gebhart/patrepeval huggingface dataset:
Inhibition of phospholipase A2; a molecular recognition study (1988)

A model of the enzyme PLA2 with a phospholipid substrate bound in the active site was derived using molecular graphics and molecular mechanics modelling techniques, and its ability to account for competitive inhibition tested by modelling the analogous complex of the enzyme and a known inhibitor; the model was then applied to the study of the binding of a new inhibitor, 3-arachidonyl-4(O-phosphoethanolamino)-methyltetrahydrofuran-2-one and the absolute stereochemistry for active site binding of this inhibitor predicted to be (3S,4R).
Cyclic β-Peptoids (2008)

The first synthesis of functionalized beta-peptoid macrocycles is reported. X-ray crystallographic structure of tetramer 9 reveals a C2-symmetrical derivative with unexpected all-cis-amide bonds and spatial disposition of the appendages toward the two opposite faces of the ring. Quantum calculations suggest that 9 is locked in this layout. These macrocycles constitute novel promising templates for multimeric ligation of biologically active ligands. The concept was exemplified by chemical decoration of tetramer 9 via "click" reactions.
SLA 3-D Printed Arrays of Miniaturized, Internally Fed, Polymer Electrospray Emitters (2015)

This paper reports the design, fabrication, and characterization of arrays of miniaturized, internally fed, polymer electrospray emitters fabricated with stereolithography. The freeform additive manufacturing process used to make the devices has associated two orders of magnitude reduction in the fabrication cost per device and fabrication time (from thousands of dollars to tens of dollars, and from months to hours, respectively) and a two orders of magnitude reduction in the cost of the manufacturing infrastructure (from millions of dollars to tens of thousands of dollars) compared with a silicon MEMS multiplexed electrospray source. The 3-D printed devices include features not easily attainable with other microfabrication methods, e.g., tapered channels and threaded holes. Through the optimization of the fabrication process 10-mm tall, isolated, straight, solid columns with diameter as small as 300 μm, and 12-mm long, straight tubes with inner diameter as small as 400 μm and wall thickness as small as 150 μm were demonstrated. Arrays with as many as 236 internally fed electrospray emitters (236 emitters in 1 cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> ) were made, i.e., a twofold increase in emitter density and a sixfold increase in array size compared with the best reported values from multiplexed, internally fed, electrospray sources made of polymer. The characterization of devices with a different array size suggests a uniform emitter operation.
Exosome-Mediated Benefits of Cell Therapy in Mouse and Human Models of Duchenne Muscular Dystrophy (2018)

Genetic deficiency of dystrophin leads to disability and premature death in Duchenne muscular dystrophy (DMD), affecting the heart as well as skeletal muscle. Here, we report that clinical-stage cardiac progenitor cells, known as cardiosphere-derived cells (CDCs), improve cardiac and skeletal myopathy in the mdx mouse model of DMD. Injection of CDCs into the hearts of mdx mice augments cardiac function, ambulatory capacity, and survival. Exosomes secreted by human CDCs reproduce the benefits of CDCs in mdx mice and in human induced pluripotent stem cell-derived Duchenne cardiomyocytes. Surprisingly, CDCs and their exosomes also transiently restored partial expression of full-length dystrophin in mdx mice. The findings further motivate the testing of CDCs in Duchenne patients, while identifying exosomes as next-generation therapeutic candidates.
Wavelength multiplexing components - A review of single-mode devices and their applications (1984)

State-of-the-art and systems applications of single-mode wavelength-division multiplexing (WDM) devices are described. The performance characteristics required differ depending on whether the method of operation is one-way or two-way. Development trends and problems of the new technology are discussed.
스칸디나비아 모델과 한국 노사관계 (2005)

