Our work

Publications

PDFs of all papers are available upon request. For a full list visit our profiles on the platforms below.

2026

AlphaFold-RandomWalk and AlphaFold-Ensemble: Sampling Alternative Protein Conformations with Perturbed Versions of AlphaFold

Taneja I, Llanos MA, Fernández-Quintero ML, Loeffler JR, Holcomb M, Ward AB, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.5c02004

2025

Meeko: Molecule Parametrization and Software Interoperability for Docking and Beyond

Santos-Martins D, He Y, Eberhardt J, Sharma P, Bruciaferri N, Holcomb M, Llanos MA, Hansel-Harris A, Barkdull AP, Tillack AF, Bianco G, Paulsen M-L, Mato J, Taneja I, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.5c02271

Structural insights into IMP2 dimerization and RNA binding

Zorc SA, Munoz-Tello P, O’Leary T, Yu X, Karadi Giridhar MN, Hondros AD, Hansel-Harris A, Forli S, Griffin PR, Kojetin DJ, Roy RN, Janiszewska M

Journal of Structural Biology

doi.org/10.1016/j.jsb.2025.108247

Structure-guided discovery of Otopetrin 1 inhibitors reveals druggable binding sites at the intrasubunit interface

Burendei B, Kaplan JP, Orellana GM, Liman ER, Forli S, Ward AB

Nature Communications

doi.org/10.1038/s41467-025-64392-0

Design principles of the common Gly-X6-Gly membrane protein building block

Golden K, Avarvarei C, Anderson CT, Holcomb M, Tang W, Dai X, Zhang M, Mailie CA, Sanchez BB, Chen JS, Forli S, Mravic M

Proceedings of the National Academy of Sciences

doi.org/10.1073/pnas.2503134122

Inactivation of peptidoglycan remodeling promotes antibiotic susceptibility in vancomycin-resistant Enterococcus faecium

Fam KT, Chodisetti PK, Wang Z, Homer JA, Smedley CJ, Kitamura S, Silva B, Xiong Y, Hansel-Harris A, Holcomb M

bioRxiv

doi.org/10.1101/2025.09.11.675460

Structure-based rational design of covalent probes

Holcomb M, Llanos M, Hansel-Harris A, Forli S

Communications Chemistry

doi.org/10.1038/s42004-025-01606-y

Sulfoxide-diazirine (SODA) as a Cleavable Photoaffinity Group To Enable the Identification of Photolabeled Modification Sites via LC–MS3

Chen S, Sanner MF, Gracias Leone D-L, Loroch S, Forli S, Verhelst SH

Analytical chemistry

doi.org/10.1021/acs.analchem.5c02409

Post-Translational Modifications Remodel Proteome-Wide Ligandability

Li W, Wei Q, Governa P, Llanos M, Chiu T-Y, Wozniak JM, Jadhav AM, Gathmann C, Cravatt J, Dongre A

bioRxiv

doi.org/10.1101/2025.07.31.667978

De novo-designed pMHC binders facilitate T cell–mediated cytotoxicity toward cancer cells

Johansen KH, Wolff DS, Scapolo B, Fernández-Quintero ML, Risager Christensen C, Loeffler JR, Rivera-de-Torre E, Overath MD, Kjærgaard Munk K, Morell O

Science

doi.org/10.1016/j.xcrm.2025.102353

Microbiota-derived secondary bile acids promote STING activation and antitumor activity

Yang X, Zhang X, Li W, Gharpure A, Hansel-Harris A, Tillack AF, Wu C, Hsieh Y-Z, Sulpizio A, Dikiy S

bioRxiv

doi.org/10.1101/2025.04.16.649255

A quantitative analysis of ligand binding at the protein-lipid bilayer interface

Barkdull AP, Holcomb M, Forli S

Communications Chemistry

doi.org/10.1038/s42004-025-01472-8

An mRNA Display Approach for Covalent Targeting of a Staphylococcus aureus Virulence Factor

