Chemically induced proximity in biology and medicine

THE CONSTITUTION AND FUNDAMENTAL PROPERTIES OF SOLIDS AND LIQUIDS. PART I. SOLIDS.

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The new frontier of genome engineering with CRISPR-Cas9

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Reaction-rate theory: fifty years after Kramers

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Selective inhibition of BET bromodomains

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The constitution and fundamental properties of solids and liquids

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Clearance of p16Ink4a-positive senescent cells delays ageing-associated disorders

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Abscisic Acid: Emergence of a Core Signaling Network

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Naturally occurring p16Ink4a-positive cells shorten healthy lifespan

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BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

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SH2 domains recognize specific phosphopeptide sequences

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Identification of a Primary Target of Thalidomide Teratogenicity

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A signature motif in transcriptional co-activators mediates binding to nuclear receptors

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A transcriptional co-repressor that interacts with nuclear hormone receptors

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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Targeted Degradation of CTCF Decouples Local Insulation of Chromosome Domains from Genomic Compartmentalization

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Mechanism of auxin perception by the TIR1 ubiquitin ligase

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An auxin-based degron system for the rapid depletion of proteins in nonplant cells

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Identification of calcineurin as a key signalling enzyme in T-lymphocyte activation

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Inducible Apoptosis as a Safety Switch for Adoptive Cell Therapy

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Catalytic in vivo protein knockdown by small-molecule PROTACs

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Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

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A Rapid, Reversible, and Tunable Method to Regulate Protein Function in Living Cells Using Synthetic Small Molecules

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ChromEMT: Visualizing 3D chromatin structure and compaction in interphase and mitotic cells

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Controlling Signal Transduction with Synthetic Ligands

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A split-Cas9 architecture for inducible genome editing and transcription modulation

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Rapid protein depletion in human cells by auxin-inducible degron tagging with short homology donors

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Modular PROTAC design for the degradation of oncogenic BCR-ABL

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The auxin-inducible degradation (AID) system enables versatile conditional protein depletion in C. elegans

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Reversible compartmentalization of de novo purine biosynthetic complexes in living cells

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Oligomerization of STIM1 couples ER calcium depletion to CRAC channel activation

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Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction

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Redesigning an FKBP–ligand interface to generate chemical dimerizers with novel specificity

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The Anchor-Away Technique: Rapid, Conditional Establishment of Yeast Mutant Phenotypes

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A humanized system for pharmacologic control of gene expression

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Infusion of donor-derived CD19-redirected virus-specific T cells for B-cell malignancies relapsed after allogeneic stem cell transplant: a phase 1 study

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HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

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A Comprehensive Mathematical Model for Three-Body Binding Equilibria

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Dosage-dependent modifiers of polycomb and antennapedia mutations in Drosophila.

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Treating B-cell cancer with T cells expressing anti-CD19 chimeric antigen receptors

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Dynamics and Memory of Heterochromatin in Living Cells

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Chronic myeloid leukemia stem cells are not dependent on Bcr-Abl kinase activity for their survival

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An expanded tool kit for the auxin‐inducible degron system in budding yeast

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BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

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Regulation of Protein Secretion Through Controlled Aggregation in the Endoplasmic Reticulum

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Complex transcriptional modulation with orthogonal and inducible dCas9 regulators

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Fat apoptosis through targeted activation of caspase 8: a new mouse model of inducible and reversible lipoatrophy

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Engineering the ABA Plant Stress Pathway for Regulation of Induced Proximity

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Transcription control by the ENL YEATS domain in acute leukaemia

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Regulated Delivery of Therapeutic Proteins After in Vivo Somatic Cell Gene Transfer

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Solution Structure of FKBP, a Rotamase Enzyme and Receptor for FK506 and Rapamycin

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TOR kinase domains are required for two distinct functions, only one of which is inhibited by rapamycin

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Inducible, reversible system for the rapid and complete degradation of proteins in mammalian cells

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Dynamics of BAF–Polycomb complex opposition on heterochromatin in normal and oncogenic states

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Evidence that Loading of Cohesin Onto Chromosomes Involves Opening of Its SMC Hinge

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Manipulation of nuclear architecture through CRISPR-mediated chromosomal looping

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Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins.

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Long-term pharmacologically regulated expression of erythropoietin in primates following AAV-mediated gene transfer

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Structure of human cyclophilin and its binding site for cyclosporin A determined by X-ray crystallography and NMR spectroscopy

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BAF complexes facilitate decatenation of DNA by topoisomerase IIα

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Dimeric ligands define a role for transcriptional activation domains in reinitiation

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Inducible Caspase-9 Selectively Modulates the Toxicities of CD19-Specific Chimeric Antigen Receptor-Modified T Cells

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Oligomerization activates c-Raf-1 through a Ras-dependent mechanism

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Rapid and orthogonal logic gating with a gibberellin-induced dimerization system

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Inducible caspase-9 suicide gene controls adverse effects from alloreplete T cells after haploidentical stem cell transplantation