본 연구는 스웨덴 노사관계에 대한 연구가 한국에서 어떤 내용과 수준으로 이루어지고 있고, 그것이 한국 노사관계에 미친 영향에 대해 논의할 것이다. 스웨덴 노사관계의 분석대상으로는 스웨덴 모델, 단체교섭, 경영 참가, 작업장 사례, 임노동자기금, 노동교육체계 등을 검토하고자 한다.
스칸디나비아모델에 대한 연구가 사회과학의 다양한 분과에서 이루어지고 있고 북유럽에 대한 일반적 관심도 높아지고 있다. 스칸디나비아모델 이 위에서 말한 사회민주주의, 단체교섭, 경영참가, 임금노동자기금, 노동 교육 영역에서 한국 노사관계에 커다란 시사점을 주는 것은 사실이다.
하지만 기본적으로 스칸디나비아국가들이 한국과는 매우 다른 역사적 전통과 문화, 노사관계체제를 지니고 있기 때문에, 스칸디나비아모델을 직접 한국 현실에 적용할 수 있는지에 대한 논쟁은 여전히 남아 있다. 어떤 학자는 스칸디나비아와 한국은 전혀 다른 사회체제이기 때문에 한국 노사 관계가 스칸디나비아모델처럼 될 수는 없다고 단정하는가 하면, 다른 학자는 한국도 노사관계의 합법칙성에 따라 스칸디나비아모델처럼 사회합의적 노사관계로 발전해갈 것이라고 주장한다.
이 점에 대해서 아직은 어떤 평가가 맞는다고 할 수 없지만, 한국 사람들이 선호하는 사회체제 또는 노사관계체제는 사회민주주의 또는 사회합의적 노사관계라는 점에는 많은 연구자들이 동의할 수 있을 것이다. 지난 해에 노동조합 간부를 대상으로 조사한 설문결과에 의하면 지향하는 사회 경제체제로 가장 높은 비중을 차지한 것이 ‘유럽식 사회민주주의’로 60.2%의 노조간부가 선택하였다. 최근 노사간의 논쟁 과정에서도 노사신뢰와 노사합의가 가장 중요한 과제로 손꼽히는 것도 동일한 맥락에서 이 해할 수 있을 것이다.
우선 스웨덴 모델이 기존 사회주의체제에 대해 일정한 수준의 대안적 체제를 구성하고 있다는 점에 많이 이들이 동의하고 있다. 한국도 스웨덴과 동일한 수준의 사회민주주의는 아니라 할지라도 ‘사회복지 확대’와 ‘공공성 확보’ 및 ‘경제민주주의의 확대’ 등 민주주의적 주장은 보편적으로 주장되고 있는 것이다. ‘민주적 시장경제’ 또는 ‘민주복지국가’ 등 용어는 다르게 표현될지라도 전반적으로 사회민주주의라는 틀 속에서 한국사회의 미래체제를 구상하고 있는 것이다.
구체적으로 노사관계로 넘어가서 스칸디나비 아모델이 한국 노사관계에 미친 영향과 시사점을 살펴보자. 세계에서도 드물게 발전한 중앙교섭 및 산별교섭은 한국의 단체교섭 발전과정에도 그대로 적용되고 있다. 보건의 료노조와 금속노조, 금융노조가 이미 산업별노조가 조직적으로 전환하여 산업별 교섭을 하고 있는 상황에 있으며 이외에도 화학노조, 사무노조, 공무원노조 등도 산업별노조를 건설할 계획을 갖고 있다.
산업별교섭 뿐만 아니라 노조조직 상의 역할 설정에 있어서 노조중앙과 작업장분회의 활동이 모두 활발한 스웨덴의 모습은 한국의 노조조직에도 산업별 노조로 가는 과정에서 기업 또는 작업장차원 노조의 역할이 적절 하게 자리잡는 데 중요한 참고자료가 되고 있다. 특히 기업별노조의 전통이 강한 한국에서 산별노조로 간다고 하더라도 기업노조의 역할이 완전히 사라질 수는 없고 산별 중앙협약에 대한 보충협약 체결권을 갖는다거나 기업차원 노조 일상활동을 어느 정도 유지할 수밖에 없기 때문이다.
노동조합의 경영참가에서도 스웨덴 등 북유럽모델의 영향을 받아 민주 노총과 한국노총은 노조의 경영참가법 제정을 정부에 요구를 한 바 있으며, 노조대표의 이사회 참가에 대해서도 사회적인 여론화가 되어 있는 상황이다. 대부분의 노조는 단체교섭에서 경영참가 및 노조대표의 이사회 참가를 명시적으로 요구하고 있다. 노조뿐만 아니라 시민사회단체에서도 기업이사회에 참여할 수 있는 사외이사제에 대한 논의가 활발하게 진행되고 있다.
경제민주주의 영역에서는 스웨덴 같은 임노동자기금 형태는 아니지만 기업이익 중의 일부를 노동조합이 집단적으로 소유운영하는 기금을 만들어 저임금노동자나 비정규노동자의 노동조건 향상을 위한 수단으로 활용 하자는 논의도 적극적으로 제기되고 있으며 국민연금 같은 기구의 이사회 에 노동조합 대표가 이사로 참가하는 방안을 개진하고 있기도 하다. 또한 일반적으로 나타나고 있는 종업원지주제나 이익배분제에 대한 논의도 활발해지고 있다. 이론적으로는 주주자본주의냐 이해당사자 자본주의냐라는 논쟁도 일어나고 있다.
노동교육에서는 스칸디나비아국가들처럼 체계적이고 폭넓게 발전하지는 못했지만, 스터디써클 방식이나 단계별 노동교육을 도입하고 있는 상황이며 노총 차원이나 연맹차원에서 노동대학 또는 노동대학원 등의 프로그램을 개발하여 진행하고 있는 상황이다. 정부기구인 노동교육원에서도 노조 교육을 위한 시설과 재정을 마련하여 노동자교육을 지원하는 사업을 대폭 확대하고 있다.
전체적으로 보면, 스칸디나비아모델 연구가 한국 노사관계에 직접ㆍ간접으로 여러 영향을 미치고 있다고 할 수 있지만 그 영향력이 어느 정도 인지 평가하기는 어렵다. 어떤 경우엔 영미형 노사관계요소가 도입되는 것처럼 보일 때도 있고 어떤 경우엔 유럽형 노사관계 요소가 도입되는 경우도 있기 때문이다. 장기적으로 한국 노사관계가 어떤 모습으로 귀결될 지는 모르지만 스칸디나비아 노사관계 연구가 한국의 이론적ㆍ현실적 발전에 풍부한 도움을 줄 것이다.
Tailored Glycopolymers:  Controlling the Carbohydrate−Protein Interaction Based on Template Effect (2000)

ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTTailored Glycopolymers: Controlling the Carbohydrate−Protein Interaction Based on Template EffectNoriko Nagahori and Shin-Ichiro NishimuraView Author Information Laboratory for Bio-Macromolecular Chemistry, Division of Biological Sciences, Graduate School of Science, Hokkaido University, Sapporo 060-0810, Japan Cite this: Biomacromolecules 2001, 2, 1, 22–24Publication Date (Web):December 28, 2000Publication History Received16 May 2000Revised2 November 2000Published online28 December 2000Published inissue 1 March 2001https://pubs.acs.org/doi/10.1021/bm0000438https://doi.org/10.1021/bm0000438rapid-communicationACS PublicationsCopyright © 2001 American Chemical SocietyRequest reuse permissionsArticle Views945Altmetric-Citations44LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information SUBJECTS:Carbohydrates,Chemical specificity,Genetics,Peptides and proteins,Polymers Get e-Alerts
Directionally Aligned Helical Peptides on Surfaces (1993)

Directionally oriented peptide layers 1000 angstroms thick were constructed by polymerization on gold and indium-tin-oxide glass. A key feature is the use of an appropriately functionalized surface on which the initiation sites for polymerization are spaced at distances consistent with the helical diameter of the peptide. Completely helical polyalanine and polyphenylalanine layers have been constructed. The helicity of the polyalanine layer was completely retained after heating at 180 degrees C for 7 days.
High frequency of leukemic clones in newborn screening blood samples of children with B-precursor acute lymphoblastic leukemia (2002)

The detection of leukemia cells on newborn genetic screening cards ("Guthrie cards") of a small group of patients and several sets of identical twins developing acute lymphoblastic leukemia (ALL) with identical phenotypic and chromosomal markers has provided evidence that childhood ALL cases may arise in utero. We conducted a retrospective study of a randomly selected group of childhood B-precursor ALL patients to determine the frequency of the presence of "leukemic" clones prenatally in ALL cases by testing newborn screening cards. The 17 ALL patients analyzed had a median age of 46 months (range, 18 months to 13 years) and had median presenting white blood cell (WBC) counts of 10 950/microL (range, 2900-70 300/microL) at diagnosis. A clonal rearrangement of the immunoglobulin heavy chain (IgH) gene was identified in diagnostic lymphoblasts and sequenced and patient-specific primers were used to amplify DNA from blood samples on the patient's newborn screening cards. Twelve of the 17 (71%) analyzed newborn cards had detectable IgH rearrangements amplified by seminested polymerase chain reaction. DNA sequencing confirmed that the IgH rearrangements detected matched the IgH sequences identified from diagnostic leukemia cells, indicating the presence of a "leukemic" clone at birth. There were no differences in age or presenting WBC counts between the cases with or without positive newborn screening cards. All 6 patients with hyperdiploid ALL had detectable "leukemic" clones on their cards. The results of our study support the notion that a high proportion of childhood B-precursor ALL cases arise in utero, although postnatal events are also important factors in leukemogenesis.
Worldwide haplotype diversity and coding sequence variation at human bitter taste receptor loci (2005)