Wang S, Woods EC, Jo J, Zhu J, Hansel-Harris A, Holcomb M, Llanos M, Pedowitz NJ, Upadhyay T, Bennett J

Journal of the American Chemical Society

doi.org/10.1021/jacs.4c15713

Docking guidance with experimental ligand structural density improves docking pose prediction and virtual screening performance

Hansel-Harris AT, Tillack AF, Santos-Martins D, Holcomb M, Forli S

Protein Science

doi.org/10.1002/pro.70082

The conformational landscape of human transthyretin revealed by cryo-EM

Basanta B, Nugroho K, Yan NL, Kline GM, Powers ET, Tsai FJ, Wu M, Hansel-Harris A, Chen JS, Forli S

Nature structural & molecular biology

doi.org/10.1038/s41594-024-01472-7

IP6, PF74 affect HIV-1 capsid stability through modulation of hexamer-hexamer tilt angle preference

Garza CM, Holcomb M, Santos-Martins D, Torbett BE, Forli S

Biophysical Journal

doi.org/10.1016/j.bpj.2024.12.016

CIAA: Integrated Proteomics and Structural Modeling for Understanding Cysteine Reactivity with Iodoacetamide Alkyne

Boatner LM, Eberhardt J, Shikwana F, Holcomb M, Lee P, Houk KN, Forli S, Backus KM

ACS Chemical Biology

doi.org/10.1021/acschembio.5c00225

Architecting Tensor Core-Based Reductions for Irregular Molecular Docking Kernels

Solis-Vasquez L, Tillack AF, Santos-Martins D, Koch A, Forli S

doi.org/10.1145/3731599.3767437

2024

CosolvKit: a Versatile Tool for Cosolvent MD Preparation and Analysis

Bruciaferri N, Eberhardt J, Llanos MA, Loeffler JR, Holcomb M, Fernandez-Quintero ML, Santos-Martins D, Ward AB, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.4c01398

Assessing AF2’s ability to predict structural ensembles of proteins

Riccabona JR, Spoendlin FC, Fischer A-LM, Loeffler JR, Quoika PK, Jenkins TP, Ferguson JA, Smorodina E, Laustsen AH, Greiff V, Forli S, Ward AB, Deane CM, Fernández-Quintero ML

Structure

doi.org/10.1016/j.str.2024.09.001

Enhanced mapping of small-molecule binding sites in cells

Wozniak JM, Li W, Governa P, Chen L-Y, Jadhav A, Dongre A, Forli S, Parker CG

Nature Chemical Biology

doi.org/10.1038/s41589-023-01514-z

Synergy of machine learning and density functional theory calculations for predicting experimental Lewis base affinity and Lewis polybase binding atoms

Huynh H, Le K, Vu L, Nguyen T, Holcomb M, Forli S, Phan H

Journal of Computational Chemistry

doi.org/10.1002/jcc.27329

The Role of Force Fields and Water Models in Protein Folding and Unfolding Dynamics

Fischer A-LM, Tichy A, Kokot J, Hoerschinger VJ, Wild RF, Riccabona JR, Loeffler JR, Waibl F, Quoika PK, Gschwandtner P, Forli S, Ward AB, Liedl KR, Zacharias M, Fernández-Quintero ML

Journal of Chemical Theory and Computation

doi.org/10.1021/acs.jctc.3c01106

Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors

Governa P, Biagi M, Manetti F, Forli S

RSC Medicinal Chemistry

doi.org/10.1039/D3MD00649B

2023

Reactive Docking: A Computational Method for High-Throughput Virtual Screenings of Reactive Species

Bianco G, Holcomb M, Santos-Martins D, Tillack A, Hansel-Harris A, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.3c00832

WaterKit: Thermodynamic Profiling of Protein Hydration Sites

Eberhardt J, Forli S

Journal of Chemical Theory and Computation

doi.org/10.1021/acs.jctc.2c01087

Richard Lerner’s Bioinspiration: Biomolecular Visualization and Modeling at Scripps Research

