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Project Development

Location:
San Mateo, California, 94404, United States
Posted:
May 28, 2010

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QING JANE LU, Ph.D.

650-***-**** (Home), 650-***-**** (Cell), Foster City, CA

abmqvr@r.postjobfree.com

Medicinal/Synthetic Organic Chemist

. Extensive pharmaceutical industry experience in small molecule drug

discovery/development including hit identification, lead optimization,

structure-based drug design, SAR analysis, ADME, PK/PD, toxicology and

IP; generated clinical and development candidates for treating

inflammation, cardio arrhythmia or antibacterial agents

. Experienced managing CRO collaborations based in US and Asia including

design targets, propose synthetic schemes, solve chemistry issues and

organize weekly teleconference to accelerate the productivity,

coordinate internal and external chemistry work

. Hands-on experience in design, execution and troubleshooting of multi-

step syntheses of natural products and heterocycles, as well as

synthetic methodology development

. Extensive experience in modern purification and characterization

methodologies, skilled in HPLC, LCMS, GILSON and ISCO systems, and

interpretation of various spectra 1D/2D NMR, MS.

. Strong computer skills with experience in MS office (Word, Excel,

Powerpoint), Chem-Draw/ISIS-Draw, Chem Office, SciFinder, Crossfire

PROFESSIONAL EXPERIENCE

Achaogen Inc. South San Francisco Medicinal Chemistry

Consultant Antibacterial Project (LpxC Inhibitors):

2010

. Assisted in transfer of project from research into development;

managed CRO and CMO collaborations in China, monitored the scale-up

work, addressed chemistry issues, handled contracts and negotiated

prices with CRO and CMO companies; coordinated production schedules

to meet the study timelines

Senior Scientist Antibacterial Project (LpxC Inhibitors):

2006-2009

. Responsible for chemistry aspects as a lead chemist in the core

project team; designed and synthesized new inhibitors; performed SAR

analysis and selected compounds for biological studies; produced

potential development candidates with big improvement in animal

efficacy, responsible for analyzing existing IP and writing patent

applications with legal support

. Managed CRO collaborations in US and Asia (up to 18 FTE): design

targets, propose synthetic schemes, solve chemistry issue and organize

weekly teleconference; coordinated the internal and external chemistry

work, supervised one senior RA internally

Scios, Inc. (a J&J company) Fremont, CA Medicinal Chemistry

1999-2006

Senior Scientist II Oct. 2005

Senior Scientist Sept. 2000

Scientist May. 1999

CaM Kinase II Project:

. Started from primary high throughput screens and hit identification,

designed and synthesized CaMKII inhibitors for treating cardio

arrhythmia; addressed issues of potency, cell activity, selectivity,

stability, PK and hERG profiles; developed two first-in-class

scaffolds with good potency in rabbit arrhythmia model

. DMPK coordinator, responsible for ADME/PK screening decisions and SAR

analysis, initiated whole blood PK studies, re-evaluated CYP assay for

optimizing ADME profile

. Worked with CRO companies in Asia monitoring chemistry progress and

solving chemistry issues and coordinating the internal and external

chemistry work to deliver on time; supervised two direct reports (one

MS and one Ph.D)

p38? Kinase Project:

. Proposed and synthesized p38? kinase inhibitors; optimized potency,

selectivity, solubility and DMPK profiles; key contributor in

generating two clinical compounds SCIO-469 (phase 2b) and SCIO-323

(phase 1) for treating rheumatoid arthritis and cancer

. Successfully produced preclinical candidate SCIO-087 with improved

solubility and PK profile as a back up scaffold, designed and

implemented synthetic route suitable for scale-up

Shaman Pharmaceuticals, S. San Francisco, CA Medicinal Chemistry

1996-1998

Scientist Diabetes Discovery Project:

. Developed efficient synthetic methods to prepare quindolone,

cryptolepine and anthranilic Acid analogues for SAR evaluation;

involved in writing and editing patents

. Designed, synthesized and scaled-up masoprocol analogues to support

preclinical development

Brandeis University, Waltham, MA

1992-1996

RA & TA, Department of Chemistry Advisor: Prof. Barry Snider

. First total synthesis of pyridoxatin and its analogues, effective free

radical scavengers

. First total synthesis of leporin A, an anti-insectan against the corn

earworm

. First synthesis of raikovenal, preraikovenal and epiraikovenal

. Taught undergraduate organic chemistry lab

EDUCATION

Ph.D. and M.S. Synthetic Organic Chemistry, Brandeis University, Waltham,

MA

B.S. Pharmaceutical Chemistry, East China Univ. of Sci. & Tech. Shanghai,

P.R. China

PATENTS

1) Moser, H; Lu, Q.; Patten, P.; Wang, D.; Kasar, R.; Kaldor, S.;

Patterson, B.; "Preparation of antibacterial agents" PCT Int. Appl.

(2008), WO 200******* A2 20081218,

2) Mavunkel, B.; Perumattam, J.; Lu, Q; Dugar S.; Goyal, B.; Wang, D.;

Sarvajit C.; Luedtke, G.; Nashashibi, I.; Tester, R.; Tan, X.

"Azaindole derivatives as inhibitors of p38 kinase" Pub. No.:

US2005/0288299 A1, Pub. Date: Dec. 29, 2005

3) Sarvajit C.; Dugar S.; Lu, Q.; Luedtke, G.; Mavunkel, B.; Perumattam,

J.; Tester, R.; "Indole-type derivatives as inhibitors of p38 kinase"

PCT Int. Appl. (2004), WO 200******* A2, pp117.

4) Mavunkel, B.; Sarvajit C.; Perumattam, J.; Dugar S.; Lu, Q.; Liang, X.

"Benzofuran derivatives as inhibitors of p38-alpha kinase" Pub. No.:

US 2003/0158417 A1, Pub. Date: Aug. 21, 2003

5) Luedtke, G.; Tester, R.; Dugar S.; Lu, Q; Perumattam, J.; Tan, X.;

"Indole-type inhibitors of p38 kinase" Pub. No.: US 2003/0100588 A1,

Pub. Date: May 29, 2003

6) Dugar S.; Perumattam, J.; Luedtke, G.; Tan, X.; Lu, Q; "Inhibitors of

p38 kinase" Pub. No.: US 2003/0092717 A1, Pub. Date: May 15, 2003

7) Mavunkel, B.; Sarvajit C.; Perumattam, J.; Sundeep D.; Lu, Q.; Liang,

X. "Indole-type derivatives as inhibitors of p38 kinase" PCT Int.

Appl. (2000), WO 200******* A1, 85 pp.

8) Bierer, D. E.; Moinet, G.; Dubenko, L. G.; Botton, G.; Patereau, G.;

Doare, L.; Kergoat, M.; Mesangeau, D.; Lu, Q. "Piperazine

Derivatives useful as Hypoglycemic Agents" PCT Int. Appl. (1999), WO

9931096 A1, 420 pp.

PUBLICATIONS

1) Tan, X; Tester, R. W.; Luedtke, G. R.; Chakravarty, S.; Mavunkel, B.

J.; Perumattam, J. J.; Lu, Q.; Nashashibi, I.; Jung, J.; Hu, Jie;

Liclican, A.; Almirez, R.; Tabora, J.; Tran, V.; Laney, M.; Levy, D.

E.; Dugar, S.; "Design and synthesis of piperazine-indole p38-alpha

MAP kinase inhibitors with improved pharmacokinetic profiles" Bioorg.

Med. Chem. Lett. 2010, 20, 828.

2) Mavunkel, B. J.; Perumattam, J. J.; Tan, X.; Luedtke, G. R.; Lu, Q.;

Lim, D.; Kizer, D.; Dugar, S.; Chakravarty, S.; Xu, Y. J.; Jung, J.;

Liclican, A.; Levy, D. E.; Tabora, J. "Piperidine-based heterocyclic

oxalyl amides as potent p38-alpha MAP kinase inhibitors" Bioorg. Med.