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Rapamycin Analogs with Differential Binding Specificity Permit Orthogonal Control of Protein Activity

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Localized light-induced protein dimerization in living cells using a photocaged dimerizer

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Plk4 haploinsufficiency causes mitotic infidelity and carcinogenesis

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Smarca4 ATPase mutations disrupt direct eviction of PRC1 from chromatin

Stanton, B. Z., Hodges, H. C., Calarco, J. P., Braun, S. M. G., Ku, W. L., Kadoch, C., Zhao, K., & Crabtree, G. R. (2016) · Nature Genetics · doi:10.1038/ng.3735 · Cited by 204 · see citing works

AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin

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Cell signaling can direct either binary or graded transcriptional responses

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Harnessing Chaperones to Generate Small-Molecule Inhibitors of Amyloid ß Aggregation

Gestwicki, J. E., Crabtree, G. R., & Graef, I. A. (2004) · Science · doi:10.1126/science.1101262 · Cited by 200 · see citing works

Synthetic activation of caspases: Artificial death switches

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Long-term outcome after haploidentical stem cell transplant and infusion of T cells expressing the inducible caspase 9 safety transgene

Zhou, X., Stasi, A. D., Tey, S., Krance, R. A., Martinez, C. A., Leung, K. S., Durett, A. G., Wu, M.-F., Liu, H., Leen, A. M., et al. (2014) · Blood · doi:10.1182/blood-2014-01-551671 · Cited by 173 · see citing works

Conditional Protein Splicing: A New Tool to Control Protein Structure and Function in Vitro and in Vivo

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Rapid and reversible epigenome editing by endogenous chromatin regulators

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p53 protects against genome instability following centriole duplication failure

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Functional analysis of Fas signaling in vivo using synthetic inducers of dimerization

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Signal transduction in T lymphocytes using a conditional allele of Sos.

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Selective Protein−Protein Interactions Direct Channeling of Intermediates between Polyketide Synthase Modules

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Conditional Protein Alleles Using Knockin Mice and a Chemical Inducer of Dimerization

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The Cyc8–Tup1 complex inhibits transcription primarily by masking the activation domain of the recruiting proteinPreprint

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Chemical rescue of cleft palate and midline defects in conditional GSK-3β mice

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Rapid targeting of nuclear proteins to the cytoplasm

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Improved Artificial Death Switches Based on Caspases and FADD

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Rapid and Reversible Chemical Inactivation of Synaptic Transmission in Genetically Targeted Neurons

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Condensin aids sister chromatid decatenation by topoisomerase II

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A Binding Site Hotspot Map of the FKBP12–Rapamycin–FRB Ternary Complex by Photoaffinity Labeling and Mass Spectrometry-Based Proteomics

Flaxman, H. A., Chang, C., Wu, H., Nakamoto, C. H., & Woo, C. M. (2019) · Journal of the American Chemical Society · doi:10.1021/jacs.9b03764 · Cited by 51 · see citing works

Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence

Duran-Frigola, M., Cigler, M., & Winter, G. E. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c11098 · Cited by 50 · see citing works

Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation

Čermáková, K., & Hodges, H. C. (2018) · Molecules · doi:10.3390/molecules23081958 · Cited by 49 · see citing works

Engineered platelets as targeted protein degraders and application to breast cancer models

Chen, Y., Pal, S., Li, W., Liu, F., Yuan, S., & Hu, Q. (2024) · Nature Biotechnology · doi:10.1038/s41587-024-02494-8 · Cited by 47 · see citing works

Proximity-inducing modalities: the past, present, and future

Singh, S., Tian, W., Severance, Z. C., Chaudhary, S. K., Anokhina, V. S., Mondal, B., Pergu, R., Singh, P. R., Dhawa, U., Singha, S., et al. (2023) · Chemical Society Reviews · doi:10.1039/d2cs00943a · Cited by 45 · see citing works

An orthogonalized PYR1-based CID module with reprogrammable ligand-binding specificity

Park, S., Qiu, J., Wei, S., Peterson, F. C., Beltrán, J., Medina‐Cucurella, A. V., Vaidya, A. S., Xing, Z., Volkman, B. F., Nusinow, D. A., et al. (2023) · Nature Chemical Biology · doi:10.1038/s41589-023-01447-7 · Cited by 43 · see citing works

Nanoparticle‐Mediated Targeted Protein Degradation: An Emerging Therapeutics Technology

Baker, A., Ho, A. P. T., Itzhaki, L. S., & Fruk, L. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202503958 · Cited by 44 · see citing works

Mandipropamid as a chemical inducer of proximity for in vivo applications

Ziegler, M. J., Yserentant, K., Dunsing, V., Middel, V., Gralak, A. J., Pakari, K., Bargstedt, J., Kern, C., Petrich, A., Chiantia, S., et al. (2021) · Nature Chemical Biology · doi:10.1038/s41589-021-00922-3 · Cited by 43 · see citing works

Enhancing Prime Editing Efficiency and Flexibility with Tethered and Split pegRNAs