Olson AJ, Sanner MF, Goodsell DS, Forli S

Israel Journal of Chemistry

doi.org/10.1002/ijch.202300055

Stretching Peptides to Generate Small Molecule β-Strand Mimics

Adams ZC, Silvestri AP, Chiorean S, Flood DT, Balo BP, Shi Y, Holcomb M, Walsh SI, Maillie CA, Pierens GK, Forli S, Rosengren KJ, Dawson PE

ACS Central Science

doi.org/10.1021/acscentsci.2c01462

Ringtail: A Python Tool for Efficient Management and Storage of Virtual Screening Results

Hansel-Harris AT, Santos-Martins D, Bruciaferri N, Tillack AF, Holcomb M, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.3c00166

Orphan receptor GPR158 serves as a metabotropic glycine receptor: mGlyR

Laboute T, Zucca S, Holcomb M, Patil DN, Garza C, Wheatley BA, Roy RN, Forli S, Martemyanov KA

Science

doi.org/10.1126/science.add7150

2022

Evaluation of AlphaFold2 structures as docking targets

Holcomb M, Chang Y-T, Goodsell DS, Forli S

Protein Science

doi.org/10.1002/pro.4530

Performance evaluation of flexible macrocycle docking in AutoDock

Holcomb M, Santos-Martins D, Tillack AF, Forli S

QRB Discovery

doi.org/10.1017/qrd.2022.18

Diversity oriented clicking delivers β-substituted alkenyl sulfonyl fluorides as covalent human neutrophil elastase inhibitors

Cheng Y, Li G, Smedley CJ, Giel M-C, Kitamura S, Woehl JL, Bianco G, Forli S, Homer JA, Cappiello JR, Wolan DW, Moses JE, Sharpless KB

Proceedings of the National Academy of Sciences

doi.org/10.1073/pnas.2208540119

Benchmarking the performance of irregular computations in AutoDock-GPU molecular docking

Solis-Vasquez L, Tillack AF, Santos-Martins D, Koch A, LeGrand S, Forli S

Parallel Computing

doi.org/10.1016/j.parco.2021.102861

Structure-based virtual screening workflow to identify antivirals targeting HIV-1 capsid

Sun Q, Biswas A, Vijayan RSK, Craveur P, Forli S, Olson AJ, Castaner AE, Kirby KA, Sarafianos SG, Deng N, Levy R

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-022-00446-5

2021

AutoDock Vina 1.2.0: New Docking Methods, Expanded Force Field, and Python Bindings

Eberhardt J, Santos-Martins D, Tillack AF, Forli S

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.1c00203

Improving Docking Power for Short Peptides Using Random Forest

Sanner MF, Dieguez L, Forli S, Lis E

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.1c00573

Discovery of Potent Coumarin-Based Kinetic Stabilizers of Amyloidogenic Immunoglobulin Light Chains Using Structure-Based Design

Yan NL, Santos-Martins D, Nair R, Chu A, Wilson IA, Johnson KA, Forli S, Morgan GJ, Petrassi HM, Kelly JW

Journal of Medicinal Chemistry

doi.org/10.1021/acs.jmedchem.1c00339

Biased Docking for Protein–Ligand Pose Prediction

Arcon JP, Turjanski AG, Martí MA, Forli S

Protein-Ligand Interactions and Drug Design

doi.org/10.1007/978-1-0716-1209-5_3

Accelerating AutoDock4 with GPUs and Gradient-Based Local Search

Santos-Martins D, Solis-Vasquez L, Tillack AF, Sanner MF, Koch A, Forli S

Journal of Chemical Theory and Computation

doi.org/10.1021/acs.jctc.0c01006

2020

Supercomputer-Based Ensemble Docking Drug Discovery Pipeline with Application to Covid-19

