnapper yields approximately twice as many valid molecules as alternative methods.
引用
收藏
页码:4263 / 4273
页数:11
相关论文
共 53 条
[1]   The $2.6 Billion Pill - Methodologic and Policy Considerations [J].
Avorn, Jerry .
NEW ENGLAND JOURNAL OF MEDICINE, 2015, 372 (20) :1877-1879
[2]   GEOM, energy-annotated molecular conformations for property prediction and molecular generation [J].
Axelrod, Simon ;
Gomez-Bombarelli, Rafael .
SCIENTIFIC DATA, 2022, 9 (01)
[3]   New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays [J].
Baell, Jonathan B. ;
Holloway, Georgina A. .
JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (07) :2719-2740
[4]   Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors [J].
Boby, Melissa L. ;
Fearon, Daren ;
Ferla, Matteo ;
Filep, Mihajlo ;
Koekemoer, Lizbe ;
Robinson, Matthew C. ;
Chodera, John D. ;
Lee, Alpha A. ;
London, Nir ;
von Delft, Annette ;
von Delft, Frank .
SCIENCE, 2023, 382 (6671)
[5]  
Bradshaw J, 2019, ADV NEUR IN, V32
[6]   Lessons learnt from assembling screening libraries for drug discovery for neglected diseases [J].
Brenk, Ruth ;
Schipani, Alessandro ;
James, Daniel ;
Krasowski, Agata ;
Gilbert, Ian Hugh ;
Frearson, Julie ;
Wyatt, Paul Graham .
CHEMMEDCHEM, 2008, 3 (03) :435-444
[7]   PoseBusters: AI-based docking methods fail to generate physically valid poses or generalise to novel sequences [J].
Buttenschoen, Martin ;
Morris, Garrett M. ;
Deane, Charlotte M. .
CHEMICAL SCIENCE, 2024, 15 (09) :3130-3139
[8]   Regulation of protein-ligand binding affinity by hydrogen bond pairing [J].
Chen, Deliang ;
Oezguen, Numan ;
Urvil, Petri ;
Ferguson, Colin ;
Dann, Sara M. ;
Savidge, Tor C. .
SCIENCE ADVANCES, 2016, 2 (03)
[9]   SCScore: Synthetic Complexity Learned from a Reaction Corpus [J].
Coley, Connor W. ;
Rogers, Luke ;
Green, William H. ;
Jensen, Klavs F. .
JOURNAL OF CHEMICAL INFORMATION AND MODELING, 2018, 58 (02) :252-261
[10]   PILOT: equivariant diffusion for pocket-conditioned de novo ligand generation with multi-objective guidance via importance sampling [J].
Cremer, Julian ;
Le, Tuan ;
Noe, Frank ;
Clevert, Djork-Arne ;
Schuett, Kristof T. .
CHEMICAL SCIENCE, 2024, 15 (36) :14954-14967