Effective drug delivery by PEGylated drug conjugates

Poly(ethylene glycol) chemistry : biotechnical and biomedical applications

1992 • 1,437 citations

Alteration of immunological properties of bovine serum albumin by covalent attachment of polyethylene glycol.

1977 • 1,311 citations

Effect of covalent attachment of polyethylene glycol on immunogenicity and circulating life of bovine liver catalase.

1977 • 1,239 citations

Treatment of Acromegaly with the Growth Hormone–Receptor Antagonist Pegvisomant

2000 • 856 citations

Distribution and Tissue Uptake of Poly(ethylene glycol) with Different Molecular Weights after Intravenous Administration to Mice

1994 • 712 citations

SMANCS and polymer-conjugated macromolecular drugs: advantages in cancer chemotherapy

2001 • 644 citations

Conjugates of anticancer agents and polymers: advantages of macromolecular therapeutics in vivo

1992 • 548 citations

Chemistry of polyethylene glycol conjugates with biologically active molecules

1995 • 536 citations

Blinded, Randomized, Multicenter Study to Evaluate Single Administration Pegfilgrastim Once per Cycle Versus Daily Filgrastim as an Adjunct to Chemotherapy in Patients With High-Risk Stage II or Stage III/IV Breast Cancer

2002 • 504 citations

Early Phase Tumor Accumulation of Macromolecules: A Great Difference in Clearance Rate between Tumor and Normal Tissues

1998 • 451 citations

Effect of molecular weight (M_w) ofN‐(2‐hydroxypropyl)methacrylamide copolymers on body distribution and rate of excretion after subcutaneous, intraperitoneal, and intravenous administration to rats

1987 • 428 citations

The uses and properties of PEG-linked proteins.

1992 • 425 citations

Camptothecin and taxol: discovery to clinic--thirteenth Bruce F. Cain Memorial Award Lecture.

1995 • 364 citations

Attachment of drugs to polyethylene glycols

1983 • 345 citations

A novel connector linkage applicable in prodrug design

1981 • 328 citations

Camptothecin and taxol: Discovery to clinic

1998 • 327 citations

Polymer conjugates with anticancer activity

1995 • 317 citations

Camptothecins: from bench research to hospital wards.

1994 • 314 citations

Soluble Polymer-Supported Organic Synthesis

2000 • 293 citations

The therapeutic value of poly(ethylene glycol)-modified proteins

1991 • 280 citations

Variable Bioavailability of Oral Mercaptopurine

1983 • 268 citations

Relationship of effective molecular size to systemic clearance in rats of recombinant interleukin-2 chemically modified with water-soluble polymers.

1988 • 265 citations

The conjugation of proteins with polyethylene glycol and other polymers

1993 • 264 citations

A Branched Monomethoxypoly(ethylene glycol) for Protein Modification

1995 • 252 citations

Synthesis and evaluation of some water-soluble prodrugs and derivatives of taxol with antitumor activity

1992 • 247 citations

Drug Delivery Systems: Water Soluble Taxol 2‘-Poly(ethylene glycol) Ester ProdrugsDesign and in Vivo Effectiveness

1996 • 221 citations

Synthesis of congeners and prodrugs. 3. Water-soluble prodrugs of taxol with potent antitumor activity

1989 • 219 citations

Direct Evidence for Peptide Transporter (PepT1)-Mediated Uptake of a Nonpeptide Prodrug, Valacyclovir

1998 • 210 citations

SMANCS and polymer-conjugated macromolecular drugs: advantages in cancer chemotherapy

1991 • 209 citations

Blinded, Randomized, Multicenter Study to Evaluate Single Administration Pegfilgrastim Once per Cycle Versus Daily Filgrastim as an Adjunct to Chemotherapy in Patients With High-Risk Stage II or Stage III/IV Breast Cancer

2002 • 206 citations

The synthesis of lignans and neolignans

1982 • 197 citations

Prodrugs

1985 • 194 citations

Structural and Biologic Characterization of Pegylated Recombinant IFN-α2b

2001 • 173 citations

Podophyllotoxin, steganacin and combretastatin: Natural products that bind at the colchicine site of tubulin