Acharya A, Agarwal R, Baker MB, Baudry J, Bhowmik D, Boehm S, Byler KG, Chen SY, Coates L, Cooper CJ, Demerdash O, Daidone I, Eblen JD, Ellingson S, Forli S, Glaser J, Gumbart JC, Gunnels J, Hernandez O, Irle S, Kneller DW, Kovalevsky A, Larkin J, Lawrence TJ, LeGrand S, Liu SH, Mitchell JC, Park G, Parks JM, Pavlova A, Petridis L, Poole D, Pouchard L, Ramanathan A, Rogers DM, Santos-Martins D, Scheinberg A, Sedova A, Shen Y, Smith JC, Smith MD, Soto C, Tsaris A, Thavappiragasam M, Tillack AF, Vermaas JV, Vuong VQ, Yin J, Yoo S, Zahran M, Zanetti-Polzi L

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.0c01010

Structure, lipid scrambling activity and role in autophagosome formation of ATG9A

Maeda S, Yamamoto H, Kinch LN, Garza CM, Takahashi S, Otomo C, Grishin NV, Forli S, Mizushima N, Otomo T

Nature Structural & Molecular Biology

doi.org/10.1038/s41594-020-00520-2

A Strain-Specific Inhibitor of Receptor-Bound HIV-1 Targets a Pocket near the Fusion Peptide

Ozorowski G, Torres JL, Santos-Martins D, Forli S, Ward AB

Cell Reports

doi.org/10.1016/j.celrep.2020.108428

Selective and Effective: Current Progress in Computational Structure-Based Drug Discovery of Targeted Covalent Inhibitors

Bianco G, Goodsell DS, Forli S

Trends in Pharmacological Sciences

doi.org/10.1016/j.tips.2020.10.005

Synthetic, Mechanistic, and Biological Interrogation of Ginkgo biloba Chemical Space En Route to (−)-Bilobalide

Demoret RM, Baker MA, Ohtawa M, Chen S, Lam CC, Khom S, Roberto M, Forli S, Houk KN, Shenvi RA

Journal of the American Chemical Society

doi.org/10.1021/jacs.0c08231

Discovery of small-molecule enzyme activators by activity-based protein profiling

Kok BP, Ghimire S, Kim W, Chatterjee S, Johns T, Kitamura S, Eberhardt J, Ogasawara D, Xu J, Sukiasyan A, Kim SM, Godio C, Bittencourt JM, Cameron M, Galmozzi A, Forli S, Wolan DW, Cravatt BF, Boger DL, Saez E

Nature Chemical Biology

doi.org/10.1038/s41589-020-0555-4

The AutoDock suite at 30

Goodsell DS, Sanner MF, Olson AJ, Forli S

Protein Science

doi.org/10.1002/pro.3934

Structural basis for the stabilization of amyloidogenic immunoglobulin light chains by hydantoins

Yan NL, Santos-Martins D, Rennella E, Sanchez BB, Chen JS, Kay LE, Wilson IA, Morgan GJ, Forli S, Kelly JW

Bioorganic & Medicinal Chemistry Letters

doi.org/10.1016/j.bmcl.2020.127356

An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells

Vinogradova EV, Zhang X, Remillard D, Lazar DC, Suciu RM, Wang Y, Bianco G, Yamashita Y, Crowley VM, Schafroth MA, Yokoyama M, Konrad DB, Lum KM, Simon GM, Kemper EK, Lazear MR, Yin S, Blewett MM, Dix MM, Nguyen N, Shokhirev MN, Chin EN, Lairson LL, Melillo B, Schreiber SL, Forli S, Teijaro JR, Cravatt BF