Chem. Lett. 2010, 20, 1059

3) Lu, Q.; Chen, Z.; Perumattam, J.; Wang, D-X.; Liang, W.; Xu, Y-J.; Do,

S.; Bonaga, L.; Higaki, J.; Dong, H.; Liclican, A.; Sideris, S.;

Laney, M.; Dugar, S.; Mavunkel, B.; Levy, D. E. "Aryl-Indolyl

Maleimides as Inhibitors of CaMKII ?: Part 3: Importance of the

indole orientation" Bioorg. Med. Chem. Lett. 2008, 18, 2399.

4) Levy, D.E; Wang, D-X.; Lu, Q.; Chen, Z.; Perumattam, J.; Xu, Y-J.;

Liclican, A.; Higaki, J.; Dong, H.; Laney, M.; Mavunkel, B.; Dugar,

S.; "Aryl-Indolyl Maleimides as Inhibitors of CaMKII ?: Part 1: SAR

of the Aryl Region" Bioorg. Med. Chem. Lett. 2008, 18, 2390.

5) Levy, D. E.; Wang, D-X.; Lu, Q.; Chen, Z.; Perumattam,J.; Xu, Y-J.;

Higaki, J.; Dong, H.; Liclican, A.; Laney, M.; Mavunkel, B.; Dugar,

S.; "Aryl-Indolyl Maleimides as Inhibitors of CaMKII ?: Part 2: SAR

of the Amine Tether" Bioorg. Med. Chem. Lett. 2008, 18, 2395.

6) Mavunkel, B.; Xu, Y-J.; Goyal, B.; Lim, Lu, Q.; Chen, Z.; Wang, D-X.;

Higaki, J.; Chakraborty, I.; Liclican, A.; Sideris, S.; Laney, M.;

Delling, U.; Catalano, R.; Higgins, L. S.; Wang, H.; Wang, J.; Feng,

Y.; Dugar, S.; and Daniel E. Levy, D. E.; "Pyrimidine-based

inhibitors of CaMKIId" Bioorg. Med. Chem. Lett. 2008, 18, 2404.

7) Brahn E; Schoettler N; Mavunkel B; Banquerigo ML; Medicherla S;

Stebbins EG; Lu Q; Perumattam J; Dugar S; Schreiner GF; Protter AA.;

"Regression of collagen-induced arthritis with an inhibitor of p38-

alpha MAP kinase" Arthritis and Rheumatism 2003 48(9,S): pS346-S347

8) Lu, Q.; Ubillas, R. P.; Zhou, Y.; Dubenko, L. G.; Dener, J. M.;

Bierer, D. B. "Synthetic Derivatives of Irlbacholine: A Novel

Antifungal Plant Metabolite Isolated from Irlbachia alata" J. Nat.

Prod. 1999, 62, 824.

9) Fort, D. M.; Litvak, J.; Lu, Q.; Phuan, P. W.; Cooper, R.; Bierer, D.

E. "Isolation and Unambiguous Synthesis of Cryptolepinone: An

Oxidation Artifact of Cryptolepine" J. Nat. Prod. 1998, 61, 1577.

10) Bierer, D.; Dubenko, L.; Zhang, P.; Lu, Q.; Imbach, P. A. et al.

"Antihyperglycemic Activity of Cryptolepine Analogues: an

Ethnobotanical Lead Structure Isolated from Cryptolepis Sanguinolenta"

J. Med. Chem. 1998, 41, 2754.

11) Bierer, D.; Fort, D. M.; Mendez, C. D.; Luo, J.; Imbach, P. A.;

Dubenko, L. G.; Gerber, E.; Lu, Q.; Zhang, P. et al. "Ethnobotanical-

directed Discovery of the Antihyperglycemic Properties of

Cryptolepine: its Isolation from Cryptolepis Sanguinolenta, synthesis

and in vitro and in vivo Activities" J. Med. Chem. 1998, 41, 894.