1993 • 172 citations

20-O-Acylcamptothecin Derivatives: Evidence for Lactone Stabilization

2000 • 150 citations

Phase I clinical and pharmacokinetic trial of dextran conjugated doxorubicin (AD-70, DOX-OXD)

1993 • 146 citations

Mucoadhesive drug carriers based on complexes of poly(acrylic acid) and PEGylated drugs having hydrolysable PEG–anhydride–drug linkages

2000 • 141 citations

Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs

1993 • 136 citations

Identification of the Major Positional Isomer of Pegylated Interferon Alpha-2b

2000 • 129 citations

The use of synthetic polymers for delivery of therapeutic antisense oligodeoxynucleotides

2002 • 127 citations

Crystalline l-Asparaginase from Escherichia coli B

1970 • 126 citations

Alteration of the circulating life and antigenic properties of bovine adenosine deaminase in mice by attachment of polyethylene glycol.

1981 • 124 citations

Higher Antitumor Efficacy of Daunomycin When Linked to Dextran: In Vivo and In Vitro Studies 2

1978 • 124 citations

Adenosine deaminase deficiency: clinical expression, molecular basis, and therapy.

1998 • 123 citations

Camptothecin delivery systems: enhanced efficacy and tumor accumulation of camptothecin following its conjugation to polyethylene glycol via a glycine linker

1998 • 123 citations

Prolonged Circulating Lives of Single-Chain Fv Proteins Conjugated with Polyethylene Glycol: A Comparison of Conjugation Chemistries and Compounds

1999 • 112 citations

Prodrug Strategies Based on Intramolecular Cyclization Reactions

1997 • 110 citations

Highly Water Soluble Taxol Derivatives: 7-Polyethylene Glycol Carbamates and Carbonates

1995 • 109 citations

Targetable polymeric prodrugs

1987 • 109 citations

The crucial role of spacer groups in macromolecular prodrug design

1996 • 106 citations

Acid-sensitive polyethylene glycol conjugates of doxorubicin: preparation, in vitro efficacy and intracellular distribution

1999 • 104 citations

Co-operative Effects of Functional Groups in Peptides. I. Aspartyl-serine Derivatives

1962 • 104 citations

Camptothecin-20-PEG ester transport forms: the effect of spacer groups on antitumor activity

1998 • 104 citations

Drug Delivery Systems Employing 1,4- or 1,6-Elimination: Poly(ethylene glycol) Prodrugs of Amine-Containing Compounds

1999 • 103 citations

Prodrugs of anticancer agents

1996 • 102 citations

Drug Delivery Systems Based on Trimethyl Lock Lactonization: Poly(ethylene glycol) Prodrugs of Amino-Containing Compounds

2000 • 101 citations

Cyclization-activated prodrugs. Basic carbamates of 4-hydroxyanisole

1990 • 100 citations

Cellular uptake mechanism of amino acid ester prodrugs in Caco-2/hPEPT1 cells overexpressing a human peptide transporter.

1998 • 96 citations

Colloid osmotic properties of modified hemoglobins: chemically cross-linked versus polyethylene glycol surface-conjugated

1997 • 93 citations

Drug Delivery Systems. 2. Camptothecin 20-O-Poly(ethylene glycol) Ester Transport Forms

1996 • 92 citations

The Chemistry and Pharmacology of Taxol® and its Derivatives

1995 • 87 citations

The double prodrug concept and its applications

1989 • 86 citations

The use of polyethylene glycol-modified interleukin-2 (PEG-IL-2) in the treatment of patients with metastatic renal cell carcinoma and melanoma

1995 • 86 citations

Anticancer drug delivery systems: multi-loaded N4-acyl poly(ethylene glycol) prodrugs of ara-C.II. Efficacy in ascites and solid tumors

2002 • 76 citations

Chemoenzymatic Synthesis of N-Ras Lipopeptides

1998 • 76 citations

The Design of Selectively-activated Anti-cancer Prodrugs for use in Antibody-directed and Gene-directed Enzyme-Prodrug Therapies

1998 • 74 citations

Highly water soluble taxol derivatives: 2′-polyethyleneglycol esters as potential prodrugs

1994 • 72 citations

N4-Behenoyl-1-beta-D-arabinofuranosylcytosine as a potential new antitumor agent.