Bitter taste perception in humans is mediated by receptors encoded by 25 genes that together comprise the TAS2R (or T2R) gene family. The ability to identify the ligand(s) for each of these receptors is dependent on understanding allelic variation in TAS2R genes, which may have a significant effect on ligand recognition. To investigate the extent of coding variation among TAS2R alleles, we performed a comprehensive evaluation of sequence and haplotype variation in the human bitter taste receptor gene repertoire. We found that these genes exhibit substantial coding sequence diversity. In a worldwide population sample of 55 individuals, we found an average of 4.2 variant amino acid positions per gene. In aggregate, the 24 genes analyzed here, along with the phenylthiocarbamide (PTC) receptor gene analyzed previously, specify 151 different protein coding haplotypes. Analyses of the ratio of synonymous and nonsynonymous nucleotide substitutions using the Ka/Ks ratio revealed an excess of amino acid substitutions relative to most other genes examined to date (Ka/Ks = 0.94). In addition, comparisons with more than 1,500 other genes revealed that levels of diversity in the TAS2R genes were significantly greater than expected (pi = 0.11%; p < 0.01), as were levels of differentiation among continental populations (FST = 0.22; p < 0.05). These diversity patterns indicate that unusually high levels of allelic variation are found within TAS2R loci and that human populations differ appreciably with respect to TAS2R allele frequencies. Diversity in the TAS2R genes may be accounted for by natural selection, which may have favored alleles responsive to toxic, bitter compounds found in plants. These findings are consistent with the view that different alleles of the TAS2R genes encode receptors that recognize different ligands, and suggest that the haplotypes we have identified will be important in studies of receptor-ligand recognition.
Thermally Reversible HydrogelsSwelling Characteristics and Activities of Copoly(N-isopropylacrylamide-acrylamide) Gels Containing Immobilized Asparaginase (1987)

Hydrogels synthesized from polymers and copolymers of N-isopropyl acrylamide (NIPAAm) shrink or swell as the temperature is raised or lowered through their lower critical solution temperature (LCST). We show here that when an enzyme is immobilized within such gels it may be "switched" on and off reversibly as the temperature is cycled. Such catalytic hydrogels may be used to control reactions by a thermal feedback mechanism.
Papel de los receptores opioides tipo kappa en la regulación de la homeostasis energética por la nicotina (2020)

La ganancia de masa corporal es el principal factor que interfiere con dejar de fumar. La nicotina, el compuesto bioactivo mas importante del tabaco, ha demostrado tener un gran impacto tanto en el gasto energetico como en la ingesta, actuando a nivel central. Entre las acciones centrales de la nicotina sobre la masa corporal, la mayoria de los estudios se han centrado sobre la termogenesis del tejido adiposo pardo (BAT, brown adipose tissue), mientras que su posible efecto termogenico sobre el tejido adiposo blanco (WAT, white adipose tissue) permanecia sin esclarecer. Aqui mostramos que la nicotina actua a nivel central induciendo browning en el WAT y que este efecto depende del receptor κ opioide (KOR), especificamente en el area lateral hipotalamica (LHA). Datos previos demuestran que pacientes fumadores presentan una mayor expresion de la proteina desacoplante 1 (uncopled protein 1, UCP1) en el WAT, y esto es consistente con nuestros resultados. Estos datos demuestran que la accion central de la nicotina sobre el browning en el WAT podrian ser una diana contra la obesidad en humanos.
Profiling of Acarviostatin Family Secondary Metabolites Secreted by Streptomyces coelicoflavus ZG0656 Using Ultraperformance Liquid Chromatography Coupled with Electrospray Ionization Mass Spectrometry (2008)