12) Snider, B. B.; Lu, Q. "Syntheses of Raikovenal, Preraikovenal, and

Epiraikovenal" Synthe. Commun. 1997, 27, 1583.

13) Snider, B. B.; Lu, Q. "Total Synthesis of Leporin A" J. Org. Chem.

1996, 61, 2839.

14) Snider, B. B.; Lu, Q. "Total Synthesis of Pyridoxatin" J. Org. Chem.

1994, 59, 8065.

15) Snider, B. B.; Lu, Q. "A Two-Step Synthesis of Pyridoxatin

Analogues" Tetrahedron Lett. 1994, 35, 531.

POSTERS AND PRESENTATION

1) Lopez, Z.; Gomez, M.; Kostrob, C.; Armstrong. E.; Miller, G.; Reyes,

N.; Lu. Q.; Moser, H.; Miller, L.; Halasohoris, S.; Mojgan. Z.; Heine,

H. S.; Patten, P. "Potency and efficacy of small molecule inhibitors

of the gram-negative bacterial enzyme LpxC against Yersinia Pestis and

other Enterobacteriaceae" Poster presentation, the Chemical and

Biological Defense Science and Technology (CBD S&T) Conference,

Dallas, Texas, November 2009

2) Lopez, Z.; Gomez, M.; Armstrong. E.; Miller, G.; Reyes, N.; Lu. Q.;

Moser, H.; Miller, L.; Halasohoris, S.; Mojgan. Z.; Heine, H. S.;

Patten, P. "Small molecule LpxC inhibitors of Burkholderia Mallei and

Burkholderia Pseudomallei: in vitro and in vivo potency and efficacy"

Poster presentation, the Chemical and Biological Defense Science and

Technology (CBD S&T) Conference, Dallas, Texas, November 2009

3) Lu, Q.; Mavunkel, B.; Sarvajit C.; Perumattam, J.; Luedtke, G.; Chen,

Z.; Xu, Y.; Dugar, S.; Protter, A.; Schreiner, G.; "SAR and

Biological Studies of Indole-type p38 Kinase Inhibitors" Poster

Presentation, Gordon Research Conference, Medicinal Chemistry, New

London, NH, Aug, 2005

4) Higaki, J.; Xu, Y.; Chakraborty, I.; Dong, H.; Laseki, M.; Laney, M.;

Levy, D. Lu, Q.; Mavunkel, B.; Dugar, S.; Higgins, L.; "Inhibition of

Calmodulin-dependant Kinase II?" Poster Presentation, Structural

Biology Symposium, Vanderbilt University, Tennessee, July. 2005

5) Dugar, S.; Mavunkel, B.; Sarvajit C.; Perumattam, J.; Luedtke, G.; Lu,

Q.; Chen, Z.; Xu, Y.; Protter, A.; Schreiner, G.; "p38? MAP kinase

inhibitors: From discovery to the clinic" Presentation, 229th ACS

National Meeting, San Diego, CA, March. 2005

6) Lu, Q.; Mavunkel, B.; Sarvajit C.; Perumattam, J.; Luedtke, G.; Chen,

Z.; Xu, Y.; Dugar, S.; Protter, A.; Schreiner, G.; "Discovery and

biological evaluation of p38? MAP kinase inhibitors SX-011" Poster

Presentation, 228th ACS National Meeting, Philadelphia, PA, Aug. 2004

7) Brahn. E.; Schoettler, Mavunkel, B.; Lu, Q.; Manquerigo, ML.;

Medicherla, S.; Stebbins, L.; Perumattam, J.; Dugar, S.; Schreiner,

DF.; Protter, AA. "Inhibition of Collagen-Induced Arthritis with an

Inhibitor of p38? MAP Kinase" Poster Presentation, American College of

Rheumatology, Orlando, Oct. 2003



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