Feng, Y., Liu, S., Mo, Q., Xiao, X., Liu, P., & Ma, H. (2022) · Protein & Cell · doi:10.1093/procel/pwac014 · Cited by 42 · see citing works

E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance

Hanzl, A., Barone, E., Bauer, S., Yue, H., Nowak, R. P., Hahn, E., Pankevich, E. V., Koren, A., Kubicek, S., Fischer, E. S., et al. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c10784 · Cited by 41 · see citing works

Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERRγ Protein–Protein Interaction as a Molecular Glue Drug Discovery Approach

Somsen, B. A., Schellekens, R. J. C., Verhoef, C. J. A., Arkin, M. R., Ottmann, C., Cossar, P. J., & Brunsveld, L. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c12781 · Cited by 41 · see citing works

From bench to bedside: current development and emerging trend of KRAS-targeted therapy

Chen, Y., Liu, Q.-P., Xie, H., & Ding, J. (2023) · Acta Pharmacologica Sinica · doi:10.1038/s41401-023-01194-4 · Cited by 44 · see citing works

Small-molecule binding and sensing with a designed protein family

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Engineering synthetic phosphorylation signaling networks in human cells

Yang, X., Rocks, J. W., Jiang, K., Walters, A. J., Rai, K., Liu, J., Nguyen, J., Olson, S. D., Mehta, P., Collins, J. J., et al. (2025) · Science · doi:10.1126/science.adm8485 · Cited by 40 · see citing works

Harnessing Effective Molarity to Design an Electrochemical DNA‐based Platform for Clinically Relevant Antibody Detection

Rossetti, M., Brannetti, S., Mocenigo, M., Marini, B., Ippodrino, R., & Porchetta, A. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.202005124 · Cited by 39 · see citing works

PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

Maneiro, M., Vita, E. D., Conole, D., Kounde, C. S., Zhang, Q., & Tate, E. W. (2021) · Progress in medicinal chemistry · doi:10.1016/bs.pmch.2021.01.002 · Cited by 38 · see citing works

Emerging Trends in Cancer Drug Discovery—From Drugging the “Undruggable” to Overcoming Resistance

Rudolph, J., Settleman, J., & Malek, S. (2021) · Cancer Discovery · doi:10.1158/2159-8290.cd-21-0260 · Cited by 38 · see citing works

A DNA‐Mediated Chemically Induced Dimerization (D‐CID) Nanodevice for Nongenetic Receptor Engineering To Control Cell Behavior

Li, H., Wang, M., Shi, T., Yang, S. Z., Zhang, J., Wang, H., & Nie, Z. (2018) · Angewandte Chemie · doi:10.1002/ange.201806155 · Cited by 38 · see citing works

Applications of protein ubiquitylation and deubiquitylation in drug discovery

Chen, Y., Xue, H., & Jin, J. (2024) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2024.107264 · Cited by 37 · see citing works

Creating Red Light-Switchable Protein Dimerization Systems as Genetically Encoded Actuators with High Specificity

Huang, Z., Li, Z., Zhang, X., Kang, S., Dong, R., Sun, L., Fu, X., Vaisar, D., Watanabe, K., & Gu, L. (2020) · ACS Synthetic Biology · doi:10.1021/acssynbio.0c00397 · Cited by 37 · see citing works

A rational blueprint for the design of chemically-controlled protein switches

Shui, S., Gaínza, P., Scheller, L., Yang, C., Kurumida, Y., Rosset, S., Georgeon, S., Roberto, R. B. D., Castellanos-Rueda, R., Reddy, S. T., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-25735-9 · Cited by 35 · see citing works

Chemically inducible split protein regulators for mammalian cells

Rihtar, E., Lebar, T., Lainšček, D., Kores, K., Lešnik, S., Bren, U., & Jerala, R. (2022) · Nature Chemical Biology · doi:10.1038/s41589-022-01136-x · Cited by 37 · see citing works

Chemically Induced Proximity in Biological Modulation

Jin, X., Zhou, C., & Zhang, X. (2026) · ACS Bio & Med Chem Au · doi:10.1021/acsbiomedchemau.6c00121

Application of induced proximity for therapeutic discovery

Cacace, A. M., Daniels, D. L., Ferguson, F. M., Mayor‐Ruiz, C., & Woo, C. M. (2024) · Cell chemical biology · doi:10.1016/j.chembiol.2024.05.015 · Cited by 1 · see citing works

Small molecules for genetically encoded control and imaging of protein proximity

Baruah, M., Rasiwala, H. S., Vaidya, U., & Kumar, P. (2026) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2026.102760

Proximity-Based Modalities for Biology and Medicine

Liu, X., & Ciulli, A. (2023) · ACS Central Science · doi:10.1021/acscentsci.3c00395 · Cited by 205 · see citing works

Recent advances in induced proximity modalities

Ng, C. S. C., & Banik, S. M. (2022) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2021.102107 · Cited by 28 · see citing works