Profiling of acarviostatin family secondary metabolites secreted by Streptomyces coelicoflavus ZG0656 was performed by means of a rapid and facile procedure using ultraperformance liquid chromatography coupled with electrospray ionization mass spectrometry (UPLC/ESI-MS). The acarviostatins were separated on a C18 UPLC column with a series of acetonitrile-aqueous ammonia gradients. The target homologues were detected using the multiple reaction monitoring mode, and the chemical structures were confirmed by analyzing the diagnostic fragment ions in their MS/MS spectra. All six known reference acarviostatins (I03, II03, II13, II23, III03, IV03) were thus identified. In addition, at least 74 acarviostatin homologues, including 65 novel compounds, were characterized. Some of the features of the novel structures included having up to five acarviosine moieties, an acarviosine moiety at the reducing terminus, or an incomplete acarviosine moiety at the nonreducing terminus. This type of investigation may be useful for researchers who study secondary metabolomics in microorganisms and plants, especially those who perform metabolic profiling of aminooligosaccharides and other natural products with similar structures.
Syntheses of N‐substituted carbazoles involving polymerizable terminal vinyl groups (1979)

Abstract Eleven N ‐substituted carbazoles (CZ) with terminal vinyl groups were synthesized by five sequences of reaction: N ‐( p ‐vinylbenzyl)‐ and N ‐β‐(vinyloxyethyl)CZ by N ‐alkylations of potassium CZ with corresponding chlorides; N ‐(β‐acryloyloxyethyl)CZ by the esterification of N ‐(β‐hydroxyethyl)CZ with acryloyl chloride; N ‐acrylamido‐or methacryl‐amido‐methyl CZ from N ‐hydroxymethyl CZ and acryl‐ or methacrylamide; N ‐(3‐acryloyl‐ or methacryloyl‐oxy‐2‐hydroxypropyl)CZ and N ‐[3‐( p ‐ or m ‐vinylanilino)‐2‐hydroxypropyl] CZ from N ‐(2,3‐epoxypropyl)CZ and acrylic or methacrylic acid and p ‐ or m ‐vinylaniline, respectively; and 2‐[β‐( N ‐carbazyl)propionyloxy]ethyl acrylate or methacrylate by the Michael addition of CZ to 2‐hydroxyethyl acrylate or methacrylate, followed by esterifications. The vinyl polymers with pendant carbazyl groups more or less distant from the polymer backbones, prepared by conventional radical or cationic polymerization procedures, indicated charge‐transfer spectra with 2,4,7‐trinitrofluorenone (TNF) in tetrahydrofuran (THF) solutions that are spread over most of the visible range.
Nanodiscs Allow Phage Display Selection for Ligands to Non-Linear Epitopes on Membrane Proteins (2013)

In this work, we exploited a method that uses polytopic membrane proteins as targets for phage display selections. Membrane proteins represent the largest class of drug targets and drug discovery is mostly based on the identification of ligands binding to target molecules. The screening of a phage display library for ligands against membrane proteins is typically hindered by the requirement of these proteins for a membrane environment, which is necessary to retain correct folding and epitope formation. Especially in proteins with multiple transmembrane domains, epitopes often are non-linear and consist of a combination of loops between transmembrane stretches of the proteins. Here, we have used bacteriorhodopsin (bR) as a model of polytopic membrane protein, assembled into nanoscale phospholipid bilayers, so called nanodiscs, to screen a phage display library for potential ligands. Nanodiscs provide a native-like environment to membrane proteins and thus selection of ligands can take place in a near physiological state. Screening a 12-mer phage display peptide library against bR nanodiscs led to the isolation of phage clones binding specifically to bR. We were further able to identify the binding site of selected phage clones proving that the clones bind to extramembranous, non-linear epitopes of bR. Thus, nanodiscs provide a suitable and general tool that allows screening of a phage display library against membrane proteins in a near native environment.
Pharmacokinetics of cysteamine bitartrate following gastrointestinal infusion (2006)

The pharmacokinetic data generated help extend our understanding of cysteamine.
Ultrasensitive Coincidence Fluorescence Detection of Single DNA Molecules (2003)