Cell

doi.org/10.1016/j.cell.2020.07.001

Initial Analysis of the Arylomycin D Antibiotics

Tan YX, Peters DS, Walsh SI, Holcomb M, Santos-Martins D, Forli S, Romesberg FE

Journal of Natural Products

doi.org/10.1021/acs.jnatprod.9b01174

Charting Hydrogen Bond Anisotropy

Santos-Martins D, Forli S

Journal of Chemical Theory and Computation

doi.org/10.1021/acs.jctc.9b01248

Art and Science of the Cellular Mesoscale

Goodsell DS, Olson AJ, Forli S

Trends in Biochemical Sciences

doi.org/10.1016/j.tibs.2020.02.010

Integrative X-ray Structure and Molecular Modeling for the Rationalization of Procaspase-8 Inhibitor Potency and Selectivity

Xu JH, Eberhardt J, Hill-Payne B, González-Páez GE, Castellón JO, Cravatt BF, Forli S, Wolan DW, Backus KM

ACS Chemical Biology

doi.org/10.1021/acschembio.0c00019

Structural basis for strand-transfer inhibitor binding to HIV intasomes

Passos DO, Li M, Jóźwik IK, Zhao XZ, Santos-Martins D, Yang R, Smith SJ, Jeon Y, Forli S, Hughes SH, Burke TR, Craigie R, Lyumkis D

Science

doi.org/10.1126/science.aay8015

2019

Comparison of affinity ranking using AutoDock-GPU and MM-GBSA scores for BACE-1 inhibitors in the D3R Grand Challenge 4

El Khoury L, Santos-Martins D, Sasmal S, Eberhardt J, Bianco G, Ambrosio FA, Solis-Vasquez L, Koch A, Forli S, Mobley DL

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-019-00240-w

D3R Grand Challenge 4: prospective pose prediction of BACE1 ligands with AutoDock-GPU

Santos-Martins D, Eberhardt J, Bianco G, Solis-Vasquez L, Ambrosio FA, Koch A, Forli S

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-019-00241-9

Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs

Wang Y, Dix MM, Bianco G, Remsberg JR, Lee H-Y, Kalocsay M, Gygi SP, Forli S, Vite G, Lawrence RM, Parker CG, Cravatt BF

Nature Chemistry

doi.org/10.1038/s41557-019-0351-5

SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase

Zheng Q, Woehl JL, Kitamura S, Santos-Martins D, Smedley CJ, Li G, Forli S, Moses JE, Wolan DW, Sharpless KB

Proceedings of the National Academy of Sciences

doi.org/10.1073/pnas.1909972116

AutoGridFR: Improvements on AutoDock Affinity Maps and Associated Software Tools

Zhang Y, Forli S, Omelchenko A, Sanner MF

Journal of Computational Chemistry

doi.org/10.1002/jcc.26054

Integrative modeling of the HIV-1 ribonucleoprotein complex

Goodsell DS, Jewett A, Olson AJ, Forli S

PLOS Computational Biology

doi.org/10.1371/journal.pcbi.1007150

Novel Intersubunit Interaction Critical for HIV-1 Core Assembly Defines a Potentially Targetable Inhibitor Binding Pocket

Craveur P, Gres AT, Kirby KA, Liu D, Hammond JA, Deng Y, Forli S, Goodsell DS, Williamson JR, Sarafianos SG, Olson AJ

mBio

doi.org/10.1128/mbio.02858-18

AutoDock Bias: improving binding mode prediction and virtual screening using known protein–ligand interactions

Arcon JP, Modenutti CP, Avendaño D, Lopez ED, Defelipe LA, Ambrosio FA, Turjanski AG, Forli S, Marti MA

Bioinformatics

doi.org/10.1093/bioinformatics/btz152

Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone

Mosure SA, Shang J, Eberhardt J, Brust R, Zheng J, Griffin PR, Forli S, Kojetin DJ

Journal of Medicinal Chemistry

doi.org/10.1021/acs.jmedchem.8b01573

2018

Humanized GPIbα–von Willebrand factor interaction in the mouse

Kanaji S, Orje JN, Kanaji T, Kamikubo Y, Morodomi Y, Chen Y, Zarpellon A, Eberhardt J, Forli S, Fahs SA, Sood R, Haberichter SL, Montgomery RR, Ruggeri ZM