1977 • 72 citations

Modified Taxols, 6. Preparation of Water-Soluble Prodrugs of Taxol

1991 • 70 citations

Synthesis and properties of oligodeoxyribonucleotide—polyethylene glycol conjugates

1994 • 69 citations

Camptothecin delivery systems: the utility of amino acid spacers for the conjugation of camptothecin with polyethylene glycol to create prodrugs.

1999 • 68 citations

Synthesis and Characterization of High-Molecular Mass Polyethylene Glycol-Conjugated Oligonucleotides

1997 • 65 citations

Efficient Clearance of Poly(ethylene glycol)-Modified Immunoenzyme with Anti-PEG Monoclonal Antibody for Prodrug Cancer Therapy

2000 • 65 citations

Drug Delivery Systems Employing 1,6-Elimination: Releasable Poly(ethylene glycol) Conjugates of Proteins

2001 • 63 citations

Functionalized Semitelechelic Poly[N-(2-hydroxypropyl)methacrylamide] for Protein Modification

1998 • 61 citations

Review: Poly(Ethylene Glycol)s with Reactive Endgroups. II. Practical Consideration for the Preparation of Protein-PEG Conjugates

1996 • 59 citations

Prodrug Approaches to the Improved Delivery of Peptide Drugs

1999 • 59 citations

Poly(ethylene glycol)–human serum albumin–paclitaxel conjugates: preparation, characterization and pharmacokinetics

2001 • 57 citations

Site-specific modification of enzymatically synthesized RNA: Transcription initiation and Diels-Alder reaction

1997 • 55 citations

Modulating pharmacokinetics of an anti-interleukin-8 F(ab′)2 by amine-specific PEGylation with preserved bioactivity

2000 • 54 citations

Antitumor activity of paclitaxel-2'-glycinate conjugated to poly(ethylene glycol): a water-soluble prodrug.

1998 • 53 citations

Tumor accumulation of poly(ethylene glycol) with different molecular weights after intravenous injection

1997 • 50 citations

Polyethylene Glycol–Derivatized Cysteine-Substitution Variants of Recombinant Staphylokinase for Single-Bolus Treatment of Acute Myocardial Infarction

2000 • 49 citations

Antigene Effect in K562 Cells of a PEG-Conjugated Triplex-Forming Oligonucleotide Targeted to the bcr/abl Oncogene

2001 • 49 citations

Enhanced tumor cell selectivity of adriamycin-monoclonal antibody conjugate via a poly(ethylene glycol)-based cleavable linker

2002 • 49 citations

Anti‐tumor activity of daunorubicin linked to poly‐<scp>L</scp>‐aspartic acid

1982 • 46 citations

Carboxyalkylated histidine is a pH-dependent product of pegylation with SC-PEG.

2001 • 45 citations

Camptothecin delivery systems: the antitumor activity of a camptothecin-20-0-polyethylene glycol ester transport form.

1997 • 45 citations

Pharmacodynamic and pharmacokinetic characterization of poly(ethylene glycol) conjugation to met-enkephalin analog [D-Pen2, D-Pen5]-enkephalin (DPDPE).

2001 • 43 citations

PEG Thiazolidine-2-thione, a Novel Reagent for Facile Protein Modification: Conjugation of Bovine Hemoglobin

1996 • 40 citations

Automated incorporation of polyethylene glycol into synthetic oligonucleotides

1993 • 39 citations

Synthesis, in vitro kinetics and in vivo studies on protein conjugates of AZT: Evaluation as a transport system to increase brain delivery

1993 • 38 citations

Filgrastim (r-metHuG-CSF) in the 21st Century: SD/01

2001 • 38 citations

Synthesis of totally chiral, multiple armed, poly Glu and poly Asp scaffoldings on bifunctional adamantane core

1997 • 37 citations

Pharmacodynamic and Safety Results of PEG-Hirudin in Healthy Volunteers

1997 • 37 citations

Drug delivery of anticancer agents: water soluble 4-poly (ethylene glycol) derivatives of the lignan, podophyllotoxin