We have detected individual DNA molecules labeled with two different fluorophores in solution by using two-color excitation and detection of coincidence fluorescence bursts. The confocal volumes of the two excitation lasers were carefully matched so that the volume overlap was 30% of the total confocal volume illuminated. This method greatly reduces the level of background fluorescence and, hence, extends the sensitivity of single molecule detection down to 50 fM. At these concentrations, the dual-labeled DNA is detectable in the presence of a 1000-fold excess of single-fluorophore-labeled DNA. We demonstrate that we can detect 100 fM dual-labeled DNA diluted in 1 microM unlabeled DNA, which was not possible with single color detection. This method can be used to detect rare molecules in complex mixtures.
Gene transfer to cervical cancer with fiber‐modified adenoviruses (2004)

Successful adenoviral (Ad) vector-mediated strategies for cancer gene therapy mandate gene-delivery systems that are capable of achieving efficient gene delivery in vivo. In many cancer types, in vivo gene-transfer efficiency remains limited due to the low or highly variable expression of the primary Ad receptor, the coxsackie Ad receptor (CAR). In this study, we evaluated the expression of CAR on cervical cancer cells as well as CAR-independent targeting strategies to integrins (Ad5.RGD), heparan sulfate proteoglycans (Ad5.pK7) or both (Ad5.RGD.pK7). We used a panel of established cervical cancer cell lines and primary cervical cancer cells isolated from patients to quantify the expression of CAR mRNA and to evaluate the gene-transfer efficiency of fiber-modified Ads. Of the fiber-modified vectors, Ad5.pK7 and Ad5.RGD.pK7 displayed significantly enhanced gene-transfer efficiency in vitro. Gene-delivery efficiency in vivo was evaluated using an s.c. cervical cancer mouse model. Ad5.RGD.pK7 significantly improves tumor targeting in vivo, resulting in a significantly improved tumor/liver ratio in mice. Our results suggest that the double-modified Ad5.RGD.pk7 vector enhances gene transfer to clinically relevant cervical cancer substrates, while the infectivity of nontarget cells in the mouse is not increased and comparable to Ad5. The fiber-modified virus described here can help achieve higher clinical efficacy of cervical cancer gene therapy.
Pharmacokinetic (PK) characterization of irinotecan liposome injection in patients (pts) with metastatic breast cancer (mBC). (2019)

e12003 Background: Irinotecan liposome injection (nal-IRI) uses intraliposomal stabilisation technology to enable high drug load and in-vivo stability. This analysis characterizes the PK profile of nal-IRI in pts with mBC. Methods: The expansion of NCT01770353 enrolled 30 pts with mBC over three cohorts (Cohort 1: ER+ and/or PR+ BC [C-1]; Cohort 2: Triple Negative BC [C-2]; and Cohort 3: BC with active Brain Metastasis [C-3]). Key inclusion criteria: ECOG ≤1; adequate organ function; and &gt;1 and ≤5 prior lines of cytotoxic therapy in metastatic setting. Most pts received nal-IRI 60 mg/m 2 salt-based equivalent (50 mg/m 2 free base equivalent [FBE]) or 80 mg/m 2 (70 mg/m 2 FBE) q2w by iv infusion, based on tolerance; 2 pts were treated at 40 mg/m 2 (35 mg/m 2 FBE). Plasma samples were collected over 360h across cycles 1, 2 &amp;3, and analysed using LC-MS/MS for total irinotecan. Data were analysed by a non-compartmental approach using Phoenix Winnonlin, and were compared with values from studies in other tumor types. Results: 21 patients were evaluable for PK analysis (C-1, n=6; C-2, n=7; and C-3, n=8). No trend for accumulation was observed in cycle 2 or 3, when comparing total irinotecan C max &amp; exposure (area under the curve at 168 h [AUC 168 ]) versus cycle 1. At 40-80 mg/m 2 (35-70 mg/m 2 FBE), C max of irinotecan tended to increase proportionally with total dose, and was comparable to studies in other tumour types (see Table). Among 29 pts who received nal-IRI, partial response (per RECIST) was observed in 10 pts. The most related TEAEs (≥ 25%) were diarrhea, nausea, vomiting, hypokalaemia, decreased appetite and fatigue. Stable disease was observed in 5 pts. Conclusions: PK parameters in patients with mBC were comparable to historical studies in patients with other tumour types. The safety profile of nal-IRI monotherapy appeared consistent with gastrointestinal and blood disorders. [Table: see text]