Blood Advances

doi.org/10.1182/bloodadvances.2018023507

Flap-site Fragment Restores Back Wild-type Behaviour in Resistant Form of HIV Protease

Luchi A, Angelina E, Bogado L, Forli S, Olson A, Peruchena N

Molecular Informatics

doi.org/10.1002/minf.201800053

“Inverse Drug Discovery” Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates

Mortenson DE, Brighty GJ, Plate L, Bare G, Chen W, Li S, Wang H, Cravatt BF, Forli S, Powers ET, Sharpless KB, Wilson IA, Kelly JW

Journal of the American Chemical Society

doi.org/10.1021/jacs.7b08366

2017

Global profiling of lysine reactivity and ligandability in the human proteome

Hacker SM, Backus KM, Lazear MR, Forli S, Correia BE, Cravatt BF

Nature Chemistry

doi.org/10.1038/nchem.2826

2016

A New Class of Allosteric HIV-1 Integrase Inhibitors Identified by Crystallographic Fragment Screening of the Catalytic Core Domain

Patel D, Antwi J, Koneru PC, Serrao E, Forli S, Kessl JJ, Feng L, Deng N, Levy RM, Fuchs JR, Olson AJ, Engelman AN, Bauman JD, Kvaratskhelia M, Arnold E

Journal of Biological Chemistry

doi.org/10.1074/jbc.M116.753384

Fragment-Based Analysis of Ligand Dockings Improves Classification of Actives

Belew RK, Forli S, Goodsell DS, O’Donnell TJ, Olson AJ

Journal of Chemical Information and Modeling

doi.org/10.1021/acs.jcim.6b00248

Directional Phosphorylation and Nuclear Transport of the Splicing Factor SRSF1 Is Regulated by an RNA Recognition Motif

Serrano P, Aubol BE, Keshwani MM, Forli S, Ma C-T, Dutta SK, Geralt M, Wüthrich K, Adams JA

Journal of Molecular Biology

doi.org/10.1016/j.jmb.2016.04.009

Proteome-wide covalent ligand discovery in native biological systems

Backus KM, Correia BE, Lum KM, Forli S, Horning BD, González-Páez GE, Chatterjee S, Lanning BR, Teijaro JR, Olson AJ, Wolan DW, Cravatt BF

Nature

doi.org/10.1038/nature18002

Natural Product Anacardic Acid from Cashew Nut Shells Stimulates Neutrophil Extracellular Trap Production and Bactericidal Activity

Hollands A, Corriden R, Gysler G, Dahesh S, Olson J, Raza Ali S, Kunkel MT, Lin AE, Forli S, Newton AC, Kumar GB, Nair BG, Perry JJP, Nizet V

Journal of Biological Chemistry

doi.org/10.1074/jbc.M115.695866

Computational protein–ligand docking and virtual drug screening with the AutoDock suite

Forli S, Huey R, Pique ME, Sanner MF, Goodsell DS, Olson AJ

Nature Protocols

doi.org/10.1038/nprot.2016.051

Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials

Fiore M, Forli S, Manetti F

Journal of Medicinal Chemistry

doi.org/10.1021/acs.jmedchem.5b01457

2015

AutoDockFR: Advances in Protein-Ligand Docking with Explicitly Specified Binding Site Flexibility

Ravindranath PA, Forli S, Goodsell DS, Olson AJ, Sanner MF

PLOS Computational Biology

doi.org/10.1371/journal.pcbi.1004586

Charting a Path to Success in Virtual Screening

Forli S

Molecules

doi.org/10.3390/molecules201018732

Covalent docking using autodock: Two-point attractor and flexible side chain methods

Bianco G, Forli S, Goodsell DS, Olson AJ

Protein Science

doi.org/10.1002/pro.2733

A Virtual Screen Discovers Novel, Fragment-Sized Inhibitors of Mycobacterium tuberculosis InhA