1999 • 36 citations

Synthesis of a novel duocarmycin derivative DU-257 and its application to immunoconjugate using poly(ethylene glycol)-dipeptidyl linker capable of tumor specific activation

2000 • 34 citations

Polyethylene glycol induces apoptosis in HT‐29 cells: potential mechanism for chemoprevention of colon cancer

2001 • 34 citations

Anticancer drug delivery systems: N4-acyl poly(ethyleneglycol) prodrugs of ara-CI. Efficacy in solid tumors

2002 • 32 citations

Enhanced antitumor potency of polyethylene glycolylated tumor necrosis factor-alpha: a novel polymer-conjugation technique with a reversible amino-protective reagent.

1999 • 32 citations

Design of Intramolecularly Activated Prodrugs

1998 • 32 citations

Preparation of Long-Acting Superoxide Dismutase Using High Molecular Weight Polyethylene Glycol (41,000-72,000 Daltons)

1991 • 32 citations

The Pharmacology of Prodrugs of 5-Fluorouracil and 1-β-D-Arabinofuranosylcytosine

1984 • 31 citations

Peginterferon alfa-2a (40 kDa) monotherapy: a novel agent for chronic hepatitis C therapy

2001 • 31 citations

Stability, Specific Binding Activity, and Plasma Concentration in Mice of an Oligodeoxynucleotide Modified at 5'-Terminal with Poly (ethylene glycol).

1995 • 31 citations

N-(Acyloxyalkoxycarbonyl) derivatives as potential prodrugs of amines. I. kinetics and mechanism of degradation in aqueous solutions

1987 • 31 citations

Paclitaxel and water-soluble poly (L-glutamic acid)-paclitaxel, induce direct chromosomal abnormalities and cell death in a murine metastatic melanoma cell line.

1998 • 28 citations

Pharmacokinetic Disposition of Polyethylene Glycol-Modified Salmon Calcitonins in Rats.

2000 • 28 citations

Synthesis and characterisation of a new amphotericin b–methoxypoly(ethylene glycol) conjugate

2001 • 28 citations

Inhibition of tumor growth by poly(ethylene glycol) derivatives of anti-ErbB2 antibodies

2000 • 27 citations

Antitumor Agents LXII: Synthesis and Biological Evaluation of Podophyllotoxin Esters and Related Derivatives

1983 • 24 citations

Intramolecular nucleophilic aminolysis of aliphatic esters. Cyclization of methyl 2-aminomethylbenzoate to phthalimidine

1976 • 24 citations

Response of Patients with Advanced Neoplasms to the Intravenous Administration of &lt;italic&gt;Alpha&lt;/italic&gt;-Peltatin&lt;xref ref-type="fn" rid="fn1"&gt;2&lt;/xref&gt;

1954 • 20 citations

3 Paclitaxel (taxol®) formulation and prodrugs

1995 • 20 citations

The Biological Effects of Some Podophyllin Compounds and Their Dependence on Chemical Structure. II

1959 • 20 citations

Branched poly(ethylene glycol) linkers

1997 • 19 citations

Amino Acids and Peptides

1997 • 18 citations

Branched Polyethylene Glycol (Bpeg) Conjugated Antisense Oligonucleotides

1998 • 18 citations

Novel oral fluoropyrimidines in the treatment of metastatic colorectal cancer

1999 • 14 citations

Synthesis and investigation of N4-substituted cytarabine derivatives as prodrugs.

1995 • 11 citations

Oligonucleotide Conjugated to Linear and Branched High Molecular Weight Polyethylene Glycol as Substrates for RNase H

1999 • 9 citations

ChemInform Abstract: THE 1,4 AND 1,6 ELIMINATIONS FROM HYDROXY‐ AND AMINO‐SUBSTITUTED BENZYL SYSTEMS: CHEMICAL AND BIOCHEMICAL APPLICATIONS

1983 • 7 citations

The Biological Effects of Some Podophyllin Compounds and Their Dependence on Chemical Structure

1957 • 5 citations

Deleted Work

1955 • 0 citations