Perryman AL, Yu W, Wang X, Ekins S, Forli S, Li S-G, Freundlich JS, Tonge PJ, Olson AJ

Journal of Chemical Information and Modeling

doi.org/10.1021/ci500672v

Distinguishing Binders from False Positives by Free Energy Calculations: Fragment Screening Against the Flap Site of HIV Protease

Deng N, Forli S, He P, Perryman A, Wickstrom L, Vijayan RSK, Tiefenbrunn T, Stout D, Gallicchio E, Olson AJ, Levy RM

The Journal of Physical Chemistry B

doi.org/10.1021/jp506376z

Computational Challenges of Structure-Based Approaches Applied to HIV

Forli S, Olson AJ

Current Topics in Microbiology and Immunology

doi.org/10.1007/82_2015_432

Postdoctoral, Graduate and Undergraduate

2014

Identification of a Novel Drug Lead That Inhibits HCV Infection and Cell-to-Cell Transmission by Targeting the HCV E2 Glycoprotein

Al Olaby RR, Cocquerel L, Zemla A, Saas L, Dubuisson J, Vielmetter J, Marcotrigiano J, Khan AG, Catalan FV, Perryman AL, Freundlich JS, Forli S, Levy S, Balhorn R, Azzazy HM

PLOS ONE

doi.org/10.1371/journal.pone.0111333

3D molecular models of whole HIV-1 virions generated with cellPACK

Johnson GT, Goodsell DS, Autin L, Forli S, Sanner MF, Olson AJ

Faraday Discussions

doi.org/10.1039/C4FD00017J

AutoDock4Zn: An Improved AutoDock Force Field for Small-Molecule Docking to Zinc Metalloproteins

Santos-Martins D, Forli S, Ramos MJ, Olson AJ

Journal of Chemical Information and Modeling

doi.org/10.1021/ci500209e

Virtual screening of integrase inhibitors by large scale binding free energy calculations: the SAMPL4 challenge

Gallicchio E, Deng N, He P, Wickstrom L, Perryman AL, Santiago DN, Forli S, Olson AJ, Levy RM

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-014-9711-9

Blind prediction of HIV integrase binding from the SAMPL4 challenge

Mobley DL, Liu S, Lim NM, Wymer KL, Perryman AL, Forli S, Deng N, Su J, Branson K, Olson AJ

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-014-9723-5

Virtual screening with AutoDock Vina and the common pharmacophore engine of a low diversity library of fragments and hits against the three allosteric sites of HIV integrase: participation in the SAMPL4 protein–ligand binding challenge

Perryman AL, Santiago DN, Forli S, Santos-Martins D, Olson AJ

Journal of Computer-Aided Molecular Design

doi.org/10.1007/s10822-014-9709-3

Epothilones: From Discovery to Clinical Trials

Forli S

Current Topics in Medicinal Chemistry

doi.org/10.2174/1568026614666141130095855

2013

Crystallographic Fragment-Based Drug Discovery: Use of a Brominated Fragment Library Targeting HIV Protease

Tiefenbrunn T, Forli S, Happer M, Gonzalez A, Tsai Y, Soltis M, Elder JH, Olson AJ, Stout CD

Chemical Biology & Drug Design

doi.org/10.1111/cbdd.12227

Small Molecule Regulation of Protein Conformation by Binding in the Flap of HIV Protease

Tiefenbrunn T, Forli S, Baksh MM, Chang MW, Happer M, Lin Y-C, Perryman AL, Rhee J-K, Torbett BE, Olson AJ, Elder JH, Finn MG, Stout CD

ACS Chemical Biology

doi.org/10.1021/cb300611p

2012

A Force Field with Discrete Displaceable Waters and Desolvation Entropy for Hydrated Ligand Docking

Forli S, Olson AJ

Journal of Medicinal Chemistry

doi.org/10.1021/jm2005145

Cyclin-dependent kinases 5 template: Useful for virtual screening

Pitchuanchom S, Boonyarat C, Forli S, Olson AJ, Yenjai C

Computers in Biology and Medicine

doi.org/10.1016/j.compbiomed.2011.10.014

2011

N-Linked Peptidoresorc[4]arene-Based Receptors as Noncompetitive Inhibitors for α-Chymotrypsin

D’Acquarica I, Cerreto A, Delle Monache G, Subrizi F, Boffi A, Tafi A, Forli S, Botta B

The Journal of Organic Chemistry

doi.org/10.1021/jo102592f

2010

Virtual screening with AutoDock: theory and practice

Cosconati S, Stefano F, L. PA, Rodney H, S. GD, and Olson AJ

Expert Opinion on Drug Discovery

doi.org/10.1517/17460441.2010.484460

A Dynamic Model of HIV Integrase Inhibition and Drug Resistance

Perryman AL, Forli S, Morris GM, Burt C, Cheng Y, Palmer MJ, Whitby K, McCammon JA, Phillips C, Olson AJ

Journal of Molecular Biology

doi.org/10.1016/j.jmb.2010.01.033

Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-Inflammatory and Analgesic Agents. Synthesis and in Vitro and in Vivo Biological Evaluation

Biava M, Porretta GC, Poce G, Battilocchio C, Manetti F, Botta M, Forli S, Sautebin L, Rossi A, Pergola C, Ghelardini C, Galeotti N, Makovec F, Giordani A, Anzellotti P, Patrignani P, Anzini M

Journal of Medicinal Chemistry

doi.org/10.1021/jm901269y

2009

Evaluation of Novel Epothilone Analogues by means of a Common Pharmacophore and a QSAR Pseudoreceptor Model for Taxanes and Epothilones

Forli S, Manetti F, Altmann K-H, Botta M

ChemMedChem

doi.org/10.1002/cmdc.200900303

2008

Molecular Modeling Approaches to Study the Binding Mode on Tubulin of Microtubule Destabilizing and Stabilizing Agents

Botta M, Forli S, Magnani M, Manetti F

Topics in Current Chemistry

doi.org/10.1007/128_2008_20

Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents

Biava M, Porretta GC, Poce G, Supino S, Manetti F, Forli S, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Norcini M, Makovec F, Giordani A, Anzellotti P, Cirilli R, Ferretti R, Gallinella B, Torre FL, Anzini M, Patrignani P

Bioorganic & Medicinal Chemistry

doi.org/10.1016/j.bmc.2008.07.058

2007

Cyclooxygenase-2 Inhibitors. 1,5-Diarylpyrrol-3-acetic Esters with Enhanced Inhibitory Activity toward Cyclooxygenase-2 and Improved Cyclooxygenase-2/Cyclooxygenase-1 Selectivity

Biava M, Porretta GC, Poce G, Supino S, Forli S, Rovini M, Cappelli A, Manetti F, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Vivoli E, Makovec F, Anzellotti P, Patrignani P, Anzini M

Journal of Medicinal Chemistry

doi.org/10.1021/jm0707525

Lennard-Jones Potential and Dummy Atom Settings to Overcome the AUTODOCK Limitation in Treating Flexible Ring Systems

Forli S, Botta M

Journal of Chemical Information and Modeling

doi.org/10.1021/ci700036j

2006

A Combination of Docking/Dynamics Simulations and Pharmacophoric Modeling To Discover New Dual c-Src/Abl Kinase Inhibitors

Manetti F, Locatelli GA, Maga G, Schenone S, Modugno M, Forli S, Corelli F, Botta M

Journal of Medicinal Chemistry

doi.org/10.1021/jm060236z

2003

3D QSAR studies of the interaction between β-tubulin and microtubule stabilizing antimitotic agents (MSAA). A combined pharmacophore generation and pseudoreceptor modeling approach applied to taxanes and epothilones

Manetti F, Forli S, Maccari L, Corelli F, Botta M

Il Farmaco

doi.org/10.1016/S0014-827X(03)00052-1